AM966

AM966 is a potent, selective, and orally active LPA(1) receptor antagonist which inhibits lung fibrosis in the mouse bleomycin model. In vitro, AM966 inhibited LPA-stimulated intracellular calcium release from Chinese hamster ovary cells stably expressing human LPA(1) receptors and inhibited LPA-induced chemotaxis of human IMR-90 lung fibroblasts expressing LPA(1) receptors. AM966 reduced lung injury, vascular leakage, inflammation and fibrosis at multiple time points following intratracheal bleomycin instillation. AM966 also decreased lactate dehydrogenase activity and tissue inhibitor of metalloproteinase-1, transforming growth factor beta1, hyaluronan and matrix metalloproteinase-7, in bronchoalveolar lavage fluid.

Properties:

Boiling point: 659.4±55.0 °C(Predicted)

density: 1.330±0.06 g/cm3 (20 ºC 760 Torr)

pka: 4.21±0.10(Predicted)

LPL Receptor Related Products:

Ki16425; Ki16198; AM095; Fingolimod hydrochloride; Siponimod; Ozanimod; CYM5520; JTE-013; Ponesimod; Etrasimod; CYM50308; NIBR-0213; VPC-23019; ONO-7300243

[1]. Swaney, JS, et al. A novel, orally active LPA1 receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. Br J Pharmacol. 2010 Aug;160(7):1699-713.

[2]. Olianas MC, et al. Antidepressants activate the lysophosphatidic acid receptor LPA(1) to induce insulin-like growth factor-I receptor transactivation, stimulation of ERK1/2 signaling and cell proliferation in CHO-K1 fibroblasts. Biochem Pharmacol. 2015 Jun 15;95(4):311-23.