BMS 986020

BMS 986020 is an antagonist of lysophosphatidic acid receptor 1 (LPA1, Kb = 0.0067 µM). It is selective for LPA1 over LPA3 in CHO cells expressing the human receptors (IC50s = 0.3 and >1 µM, respectively). 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). 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. 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.Formal Name: 1-[4'-[3-methyl-4-[[[(1R)-1-phenylethoxy]carbonyl]amino]-5-isoxazolyl][1,1'-biphenyl]-4-yl]-cyclopropanecarboxylic acid. CAS Number: 1257213-50-5. Synonyms: AM-000152. Molecular Formula: C29H26N2O5. Formula Weight: 482.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml, DMF:PBS (pH7.2) (1:40): 0.02 mg/ml, DMSO: 25 mg/ml, Ethanol: 20 mg/ml. lambdamax: 297 nm. SMILES: O=C(O)C1(CC1)C(C=C2)=CC=C2C(C=C3)=CC=C3C4=C(NC(O[C@H](C)C5=CC=CC=C5)=O)C(C)=NO4. InChi Code: InChI=1S/C29H26N2O5/c1-18-25(30-28(34)35-19(2)20-6-4-3-5-7-20)26(36-31-18)23-10-8-21(9-11-23)22-12-14-24(15-13-22)29(16-17-29)27(32)33/h3-15,19H,16-17H2,1-2H3,(H,30,34)(H,32,33)/t19-/m1/s1. InChi Key: GQBRZBHEPUQRPL-LJQANCHMSA-N.