DS-6930

DS-6930 is a potent and selective agonist of PPARγ, with an EC₅₀ of 41 nM. DS-6930 could robust reduce plasma glucose (PG), and with fewer PPARγ-related adverse effects than Rosiglitazone. DS-6930 can be used for the research of diabetes^[1]. IC50 & Target: EC50: 41 nM (PPARγ)^[1] In Vitro: DS-6930 exhibits high potency in vitro with an intermediate PPARγ agonist activity (EC₅₀=41 nM, E_max=68%), and possesses high PPARα or PPARδ selectivity (13% PPARα activation at 10 μM and no PPARδ activation at 10 μM) ^[1].
DS-6930 (10-100 μM) exhibits lower cell toxicity at 100 μM^[1]. In Vivo: DS-6930 (0.1-3 mg/kg; p.o. for 3 weeks) decreases plasma glucose (PG) levels in a dose-dependent manner in rats^[1].
DS-6930 (100-1000 mg/kg; p.o.for 4 weeks) does not affect any liver enzyme activities and has no remarkable change in relative heart weigh in F344 rats^[1].
DS-6930 exhibits C_max=0.0792 μg/mL, T_max=1.8 h, and AUC_0-24h=0.861 h?μg/mL following oral (0.3 mg/kg) administration on day 22 in rats^[1].
DS-6930 exhibits C_max=2.25 μg/mL, T_max=5.0 h, T_1/2=13.5 h, and AUC_last=23.5 h?μg/mL following oral (3 mg/kg) administration in cynomolgus monkeys^[1].
DS-6930 exhibits excellent bioavailability (F=89%), total body clearance (CL=2.06 mL/min/kg), and distribution volume at steady state (Vss=0.36 L/kg) following intravenous (1 mg/kg) administration in cynomolgus monkeys^[1].