Description
An LPA1 receptor antagonist (IC50s = 25 and 23 nM in CHO cells expressing human or mouse receptors, respectively); selective for LPA1 over LPA2, LPA3, LPA4, and LPA5 (IC50s = >10,000 nM for human LPA2-5); inhibits chemotaxis of CHO cells overexpressing LPA1 and of A2058 human melanoma cells (IC50s = 778 and 233 nM, respectively); prevents LPA-induced increases in plasma histamine levels in mice (ED50 = 8.3 mg/kg); decreases kidney fibrosis in a mouse model of unilateral ureteral obstruction at 30 mg/kg for eight days