AM095 sodium

Description: AM095 sodium is a novel, potent and selective LPA1 receptor antagonist that inhibited GTPgammaS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA1 with IC50 of 0.98 and 0.73 uM, respectively. It exhibited no LPA1 agonism. Lysophosphatidic acid (LPA) is a bioactive phospholipid that signals through a family of at least six G protein-coupled receptors designated LPA1-6. LPA type 1 receptor (LPA1) exhibits widespread tissue distribution and regulates a variety of physiological and pathological cellular functions.

References:

1. Swaney JS, et al. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. J Pharmacol Exp Ther. 2011 Mar; 336(3):693-700.

2. Castelino FV, et al. Amelioration of dermal fibrosis by genetic deletion or pharmacologic antagonism of lysophosphatidic acid receptor 1 in a mouse model of scleroderma. Arthritis Rheum. 2011 May; 63(5):1405-15.

3. Im DS. Intercellular Lipid Mediators and GPCR Drug Discovery. Biomol Ther (Seoul). 2013 Nov; 21(6):411-22. doi: 10.4062/biomolther.2013.080. Review.

Related CAS #: 1345614-59-6 (sodium) 1228690-36-5 (free acid)