T0901317

目录号: HY-10626 纯度: 99.93%: Data Sheet SDS COA 产品使用指南
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T0901317 是口服有效且高度选择性的 LXR 激动剂，对 LXRα 的 EC₅₀ 为 20 nM。T0901317 激活 FXR，EC₅₀ 为 5 μM。T0901317 是 RORα 和 RORγ 双重反向激动剂，K_i 值分别为 132 nM 和 51 nM。T0901317 诱导细胞凋亡 (apoptosis)，并抑制低密度脂蛋白 (LDL) 受体缺失小鼠动脉粥样硬化的发展。

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T0901317 Chemical Structure

CAS No. : 293754-55-9

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥660	In-stock
5 mg	￥375	In-stock
10 mg	￥600	In-stock
50 mg	￥1200	In-stock
100 mg	￥1950	In-stock
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T0901317 (Standard) 询价

MCE 顾客使用本产品发表的 35 篇科研文献

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RORγ RORα RORβ

生物活性
纯度 & 产品资料
参考文献

生物活性

T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα^[1]. T0901317 activates FXR with an EC₅₀ of 5 μM^[2]. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively^[3]. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice^[4]^[5].

IC₅₀ & Target

EC50: 20 nM (LXRα) and 5 μM (FXR)^[1]^[2]
Ki: 132 nM (RORα) and 51 nM (RORγ)^[3]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CHO	EC₅₀	16 nM Compound: 1, T0901317	Agonist activity at human recombinant LXRbeta expressed in CHO cells assessed as effect on secreted alkaline phosphatase by LAFbeta assay Agonist activity at human recombinant LXRbeta expressed in CHO cells assessed as effect on secreted alkaline phosphatase by LAFbeta assay	[PMID: 19853462]
CHO	EC₅₀	16 nM Compound: 3, TO901317	Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay	[PMID: 17034119]
CHO-K1	EC₅₀	0.41 μM Compound: 1, T0901317	Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 25677664]
CHO-K1	EC₅₀	0.41 μM Compound: T0901317	Agonist activity at GAL4 fused LXRbeta-LBD (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay Agonist activity at GAL4 fused LXRbeta-LBD (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 27283790]
CHO-K1	EC₅₀	0.49 μM Compound: 1, T0901317	Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 25677664]
CHO-K1	EC₅₀	0.49 μM Compound: T0901317	Agonist activity at GAL4 fused LXRalpha (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay Agonist activity at GAL4 fused LXRalpha (unknown origin) transfected in CHOK1 cells after 24 hrs by luciferase reporter gene assay	[PMID: 27283790]
COS-7	EC₅₀	0.011 μM Compound: T0901317	Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay	[PMID: 17416521]
COS-7	EC₅₀	0.011 μM Compound: T0901317	Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay	[PMID: 17587573]
COS-7	EC₅₀	84 % Compound: T0901317	Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay relative to GW-3965 Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay relative to GW-3965	[PMID: 17587573]
CV-1	EC₅₀	0.03 μM Compound: 1, T0901317	Agonist activity at human LXRalpha expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay Agonist activity at human LXRalpha expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay	[PMID: 26238323]
CV-1	EC₅₀	0.13 μM Compound: 1, T0901317	Agonist activity at human LXRbeta expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay Agonist activity at human LXRbeta expressed in African green monkey kidney CV1 cells co-expressing pTAL-LXRE including LXR response element incubated for 20 hrs by luciferase reporter gene assay	[PMID: 26238323]
CV-1	EC₅₀	140 nM Compound: 1a, TO-091317	Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay	[PMID: 25435151]
CV-1	EC₅₀	28 nM Compound: 1a, TO-091317	Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferase reporter gene assay Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferase reporter gene assay	[PMID: 25435151]
H4	EC₅₀	0.02 μM Compound: 1; TO-091317	Agonist activity at LXRbeta (unknown origin) expressed in human H4 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay Agonist activity at LXRbeta (unknown origin) expressed in human H4 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay	[PMID: 27011007]
H4	EC₅₀	3.6 μM Compound: 4, TO901317	Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as increase in Amyloid beta-42 formation LPECL assay Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as increase in Amyloid beta-42 formation LPECL assay	[PMID: 17723298]
H4	IC₅₀	4.5 μM Compound: 4, TO901317	Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-38 formation by LPECL assay Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-38 formation by LPECL assay	[PMID: 17723298]
H4	IC₅₀	> 40 μM Compound: 4, TO901317	Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-40 formation LPECL assay Effect on gamma-secretase activity in human H4 cells expressing APP695 assessed as reduction of Amyloid beta-40 formation LPECL assay	[PMID: 17723298]
HEK-293T	EC₅₀	0.036 μM Compound: 1, T0901317	Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	0.156 μM Compound: 1, T0901317	Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	0.25 μM Compound: T0901317	Agonist activity at GAL4-fused LXR alpha (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay Agonist activity at GAL4-fused LXR alpha (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay	10.1039/C3MD00005B
HEK-293T	EC₅₀	0.373 μM Compound: 1, T0901317	Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	0.463 μM Compound: 1, T0901317	Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	0.8 μM Compound: 4; T0901317	Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at recombinant human GAL4-DBD-fused LXRbeta-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay	[PMID: 28169169]
HEK-293T	EC₅₀	0.94 μM Compound: 4; T0901317	Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay Partial agonist activity at recombinant human GAL4-DBD-fused LXRalpha-LBD expressed in HEK293T cells measured after 12 to 14 hrs by dual-glo luciferase reporter gene assay	[PMID: 28169169]
HEK-293T	EC₅₀	1 μM Compound: 1, T0901317	Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	5 μM Compound: 1, T0901317	Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	EC₅₀	6 μM Compound: 1, T0901317	Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay	[PMID: 24239186]
HEK-293T	IC₅₀	1.7 μM Compound: T0901317	Inverse agonist activity at GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay Inverse agonist activity at GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay	10.1039/C3MD00005B
HEK-293T	IC₅₀	2 μM Compound: T0901317	Inverse agonist activity at GAL4-fused ROR alpha (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay Inverse agonist activity at GAL4-fused ROR alpha (unknown origin) expressed in HEK293T cells after 20 hrs by luciferase reporter gene assay	10.1039/C3MD00005B
HEK293	EC₅₀	0.01 μM Compound: T0901317	Activity against LXR alpha transiently transfected in HEK293 cells Activity against LXR alpha transiently transfected in HEK293 cells	[PMID: 16386417]
HEK293	EC₅₀	0.019 μM Compound: 1a	Agonist activity at human LXRbeta in HEK293 cells assessed as Gal4 transactivation Agonist activity at human LXRbeta in HEK293 cells assessed as Gal4 transactivation	[PMID: 20350005]
HEK293	EC₅₀	0.036 μM Compound: 8, T0901317	Agonist activity at PXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at PXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	0.053 μM Compound: 1a	Agonist activity at human LXRalpha in HEK293 cells assessed as Gal4 transactivation Agonist activity at human LXRalpha in HEK293 cells assessed as Gal4 transactivation	[PMID: 20350005]
HEK293	EC₅₀	0.066 μM Compound: 3, T0901317	Agonist activity at human LXR-beta transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay Agonist activity at human LXR-beta transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 26288691]
HEK293	EC₅₀	0.09 μM Compound: 3, T1317	Transactivational agonist activity at human LXRbeta transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay Transactivational agonist activity at human LXRbeta transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay	[PMID: 22873709]
HEK293	EC₅₀	0.12 μM Compound: T0901317	Agonist activity at human LXR-beta expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay Agonist activity at human LXR-beta expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 24702856]
HEK293	EC₅₀	0.16 μM Compound: 8, T0901317	Agonist activity at LXRbeta (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at LXRbeta (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	0.21 μM Compound: 3, T0901317	Agonist activity at human LXR-alpha transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay Agonist activity at human LXR-alpha transfected in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 26288691]
HEK293	EC₅₀	0.23 μM Compound: 5; T0901317	Agonist activity at human LXRbeta transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at human LXRbeta transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 26905831]
HEK293	EC₅₀	0.27 μM Compound: 5; T0901317	Agonist activity at human PXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at human PXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 26905831]
HEK293	EC₅₀	0.29 μM Compound: T0901317	Agonist activity at human LXR-alpha expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay Agonist activity at human LXR-alpha expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 24702856]
HEK293	EC₅₀	0.34 μM Compound: 3, T1317	Transactivational agonist activity at human LXRalpha transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay Transactivational agonist activity at human LXRalpha transfected in HEK293 cells expressing CMX-Gal4N assessed as luciferase activity after 16 hrs by reporter gene assay	[PMID: 22873709]
HEK293	EC₅₀	0.37 μM Compound: 8, T0901317	Agonist activity at LXRalpha (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at LXRalpha (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	0.4 μM Compound: 5; T0901317	Agonist activity at human LXRalpha transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at human LXRalpha transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 26905831]
HEK293	EC₅₀	0.46 μM Compound: 8, T0901317	Agonist activity at RoRc (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at RoRc (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	1.3 μM Compound: 8, T0901317	Agonist activity at FXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at FXR (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	3.4 μM Compound: 5; T0901317	Agonist activity at human FXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay Agonist activity at human FXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay	[PMID: 26905831]
HEK293	EC₅₀	5 μM Compound: 8, T0901317	Agonist activity at RoRa (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at RoRa (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	6 μM Compound: 8, T0901317	Agonist activity at RoRb (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay Agonist activity at RoRb (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 NR reporter cell-based assay	[PMID: 24502334]
HEK293	EC₅₀	85 nM Compound: T0901317	Agonist activity at human LXRbeta expressed in HEK293 cells by luciferase reporter gene assay Agonist activity at human LXRbeta expressed in HEK293 cells by luciferase reporter gene assay	[PMID: 25305688]
HEK293	IC₅₀	3 μM Compound: 5; T0901317	Inverse agonist activity at human RORgamma transfected in HEK293 cells after 24 hrs by beta galactosidase luciferase reporter gene assay Inverse agonist activity at human RORgamma transfected in HEK293 cells after 24 hrs by beta galactosidase luciferase reporter gene assay	[PMID: 26905831]
HEK293	IC₅₀	6.5 μM Compound: T0901317	Inverse agonist activity at human ROR-gamma1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay Inverse agonist activity at human ROR-gamma1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 24702856]
HEK293	IC₅₀	> 20 μM Compound: T0901317	Inverse agonist activity at human ROR-alpha1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay Inverse agonist activity at human ROR-alpha1 expressed in HEK293 cells after 16 hrs by luciferase reporter gene assay	[PMID: 24702856]
HeLa	EC₅₀	17 nM Compound: 1a, TO-091317	Transactivation of LXR (unknown origin) expressed in human HeLa cells by ABCA1 LXREx3 reporter assay Transactivation of LXR (unknown origin) expressed in human HeLa cells by ABCA1 LXREx3 reporter assay	[PMID: 25435151]
HepG2	EC₅₀	0.02 μM Compound: 1; TO-091317	Agonist activity at LXRalpha (unknown origin) expressed in human HepG2 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay Agonist activity at LXRalpha (unknown origin) expressed in human HepG2 cells co-expressing ABCA1 promoter measured after 48 hrs by cell-based transactivation assay	[PMID: 27011007]
HepG2	EC₅₀	0.137 μM Compound: 1 (TO901317)	Effect on triglyceride accumulation in human HepG2 cells Effect on triglyceride accumulation in human HepG2 cells	[PMID: 19962892]
HepG2	EC₅₀	0.137 μM Compound: 1, T0901317	Increase in cellular triglyceride level in human HepG2 cells Increase in cellular triglyceride level in human HepG2 cells	[PMID: 20005711]
HepG2	EC₅₀	0.14 μM Compound: 1a	Induction of [3H]cholesterol efflux in human HepG2 cells loaded with ac-LDL assessed as lipid accumulation Induction of [3H]cholesterol efflux in human HepG2 cells loaded with ac-LDL assessed as lipid accumulation	[PMID: 20350005]
HepG2	EC₅₀	104 nM Compound: 1, T0901317	Increase in cellular triglyceride level in human HepG2 cells Increase in cellular triglyceride level in human HepG2 cells	[PMID: 20006495]
HepG2	EC₅₀	107 nM Compound: 1, T0901317	Increase in triglyceride level in human HepG2 cells Increase in triglyceride level in human HepG2 cells	[PMID: 20382019]
HepG2	EC₅₀	137 nM Compound: 1, T0901317	Effect on triglyceride accumulation in human HepG2 cells Effect on triglyceride accumulation in human HepG2 cells	[PMID: 18973288]
HepG2	EC₅₀	137 nM Compound: 3, TO901317	Effect on LXR-mediated intracellular triglyceride level in human HepG2 cells after 4 to 5 days Effect on LXR-mediated intracellular triglyceride level in human HepG2 cells after 4 to 5 days	[PMID: 18023179]
HepG2	EC₅₀	190 nM Compound: 6, GW3965	Agonist activity at Homo sapiens (human) LXRalpha expressed in HepG2 cells assessed as transactivation of CYP7A1 gene expression after 48 hr by luciferase reporter gene assay Agonist activity at Homo sapiens (human) LXRalpha expressed in HepG2 cells assessed as transactivation of CYP7A1 gene expression after 48 hr by luciferase reporter gene assay	10.1007/s00044-012-0359-5
HepG2	EC₅₀	61 nM Compound: 1, T0901317	Effect on SREBP1c gene expression in human HepG2 cells Effect on SREBP1c gene expression in human HepG2 cells	[PMID: 18973288]
HepG2	EC₅₀	67 nM Compound: 3, TO901317	Effect on SREBP1c gene expression in human HepG2 cells Effect on SREBP1c gene expression in human HepG2 cells	[PMID: 18023179]
Huh-7	EC₅₀	0.067 μM Compound: 3, TO901317	Induction of SREBP-1C mRNA expression in human HuH7 cells after 18 hrs by RT-PCR Induction of SREBP-1C mRNA expression in human HuH7 cells after 18 hrs by RT-PCR	[PMID: 19394832]
Huh-7	EC₅₀	0.135 μM Compound: 1, T0901317	Agonist activity at human Gal4-LBD fused LXRbeta LBD expressed in Huh7 cells by transient transactivation assay Agonist activity at human Gal4-LBD fused LXRbeta LBD expressed in Huh7 cells by transient transactivation assay	[PMID: 20005711]
Huh-7	EC₅₀	0.135 μM Compound: 3, TO901317	Agonist activity at human LXRalpha ligand binding domain (205-448) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay Agonist activity at human LXRalpha ligand binding domain (205-448) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay	[PMID: 19394832]
Huh-7	EC₅₀	0.14 μM Compound: 1 (TO901317)	Agonist activity at human LXRalpha ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay Agonist activity at human LXRalpha ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay	[PMID: 19962892]
Huh-7	EC₅₀	0.14 μM Compound: 1, T0901317	Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 18973288]
Huh-7	EC₅₀	0.14 μM Compound: 1a	Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 20350005]
Huh-7	EC₅₀	0.17 μM Compound: 1 (TO901317)	Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay Agonist activity at human LXRbeta ligand binding domain expressed in human HuH7 cells co-transfected with Gal4-DBD by transactivation assay	[PMID: 19962892]
Huh-7	EC₅₀	0.17 μM Compound: 1, T0901317	Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 18973288]
Huh-7	EC₅₀	0.17 μM Compound: 1, T0901317	Agonist activity at human Gal4-LBD fused LXRalpha LBD expressed in Huh7 cells by transient transactivation assay Agonist activity at human Gal4-LBD fused LXRalpha LBD expressed in Huh7 cells by transient transactivation assay	[PMID: 20005711]
Huh-7	EC₅₀	0.17 μM Compound: 1a	Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay	[PMID: 20350005]
Huh-7	EC₅₀	0.178 μM Compound: 3, TO901317	Agonist activity at human LXRbeta ligand binding domain (219-462) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay Agonist activity at human LXRbeta ligand binding domain (219-462) expressed in human HuH7 cells co-transfected with Gal4-DBD by luciferase transactivation assay	[PMID: 19394832]
Huh-7	EC₅₀	135 nM Compound: 3, TO901317	Agonist activity at human LXRalpha expressed in Huh7 cells by Gal4 transactivation assay Agonist activity at human LXRalpha expressed in Huh7 cells by Gal4 transactivation assay	[PMID: 18023179]
Huh-7	EC₅₀	170 nM Compound: 1, T0901317	Agonist activity at human recombinant LXRbeta ligand binding domain in HuH7 cells by Gal4 transactivation assay Agonist activity at human recombinant LXRbeta ligand binding domain in HuH7 cells by Gal4 transactivation assay	[PMID: 20382019]
Huh-7	EC₅₀	178 nM Compound: 3, TO901317	Agonist activity at human LXRbeta expressed in Huh7 cells by Gal4 transactivation assay Agonist activity at human LXRbeta expressed in Huh7 cells by Gal4 transactivation assay	[PMID: 18023179]
Huh-7	EC₅₀	36 nM Compound: 1, T0901317	Upregulation of SREB1c mRNA level in human HuH7 cells Upregulation of SREB1c mRNA level in human HuH7 cells	[PMID: 20382019]
J774	EC₅₀	27 nM Compound: 1, T0901317	Agonist activity at LXRbeta in mouse J774 cells assessed as upregulation of ABCA1 mRNA expression Agonist activity at LXRbeta in mouse J774 cells assessed as upregulation of ABCA1 mRNA expression	[PMID: 19853462]
J774	EC₅₀	35 nM Compound: 1, T0901317	Upregulation of ABCA1 mRNA level in mouse J774 cells Upregulation of ABCA1 mRNA level in mouse J774 cells	[PMID: 20382019]
J774	EC₅₀	35 nM Compound: 3, TO901317	Effect on ABCA1 gene expression in mouse J774 cells Effect on ABCA1 gene expression in mouse J774 cells	[PMID: 18023179]
J774.A1	EC₅₀	0.034 μM Compound: 3, TO901317	Induction of ABCA1 mRNA expression in mouse J774A1 cells after 18 hrs by RT-PCR Induction of ABCA1 mRNA expression in mouse J774A1 cells after 18 hrs by RT-PCR	[PMID: 19394832]
J774.A1	EC₅₀	35 nM Compound: 1	Induction of ABCA1 mRNA expression in mouse J774A1 cells Induction of ABCA1 mRNA expression in mouse J774A1 cells	[PMID: 19932617]
L02	EC₅₀	0.53 μM Compound: TO901317	Transactivation of recombinant GAL4-fused human LXRalpha LBD (163 to 447 residues) expressed in human L02 cells measured after 24 hrs by luciferase reporter gene assay Transactivation of recombinant GAL4-fused human LXRalpha LBD (163 to 447 residues) expressed in human L02 cells measured after 24 hrs by luciferase reporter gene assay	[PMID: 31095389]
LS180	IC₅₀	> 50 μM Compound: 6; T0901317	Cytotoxicity against human LS180 cells assessed as effect on cell viability measured after 24 hrs by MTT assay Cytotoxicity against human LS180 cells assessed as effect on cell viability measured after 24 hrs by MTT assay	[PMID: 27497733]
PBMC	EC₅₀	3 μM Compound: 1, T0901317	Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA	[PMID: 24239186]
PBMC	EC₅₀	> 20 μM Compound: 1, T0901317	Cytotoxicity against human PBMC assessed as effect on cell physiology after 48 hrs by CellTiter-Glo assay Cytotoxicity against human PBMC assessed as effect on cell physiology after 48 hrs by CellTiter-Glo assay	[PMID: 24239186]
PBMC	EC₅₀	> 20 μM Compound: 1, T0901317	Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA Inhibition of IFNgamma production in human PBMC after 48 hrs by Sandwich ELISA	[PMID: 24239186]
Platelet	IC₅₀	> 50 nM Compound: T0901317	Inhibition of collagen-induced platelet aggregation in human platelet suspension preincubated for 10 mins followed by collagen stimulation by light transmission-based assay Inhibition of collagen-induced platelet aggregation in human platelet suspension preincubated for 10 mins followed by collagen stimulation by light transmission-based assay	[PMID: 32463237]
SH-SY5Y	EC₅₀	0.075 μM Compound: 2, T0901317	Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay	[PMID: 19264481]
SH-SY5Y	EC₅₀	0.085 μM Compound: 2, T0901317	Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay	[PMID: 19264481]
SH-SY5Y	IC₅₀	> 50 μM Compound: 6; T0901317	Cytotoxicity against human SH-SY5Y cells assessed as effect on cell viability measured after 24 hrs by MTT assay Cytotoxicity against human SH-SY5Y cells assessed as effect on cell viability measured after 24 hrs by MTT assay	[PMID: 27497733]
THP-1	EC₅₀	0.033 μM Compound: T0901317	Induction of cholesterol efflux in THP1 cells after 18 hrs Induction of cholesterol efflux in THP1 cells after 18 hrs	[PMID: 17416521]
THP-1	EC₅₀	0.033 μM Compound: T0901317	Induction of cholesterol efflux in THP1 cells Induction of cholesterol efflux in THP1 cells	[PMID: 17587573]
THP-1	EC₅₀	0.044 μM Compound: 1 (TO901317)	Effect on ABCA1 gene expression in human differentiated THP1 cells Effect on ABCA1 gene expression in human differentiated THP1 cells	[PMID: 19962892]
THP-1	EC₅₀	0.044 μM Compound: 1, T0901317	Induction of ABCA1 mRNA upregulation in human THP1 cells Induction of ABCA1 mRNA upregulation in human THP1 cells	[PMID: 20005711]
THP-1	EC₅₀	0.044 μM Compound: 1a	Induction of ABCA1 expression in human THP1 cells Induction of ABCA1 expression in human THP1 cells	[PMID: 20350005]
THP-1	EC₅₀	3 nM Compound: 1 (TO901317)	Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL	[PMID: 19962892]
THP-1	EC₅₀	3 nM Compound: 1 (TO901317)	Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL relative to TO901317 Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL relative to TO901317	[PMID: 19962892]
THP-1	EC₅₀	3 nM Compound: 1, T0901317	Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL	[PMID: 18973288]
THP-1	EC₅₀	35 nM Compound: 1, T0901317	Induction of ABCA1 mRNA upregulation in human THP1 cells Induction of ABCA1 mRNA upregulation in human THP1 cells	[PMID: 20006495]
THP-1	EC₅₀	44 nM Compound: 1, T0901317	Effect on ABCA1 gene expression in human differentiated THP1 cells Effect on ABCA1 gene expression in human differentiated THP1 cells	[PMID: 18973288]
THP-1	EC₅₀	44 nM Compound: 3, TO901317	Effect on ABCA1 gene expression in human THP1 cells Effect on ABCA1 gene expression in human THP1 cells	[PMID: 18023179]
THP-1	IC₅₀	100 nM Compound: 3, T1317	Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA	[PMID: 18800767]
THP-1	IC₅₀	26 μM Compound: 3, T0901317	Transrepression activity of LXR in human THP1 cells assessed as inhibition of LPS-induced IL-6 level after 18 hrs by ELISA Transrepression activity of LXR in human THP1 cells assessed as inhibition of LPS-induced IL-6 level after 18 hrs by ELISA	[PMID: 26288691]
THP-1	IC₅₀	> 10 μM Compound: 3, T1317	Transrepressional activity at LXR in human TPA-activated THP1 cells assessed as inhibition of LPS-induced IL6 production incubated for 6 hrs prior to LPS-challenge measured after 18 hrs by ELISA Transrepressional activity at LXR in human TPA-activated THP1 cells assessed as inhibition of LPS-induced IL6 production incubated for 6 hrs prior to LPS-challenge measured after 18 hrs by ELISA	[PMID: 22873709]

体外研究
(In Vitro)

T0901317 (5-50 μM；72 小时) 以剂量依赖性和时间依赖性方式显著抑制 CaOV3、SKOV3、A2780 (人卵巢癌细胞系) 的细胞增殖^[5]。
T0901317 (10 μM；24-72 小时) 降低处于 S 期的细胞百分比并增加处于 G0/G1 期的细胞百分比，表明细胞周期停滞在 G1-S 检查点。G0/G1期细胞百分比呈时间依赖性增加^[5]。
T0901317 (10-40 μM；24 hours) 导致细胞早期凋亡显著增加^[5]。
T0901317 (5-40 μM；48 小时) 导致 p21 和 p27 蛋白表达在 48 小时后以剂量依赖性方式增加^[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[5]

Cell Line:	A2780, CaOV3 and SKOV3 ovarian cancer cell lines
Concentration:	5, 10, 20, 40 or 50 μM
Incubation Time:	72 hours
Result:	Inhibited cellular proliferation in all cell lines in a dose-dependent and time-dependent manner.

Cell Cycle Analysis^[5]

Cell Line:	A2780, CaOV3 and SKOV3 cells
Concentration:	10 μM
Incubation Time:	24, 48 or 72 hours
Result:	Decreased the percentage of cells in S phase and increased the percentage of cells in the G0/G1 phase.

Apoptosis Analysis^[5]

Cell Line:	CaOV3 cells
Concentration:	10 to 40 μM
Incubation Time:	24 hours
Result:	Resulted in a significant increase of cells in early apoptosis.

Western Blot Analysis^[5]

Cell Line:	CaOV3 cells
Concentration:	5 to 40 μM
Incubation Time:	48 hours
Result:	Resulted in an increase of p21 and p27 protein expression in a dose-dependent manner.

体内研究
(In Vivo)

T0901317 (10 毫克/公斤/天；口服；持续 12 周) 抑制动脉粥样硬化的进展^[5]。
T0901317 (腹腔注射；50 毫克/公斤；每周两次，持续 7 天) 可以保护雄性 C57BL/6 小鼠免受高脂饮食诱导的肥胖和胰岛素抵抗^[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	8- to 10-week-old LDL receptor null mice^[5]
Dosage:	10 mg/kg
Administration:	Orally; daily; for 12 weeks
Result:	Inhibited the progression of atherosclerosis.

分子量

481.33

Formula

C₁₇H₁₂F₉NO₃S

CAS 号

293754-55-9

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (207.76 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

Ethanol 中的溶解度 : 100 mg/mL (207.76 mM; 超声助溶)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0776 mL	10.3879 mL	20.7758 mL
5 mM	0.4155 mL	2.0776 mL	4.1552 mL
10 mM	0.2078 mL	1.0388 mL	2.0776 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (6.23 mM); 澄清溶液

此方案可获得 ≥ 3 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (6.23 mM); 澄清溶液

此方案可获得 ≥ 3 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (6.23 mM); 澄清溶液

此方案可获得 ≥ 3 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
方案四

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.5 mg/mL (5.19 mM); 悬浊液; 超声助溶
方案五

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.19 mM); 澄清溶液

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.93%

选择批次：

Data Sheet (652 KB) SDS (393 KB)

COA (290 KB) HNMR (272 KB) RP-HPLC (242 KB) LCMS (94 KB)

产品使用指南 (1538 KB)

参考文献

[1]. J R Schultz, et al. Role of LXRs in Control of Lipogenesis. Genes Dev. 2000 Nov 15;14(22):2831-8. [Content Brief]

[2]. Keith A Houck, et al. T0901317 Is a Dual LXR/FXR Agonist. Mol Genet Metab. Sep-Oct 2004;83(1-2):184-7. [Content Brief]

[3]. Naresh Kumar, et al. The Benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] Is a Novel Retinoic Acid Receptor-Related Orphan Receptor-Alpha/Gamma Inverse Agonist. Mol Pharmacol. 2010 Feb;77(2):228-36. [Content Brief]

[4]. Rough JJ, et al. Anti-proliferative effect of LXR agonist T0901317 in ovarian carcinoma cells. J Ovarian Res. 2010 May 26;3:13. [Content Brief]

[5]. Todd G Kirchgessner, et al. Beneficial and Adverse Effects of an LXR Agonist on Human Lipid and Lipoprotein Metabolism and Circulating Neutrophils. Cell Metab. 2016 Aug 9;24(2):223-33. [Content Brief]

[6]. Mingming Gao, et al. The Liver X Receptor Agonist T0901317 Protects Mice From High Fat Diet-Induced Obesity and Insulin Resistance. AAPS J. 2013 Jan;15(1):258-66. [Content Brief]

T0901317 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO / Ethanol	1 mM	2.0776 mL	10.3879 mL	20.7758 mL	51.9394 mL
	5 mM	0.4155 mL	2.0776 mL	4.1552 mL	10.3879 mL
	10 mM	0.2078 mL	1.0388 mL	2.0776 mL	5.1939 mL
	15 mM	0.1385 mL	0.6925 mL	1.3851 mL	3.4626 mL
	20 mM	0.1039 mL	0.5194 mL	1.0388 mL	2.5970 mL
	25 mM	0.0831 mL	0.4155 mL	0.8310 mL	2.0776 mL
	30 mM	0.0693 mL	0.3463 mL	0.6925 mL	1.7313 mL
	40 mM	0.0519 mL	0.2597 mL	0.5194 mL	1.2985 mL
	50 mM	0.0416 mL	0.2078 mL	0.4155 mL	1.0388 mL
	60 mM	0.0346 mL	0.1731 mL	0.3463 mL	0.8657 mL
	80 mM	0.0260 mL	0.1298 mL	0.2597 mL	0.6492 mL
	100 mM	0.0208 mL	0.1039 mL	0.2078 mL	0.5194 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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