AM095 free acid 是LPA1受体拮抗剂，对重组人和小鼠 LPA1 的IC50值分别为 0.98 和 0.73 μM。

AM095 (free acid) is a potent LPA1 receptor antagonist (IC50s: 0.98 and 0.73 μM for recombinant human or mouse LPA1).

In vitro, AM095 was a potent LPA receptor antagonist because it inhibited GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA with IC values of 0.98 and 0.73 μM, respectively, and exhibited no LPA agonism.?In functional assays, AM095 inhibited LPA-driven chemotaxis of CHO cells overexpressing mouse LPA (IC = 778 nM) and human A2058 melanoma cells (IC = 233 nM)[3].

In vivo, AM095: 1) had high oral bioavailability and a moderate half-life and was well tolerated at the doses tested in rats and dogs after oral and intravenous dosing, 2) dose-dependently reduced LPA-stimulated histamine release, 3) attenuated bleomycin-induced increases in collagen, protein, and inflammatory cell infiltration in bronchalveolar lavage fluid, and 4) decreased kidney fibrosis in a mouse unilateral ureteral obstruction model[3].

1228690-36-5

C27H24N2O5

456.49

[4'-[3-甲基-4-[[[((R)-1-苯基乙基)氧基]羰基]氨基]异恶唑-5-基]联苯-4-基]乙酸

DMSO:67.3 mg/mL (147.43 mM),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years