Description
BMS 986020 is a potent G protein-coupled lysophosphatidic acid receptor 1 (LPA
1) antagonist with an IC
50 value less than 300 nM for human LPA
1 expressing CHO cells. Formulations containing BMS 986020 are being investigated in clinical trials for efficacy in idiopathic pulmonary fibrosis.
References
[1] PETER T. W. CHENG*. Discovery of an Oxycyclohexyl Acid Lysophosphatidic Acid Receptor 1 (LPA1) Antagonist BMS-986278 for the Treatment of Pulmonary Fibrotic Diseases[J]. Journal of Medicinal Chemistry, 2021, 64 21: 15549-15581. DOI:
10.1021/acs.jmedchem.1c01256[2] VEERESA GUDUDURU . Identification of Darmstoff analogs as selective agonists and antagonists of lysophosphatidic acid receptors[J]. Bioorganic & Medicinal Chemistry Letters, 2006, 16 2: Pages 451-456. DOI:
10.1016/j.bmcl.2005.08.096[3] L. SIVARAMAN . Structure dependence and species sensitivity of in vivo hepatobiliary toxicity with lysophosphatidic acid receptor 1 (LPA1) antagonists[J]. Toxicology and applied pharmacology, 2022, 438: Article 115846. DOI:
10.1016/j.taap.2021.115846[4] BHAKTA PRASAD GAIRE Ji W C Arjun Sapkota. BMS-986020, a Specific LPA1 Antagonist, Provides Neuroprotection against Ischemic Stroke in Mice.[J]. Antioxidants, 2020, 9 11. DOI:
10.3390/antiox9111097
