产品描述:
BMS 986020 is an antagonist of lysophosphatidic acid receptor 1 (LPA1; Kb = 0.0067 µM).{65080} It is selective for LPA1 over LPA3 in CHO cells expressing the human receptors (IC50s = 0.3 and >1 µM, respectively).{37079} BMS 986020 also inhibits organic anion transporting polypeptide 1B1 (OATP1B1), OATP1B3, the bile salt export pump (BSEP), multidrug resistant protein 3 (MDR3), multidrug resistance-associated protein 3 (MRP3), and MRP4 (IC50s = 0.17, 0.57, 4.8, 7.5, 22, and 6.2 µM, respectively).{65080} It reduces bleomycin-induced lung fibrosis in rats when administered at a dose of 30 mg/kg twice per day. BMS 986020 (225 and 500 mg/kg per day) decreases total biliary bile acid levels and induces bile duct hyperplasia, cholangitis, and cholestasis in monkeys.{65081} It decreases infarct volume and neurological deficits in a mouse model of ischemic stroke induced by transient middle cerebral artery occlusion (MCAO) when administered at a dose of 5 mg/kg.{65082}