For research use only. Not Intended for Therapeutic Use!
|IC50:||10 nM (EC50)|
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BMS-687453 is a potent and selective PPARα agonist, with an EC50 of 10 nM for human PPARα and 410-fold selectivity vs human PPARγ in PPAR-GAL4 transactivation assays.
IC50 value: 10 nM (EC50)
in vitro: BMS-687453 shows negligible activity (EC50 for transactivation of >25 μM and efficacies of <15% of standard) against a panel of human nuclear hormone receptors, including PPARδ LXR and RXR. BMS-687453 as a potent, highly selective PPARalpha agonist with an excellent preclinical safety profile. 
in vivo: BMS-687453 exhibits low plasma clearance in the mouse, rat, and monkey and moderate plasma clearance in the dog, and the volume of distribution ranged from 0.7 L/kg (rat) to 3.5 L/kg (cynomolgusmonkey),which is comparable to the total body water in the rat and greater than total body water in the mouse, dog, and monkey. The half-life of BMS-687453 ranges from 3 h in mouse to 12 h in cynomolgus monkeys. BMS-687453 also possesses excellent absolute oral bioavailability ranging from 58% (dog) to 91% (rat). Additionally, BMS-687453 has excellent pharmaceutical properties, with a crystalline aqueous solubility being 280 μg/mL atpH6.5, increasing to > 4 mg/mL at pH 7.9.