Cayman 4-Nitrophenyl Betad-Cellotrioside; Purity- Greater Than

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 LPA_2-5). 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.

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