BMS-852927 (XL041) is a highly potent liver X receptor β (LXRβ) agonist with Ki of 12 and 19 nM for LXRβ and LXRα, respectively.
BMS-852927 demonstrates robust LXRβ activity (88%, EC50=24 nM) with low partial LXRα agonist activity (<25%) in cell assays.
BMS-852927 exhibits desired blood cell ABCG1 gene induction in cynomolgus monkeys with limited elevation of plasma triglycerides.
BMS-852927 has favorable combination of in vitro properties, excellent pharmacokinetic parameters, and a favorable lipid profile.
