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1000998-59-3 | BMS-687453

BMS-687453 NLT 98%

SKU : MC500281

CAS Number : 1000998-59-3

Molecular Formula : C22H21ClN2O6 | Molecular Weight : 444.86

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Purity NLT 98%
Storage at 20ºC 2 years
*The above information is for reference only.
Chemical Name BMS-687453
CAS Number 1000998-59-3
MDL Number MFCD18251482
Molecular Formula C22H21ClN2O6
Molecular Weight 444.86
Introduction of 1000998-59-3 :

BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays. IC50 & Target: EC50: 10 nM (GAL4-human PPARα), 4100 nM (GAL4-human PPARγ)[1]
IC50: 260 nM (Human PPARα), >15000 nM (Human PPARγ)[1]
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[1]. 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[1]. BMS-687453 induces PDK4 mRNA in the liver, with ED50 value of 0.24 mg/kg[2]. 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[3].

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