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Pirinixic Acid

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Chemical Structure| 50892-23-4 同义名 : Wy-14643;NSC 310038
CAS号 : 50892-23-4
货号 : A180605
分子式 : C14H14ClN3O2S
纯度 : 98%
分子量 : 323.798
MDL号 : MFCD00191335
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(324.28 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

30% PEG400+2% Tween 80+water 5 mg/mL

生物活性
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
细胞系 浓度 检测类型 检测时间 活动说明 数据源
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
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.09mL

0.62mL

0.31mL

15.44mL

3.09mL

1.54mL

30.88mL

6.18mL

3.09mL
参考文献

[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.