YS121

目录号: HY-111140 纯度: 99.74%: Data Sheet SDS COA 产品使用指南
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YS121 是微粒体前列腺素 E2 合酶 -1 (mPGES-1 ; IC₅₀ = 3.4 μM) 和 5- 脂氧合酶 (5-LOX ; IC₅₀ = 6.5 μM) 的双重抑制剂。YS121 与 mPGES-1 (K_D = 10-14 μM) 具有直接、可逆和特异性的结合。YS121 能剂量依赖性地抑制 IL-1β-stimulated A549 细胞中 PGE₂ 的产生，其效力表现为 EC₅₀ 值为 12 μM。YS121 可激活过氧化物酶体增殖物激活受体 (PPAR) -α 与 -γ (其 EC₅₀ 值分别为 1 μM 和 3.6 μM)。YS121 在人体全血模型和体内实验中均显示出抗炎功效，可用于炎症研究。

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YS121 Chemical Structure

CAS No. : 916482-17-2

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10 mg	￥2400	In-stock
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YS121 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Lipoxygenase 亚型特异性产品:

查看所有亚型

5-LOX 12-LOX 15-LOX

查看 PPAR 亚型特异性产品:

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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

YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC₅₀ = 3.4 μM) and 5-lipoxygenase (5-LOX; IC₅₀ = 6.5 μM). YS121 exhibits direct, reversible, and specific binding to mPGES-1 (K_D = 10-14 μM)^[1]. YS121 dose-dependently reduces PGE₂ production with an EC₅₀ of 12 μM in IL-1β-stimulated A549 cells^[2]. YS121 (compound 9) activates PPAR-α and -γ (EC₅₀ = 1 and 3.6 μM, respectively)^[3]. YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research^[1].

IC₅₀ & Target

PPAR-α

1 μM (EC₅₀)

PPAR-γ

3.6 μM (EC₅₀)

5-Lipoxygenase

6.5 μM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	12 μM Compound: 2d	Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation by cell-intact assay Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation by cell-intact assay	[PMID: 19053751]
A549	IC₅₀	3.9 μM Compound: 2d	Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay	[PMID: 19053751]
COS-7	EC₅₀	1 μM Compound: 3	Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay	[PMID: 25022880]
COS-7	IC₅₀	1 μM Compound: 2	Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay	[PMID: 25037914]
COS-7	EC₅₀	3.6 μM Compound: 3	Agonist activity at human PPARgamma LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay Agonist activity at human PPARgamma LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay	[PMID: 25022880]
COS-7	EC₅₀	3.6 μM Compound: 2	Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay	[PMID: 20307981]
COS-7	IC₅₀	3.6 μM Compound: 2	Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay	[PMID: 25037914]

体外研究
(In Vitro)

YS121 (0.3-30 μM) 是一种强效选择性抑制剂，可抑制 IL-1β-stimulated A549 细胞微粒体中的 mPGES-1，可浓度依赖性地、非竞争性地阻断 PGH₂ 至 PGE₂ 的转化，且不显著抑制其他 PGES 酶^[1]。
YS121 (0.1-30 μM) 对 PGE2 的生成呈浓度依赖性抑制，IC₅₀ 值为 3 μM，且在无 CV4151 的条件下也能中度抑制 PGE₂ 的合成^[1]。
YS121 (0.1-30 μM) 在人体全血中对 PGE₂ 的生成具有选择性抑制作用，表现为不影响 COX-2 途径产物 (6-keto PGF_1α、TxB₂) 以及 COX-1 途径产物 (12-HHT) 的合成^[1]。
YS121 (10 μM, 0-48小时) 可在 48 小时内选择性调节蛋白质表达，表现为在 24 小时后降低 COX-2 水平，但不改变 mPGES-1 的表达^[1]。

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

Western Blot Analysis^[1]

Cell Line:	interleukin-1β-stimulated human A549 cells
Concentration:	10 μM
Incubation Time:	0, 12, 24, and 48 h
Result:	Decreased the levels of COX-2 after 24 to 48 h in interleukin-1β-stimulated human A549 cells. Had no significant impact on mPGES-1 expression levels over 48 hours.

体内研究
(In Vivo)

YS121 (1.5 mg/kg，腹腔注射，建模前30分钟，单次给药) 在角叉菜胶诱发的大鼠胸膜炎模型中表现出强大的抗炎功效^[1]。

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

Animal Model:	Male adult Wistar Han rats (200-220 g) injected intraperitoneally with carrageenan^[1]
Dosage:	1.5 mg/kg
Administration:	i.p., 30 min pre-modeling, once
Result:	Significantly inhibited the exudate formation by 62 % and cell infiltration by 40 %. Reduced the levels of PGE₂, LTB₄ and 6-keto PGF_1α.

分子量

407.96

Formula

C₂₀H₂₆ClN₃O₂S

CAS 号

916482-17-2

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, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据

细胞实验：

DMSO 中的溶解度 : 125 mg/mL (306.40 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)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.4512 mL	12.2561 mL	24.5122 mL
5 mM	0.4902 mL	2.4512 mL	4.9024 mL
10 mM	0.2451 mL	1.2256 mL	2.4512 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 (protect from light)。-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

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.74%

选择批次：

Data Sheet (622 KB) SDS (393 KB)

COA (282 KB) HNMR (276 KB) LCMS (90 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Koeberle A, et al. The molecular pharmacology and in vivo activity of 2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid (YS121), a dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase. J Pharmacol Exp Ther. 2010 Mar;332(3):840-8. [Content Brief]

[2]. Chang HH, et al. Identification and development of mPGES-1 inhibitors: where we are at? Future Med Chem. 2011 Nov;3(15):1909-34.

[3]. Rau O, et al. Alpha-alkyl substituted pirinixic acid derivatives as potent dual agonists of the peroxisome proliferator activated receptor alpha and gamma. Arch Pharm (Weinheim). 2008 Mar;341(3):191-5. [Content Brief]

YS121 相关分类

Inflammation/Immunology

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	1 mM	2.4512 mL	12.2561 mL	24.5122 mL	61.2805 mL
	5 mM	0.4902 mL	2.4512 mL	4.9024 mL	12.2561 mL
	10 mM	0.2451 mL	1.2256 mL	2.4512 mL	6.1281 mL
	15 mM	0.1634 mL	0.8171 mL	1.6341 mL	4.0854 mL
	20 mM	0.1226 mL	0.6128 mL	1.2256 mL	3.0640 mL
	25 mM	0.0980 mL	0.4902 mL	0.9805 mL	2.4512 mL
	30 mM	0.0817 mL	0.4085 mL	0.8171 mL	2.0427 mL
	40 mM	0.0613 mL	0.3064 mL	0.6128 mL	1.5320 mL
	50 mM	0.0490 mL	0.2451 mL	0.4902 mL	1.2256 mL
	60 mM	0.0409 mL	0.2043 mL	0.4085 mL	1.0213 mL
	80 mM	0.0306 mL	0.1532 mL	0.3064 mL	0.7660 mL
	100 mM	0.0245 mL	0.1226 mL	0.2451 mL	0.6128 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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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

YS121

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