BMS-687453

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 PPARα 激动剂，在 PPAR-GAL4 反式激活测定中，对人 PPARα 的 EC50 为 10 nM，选择性是人 PPARγ 的 410 倍。

A potent and selective PPARα agonist with EC50 of 10 nM for human PPARα and 410-fold selectivity over human PPARγ in PPAR-GAL4 transactivation assays; has negligible cross-reactivity against a panel of human nuclear hormone receptors including PPARδ; demonstrates an excellent pharmacological and safety profile for the treatment of atherosclerosis and dyslipidemia.Dyslipidemia Preclinical

BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and ～410-fold and more than 57-fold selectivity vs human PPARγ of 4100 nM and >15000 nM in PPAR-GAL4 transactivation assays. BMS-687453 exhibits high PPARα potency (EC50 = 47 nM) with ～50-fold selectivity vs PPARγ (EC50 = 2400 nM) in HepG2 cells. However, BMS-687453 shows less potent activities in rodent PPARα functional assays, with a moderate EC50 of 426 nM for mouse and 488 nM for hamster but remains a full PPARα agonist in both species.

BMS-687453 (10, 50, 100, p.o.) dose-dependently increases serum ApoA1 protein levels and low-density lipoprotein-cholesterol (LDLc) levels in mice. BMS-687453 (1, 3, 10 mg/kg, p.o.) decreases HDLc levels in high fat-fed hamsters. BMS-687453 induces PDK4 mRNA in the liver, with ED50 value of 0.24 mg/kg. BMS-687453 (300 mg/kg, p.o.) causes skeletal myofiber degeneration and necrosis characterized by observed discoid changes, myofibril lysis, hyalinization, and cellular infiltration in male rats. BMS-687453 (300 mg/kg, p.o.) induces a mild toxicity in both fast and slow-twitch muscles in male rats.

BMS687453 | BMS 687453

Metabolic Enzyme/Protease

PPAR

PPAR

Cardiovascular Disease

Dyslipidemia

1000998-59-3

444.8649

C22H21ClN2O6

>98% (HPLC)

DMSO: ≥ 31 mg/mL

O=C(O)CN(CC1=CC=CC(OCC2=C(C)OC(C3=CC=C(Cl)C=C3)=N2)=C1)C(OC)=O

Glycine, N-[[3-[[2-(4-chlorophenyl)-5-methyl-4-oxazolyl]methoxy]phenyl]methyl]-N-(methoxycarbonyl)-

(-20℃)

With Ice Pack

≥ 2 years