|2-((4-氯-6-(((2,3-二甲基苯基)氨基)嘧啶-2-基)硫基)乙酸|CsnPharm

CAS No.: 50892-23-4

匹立尼酸 Catalog No. CSN12217

Synonyms: Wy-14643;NSC 310038;Pirinixic Acid

Wy-14643 is an agonist of PPARα with EC50 of 0.63 μM that can decrease the inflammatory response. It has other functions including lipid metabolism, cell proliferation, differentiation, adipogenesis etc..

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PPARα

IC50:36.5μM PPARγ

IC50:53.7μM
描述Wy-14643 is a selective PPARα agonist with EC50 values of 5μM and 0.63μM for human and murine PPARα, also exhibited less potency to human PPARγ/δwith IC50 values of 60 and 35μM, respectively, and murine PPARγ with IC50 value of 32μM in cell-based transactivation assays. Wy-14643 has been developed as hypolipidemic agents through optimization of their lipid-lowering activity in rodents^[1]. Wy-14643 induced expression of UCP3 in rat neonates^[2]. Oral administration of Wy-14643 0.1% in diet for 10 days in high-fat-diet mice or chow-fed foz/foz mice reduced steatosis in nonalcoholic steatohepatitis and simple steatosis livers and fewer inflammatory foci, with hepatoprotection against ischemia–reperfusion injury by alanine aminotransferase release. The reduction of hepatic VCAM-1 and ICAM-1 expression, IL-1α, TNF-α, IL-12 and activated NF-κB, p38, IL-6 production and cell cycle entry observed^[4].
作用机制Wy-14643 is a synthetic PPARα ligand.^[4]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
COS7 cells	-	Function assay	-	Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay, IC50=36.3 μM	25037914
EAhy926 cells	10 uM	Function assay	12 h	Inhibition of tube formation in human EAhy926 cells at 10 uM pre-incubated for 12 hrs measured after 24 hrs by phase-contrast microscopy	19036594
HEK293 cells	-	Function assay	-	Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay, EC50=23.33 μM	23265844

更多
动物研究
剂量
Rat: 1 mg/kg (i.p.); 1 mg/kg^[5] (i.v.) Mice: 3.125 mg/kg - 25 mg/kg^[6] (i.p.), 80 mg/kg^[7] (i.p.), 60 mg/kg - 250 mg/kg^[8] (i.p.)

给药途径
i.p., i.v.
参考文献

动物研究
剂量	Rat: 1 mg/kg (i.p.); 1 mg/kg^[5] (i.v.) Mice: 3.125 mg/kg - 25 mg/kg^[6] (i.p.), 80 mg/kg^[7] (i.p.), 60 mg/kg - 250 mg/kg^[8] (i.p.)
给药途径	i.p., i.v.

[1] Willson TM, Brown PJ, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50.
[2] Brun S, Carmona MC, et al. Activators of peroxisome proliferator-activated receptor-alpha induce the expression of the uncoupling protein-3 gene in skeletal muscle: a potential mechanism for the lipid intake-dependent activation of uncoupling protein-3 gene expression at birth. Diabetes. 1999 Jun;48(6):1217-22.
[3] Teoh NC, Williams J, et al. Short-term therapy with peroxisome proliferation-activator receptor-alpha agonist Wy-14,643 protects murine fatty liver against ischemia-reperfusion injury. Hepatology. 2010 Mar;51(3):996-1006.
[4] Bishop-Bailey D, et al. Peroxisome proliferator-activated receptors in the cardiovascular system. Br J Pharmacol. 2000 Mar;129(5):823-34.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0883 mL
- 15.4417 mL
- 30.8835 mL
- 5 mM
- 0.6177 mL
- 3.0883 mL
- 6.1767 mL
- 10 mM
- 0.3088 mL
- 1.5442 mL
- 3.0883 mL

技术信息

CAS号

50892-23-4

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H14ClN3O2S

运输

蓝冰

分子量

323.80

别名

Wy-14643;NSC 310038;Pirinixic Acid

溶解度

DMSO	64.0 mg/mL (197.7 mM)
Water	Insoluble
Ethanol	52.0 mg/mL (160.6 mM)

动物实验配方

30% PEG400+2% Tween 80+water

5 mg/mL

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靶点	Description	IC50
PPARα		IC50:36.5μM
PPARγ		IC50:53.7μM

匹立尼酸 Catalog No. CSN12217

靶点选择性

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