AM095

AM095 is an orally bioavailable antagonist of lysophosphatidic acid receptor 1 (LPA1) with IC50 values of 25 and 23 nM in CHO cells expressing human or mouse receptors, respectively. It is selective for LPA1 over LPA2, LPA3, LPA4, and LPA5 (IC50s = >10,000 nM for human LPA2-5). It inhibits chemotaxis of CHO cells overexpressing LPA1 and of A2058 human melanoma cells (IC50s = 778 and 233 nM, respectively) and prevents LPA-induced increases in plasma histamine levels in mice (ED50 = 8.3 mg/kg). It also decreases collagen and protein levels in bronchoalveolar lavage fluid (BALF) in a mouse model of bleomycin-induced lung injury (ED50s = ~10 mg/kg for both) and decreases kidney fibrosis in a mouse model of unilateral ureteral obstruction when administered at a dose of 30 mg/kg for eight days.Formal Name: 4'-[3-methyl-4-[[[(1R)-1-phenylethoxy]carbonyl]amino]-5-isoxazolyl]-[1,1'-biphenyl]-4-acetic acid. CAS Number: 1228690-36-5. Molecular Formula: C27H24N2O5. Formula Weight: 456.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: Soluble. lambdamax: 297 nm. SMILES: O=C(O)CC(C=C1)=CC=C1C(C=C2)=CC=C2C3=C(NC(O[C@H](C)C4=CC=CC=C4)=O)C(C)=NO3. InChi Code: InChI=1S/C27H24N2O5/c1-17-25(28-27(32)33-18(2)20-6-4-3-5-7-20)26(34-29-17)23-14-12-22(13-15-23)21-10-8-19(9-11-21)16-24(30)31/h3-15,18H,16H2,1-2H3,(H,28,32)(H,30,31)/t18-/m1/s1. InChi Key: LNDDRUPAICPXIN-GOSISDBHSA-N.