产品描述:
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.{41865} 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).{41866} 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.