2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  3. PPAR
  4. Tesaglitazar

Tesaglitazar 是一种 PPARα/γ 双靶点激动剂，对大鼠 PPARα 的 EC50 为 13.4 μM，对人 PPARα 的 EC50 为 3.6 μM。Tesaglitazar 通过激活 PPARα 和 PPARγ 受体，影响脂质和葡萄糖代谢，并具有改善血糖、缓解疼痛的潜力。Tesaglitazar 可用于诱导体内肿瘤模型，并能够用于 2 型糖尿病、血脂异常以及神经病理性疼痛的研究。

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Tesaglitazar

Tesaglitazar Chemical Structure

CAS No. : 251565-85-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥809
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1 mg ￥500
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5 mg ￥900
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10 mg ￥1350
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25 mg ￥2700
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50 mg ￥4250
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100 mg ￥5950
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200 mg   询价  
500 mg   询价  

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Tesaglitazar 相关抗体

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PPARα PPARβ/δ PPARγ PPAR PPARδ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Tesaglitazar is a dual-target PPARα/γ agonist with an EC50 of 13.4 μM for rat PPARα and 3.6 μM for human PPARα. Tesaglitazar affects lipid and glucose metabolism by activating PPARα and PPARγ receptors, and has the potential to improve blood sugar and relieve pain. Tesaglitazar can be used to induce in vivo tumor models and can be used in the study of type 2 diabetes, dyslipidemia, and neuropathic pain[1][2][3].

IC50 & Target

EC50: 13.4 μM (rat PPARα), 3.6 μM (human PPARα), 0.2 μM (PPARγ)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CV-1 EC50
0.704 μM
Compound: (S)-tesaglitazar
Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay
Agonist activity at human PPARgamma ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay
[PMID: 18826205]
CV-1 EC50
3.124 μM
Compound: (S)-tesaglitazar
Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay
Agonist activity at human PPARalpha ligand binding domain expressed in african green monkey CV1 cells co-transfected with fused Gal4-DBD by transactivation assay
[PMID: 18826205]
HEK293 EC50
0.36 μM
Compound: (S)-2b
Agonist activity at GAL4N fused human PPARgamma LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay
Agonist activity at GAL4N fused human PPARgamma LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay
[PMID: 28539218]
HEK293 EC50
3.8 μM
Compound: (S)-2b
Agonist activity at GAL4N fused human PPARalpha LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay
Agonist activity at GAL4N fused human PPARalpha LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay
[PMID: 28539218]
HepG2 EC50
0.013 μM
Compound: tesaglitazar
Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay
Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay
[PMID: 18805005]
HepG2 EC50
0.82 μM
Compound: tesaglitazar
Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay
Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay
[PMID: 18805005]
HepG2 EC50
3528 nM
Compound: 3,tesaglitazar
Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay
Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assay
[PMID: 17157019]
HepG2 EC50
9798 nM
Compound: 3,tesaglitazar
Agonist activity at human PPARalpha in HepG2 cells by PPAR-GAL4 transactivation assay
Agonist activity at human PPARalpha in HepG2 cells by PPAR-GAL4 transactivation assay
[PMID: 17157019]
体外研究
(In Vitro)

Tesaglitazar 介导 PPARα 转录激活，靶向大鼠和人 PPARα 的 EC50 分别为 13.4 μM 和 3.6μM，靶向大鼠和人 PPARγ 的 EC50 约为 0.2 μM[1]。
Tesaglitazar (2 μM；预处理 6 小时) 在钴摄取实验中，可显著抑制 10 μM Capsaicin (HY-10448) 诱发的背根神经节 (DRG) 神经元钴内流，且该抑制作用呈 PPARα和 PPARγ依赖性[3]。

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

Tesaglitazar 相关抗体:
体内研究
(In Vivo)

Tesaglitazar (0.3-10 μmol/kg；po；每日 1 次；104 周) 在 Wistar Hannover Galas 大鼠中诱导大鼠皮下间质肉瘤 (纤维肉瘤)，同时还会引发多种非肿瘤性变化，如心肌肥大、肝脏改变等[1]。
Tesaglitazar (1、10 μmol/kg；po；每日 1 次；2 或 12 周) 在 Wistar Hannover Galas 大鼠中，持续刺激 DNA 合成，使 BrdU 标记细胞增加[1]。
Tesaglitazar (50 nmol/kg；sc；每日 1 次；14 天) 在雄性 C57BL/6J 饮食诱导肥胖 (DIO) 小鼠模型中，可降低体重、食物摄入量、空腹血糖和胰岛素水平，改善胰岛素敏感性和葡萄糖代谢，对肾功能无明显影响[2]。
Tesaglitazar (5 或 100 nmol/kg；sc；单次给药) 在 DIO 小鼠模型中，高剂量 (100 nmol/kg) 诱导葡萄糖耐量急性恶化，但低剂量 (5 nmol/kg) 可降低体重、食物摄入量和空腹血糖水平，改善葡萄糖耐量[2]。
Tesaglitazar (10-20 μg/kg；腹腔注射；单次给药) 在 Streptozotocin (HY-13753) 诱导大鼠糖尿病神经病变疼痛模型中，可显著恢复机械性缩足阈值 (PWT)，且不影响血糖水平[3]。

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

Animal Model: Wistar Hannover Galas rats (6-8 weeks old; carcinogenicity model)[1]
Dosage: 0.3, 1, 3, 10 μmol/kg (dissolved in 5mM sodium hydrogen carbonate buffer solution, pH 8.5)
Administration: Oral gavage, once daily, 104 weeks
Result: Induced subcutaneous mesenchymal sarcomas (fibrosarcomas) in both male and female rats (10 μmol/kg).
Caused various non-neoplastic changes, such as myocardial hypertrophy, liver changes, and alterations in multiple organ systems.
Clinical Trial
分子量

408.47

Formula

C20H24O7S
CAS 号
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

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 200 mg/mL (489.63 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4482 mL 12.2408 mL 24.4816 mL
5 mM 0.4896 mL 2.4482 mL 4.8963 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 (sealed storage, away from moisture)。-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)

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

g

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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.08%

COA (284 KB) HNMR (132 KB) RP-HPLC (242 KB) MS (204 KB)

产品使用指南 (1538 KB)
参考文献

Tesaglitazar 相关分类

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 (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4482 mL 12.2408 mL 24.4816 mL 61.2040 mL
5 mM 0.4896 mL 2.4482 mL 4.8963 mL 12.2408 mL
10 mM 0.2448 mL 1.2241 mL 2.4482 mL 6.1204 mL
15 mM 0.1632 mL 0.8161 mL 1.6321 mL 4.0803 mL
20 mM 0.1224 mL 0.6120 mL 1.2241 mL 3.0602 mL
25 mM 0.0979 mL 0.4896 mL 0.9793 mL 2.4482 mL
30 mM 0.0816 mL 0.4080 mL 0.8161 mL 2.0401 mL
40 mM 0.0612 mL 0.3060 mL 0.6120 mL 1.5301 mL
50 mM 0.0490 mL 0.2448 mL 0.4896 mL 1.2241 mL
60 mM 0.0408 mL 0.2040 mL 0.4080 mL 1.0201 mL
80 mM 0.0306 mL 0.1530 mL 0.3060 mL 0.7651 mL
100 mM 0.0245 mL 0.1224 mL 0.2448 mL 0.6120 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.

Keywords:

Tesaglitazar251565-85-2PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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