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BMS-687453

CAS No. : 1000998-59-3

MCE 站：BMS-687453

产品活性：BMS-687453 是一种有效的，选择性的 PPARα 激动剂，对人 PPARα 的 EC₅₀ 和 IC₅₀ 分别为 10 nM 和 260 nM；较弱地抑制 PPARγ 的活性，EC₅₀ 和 IC₅₀ 值分别为 4100 nM 和 >15000 nM。

研究领域：Cell Cycle/DNA Damage

作用靶点：PPAR

In Vitro: 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.

In Vivo: 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.

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