BMS 986020

BMS 986020 is an antagonist of lysophosphatidic acid receptor 1 (LPA₁; K_b = 0.0067 µM).¹ It is selective for LPA₁ over LPA₃ in CHO cells expressing the human receptors (IC₅₀s = 0.3 and >1 µM, respectively).² BMS 986020 also inhibits organic anion transporting polypeptide 1B1 (OATP1B1), OATP1B3, the bile salt export pump (BSEP), multidrug resistant protein 3 (MDR3), multidrug resistance-associated protein 3 (MRP3), and MRP4 (IC₅₀s = 0.17, 0.57, 4.8, 7.5, 22, and 6.2 µM, respectively).¹ It reduces bleomycin-induced lung fibrosis in rats when administered at a dose of 30 mg/kg twice per day. BMS 986020 (225 and 500 mg/kg per day) decreases total biliary bile acid levels and induces bile duct hyperplasia, cholangitis, and cholestasis in monkeys.³ It decreases infarct volume and neurological deficits in a mouse model of ischemic stroke induced by transient middle cerebral artery occlusion (MCAO) when administered at a dose of 5 mg/kg.⁴

WARNING This product is not for human or veterinary use.

1. Cheng, P.T.W., Kaltenbach, R.F., III, Zhang, H., et al. Discovery of an oxycyclohexyl acid lysophosphatidic acid receptor 1 (LPA₁) antagonist BMS-986278 for the treatment of pulmonary fibrotic diseases. J. Med. Chem. 64(21), 15549-15581 (2021).

2. Hutchinson, J.H., Seiders, T.J., Wang, B., et al. Polycyclic antagonists of lysophosphatidic acid receptors. (2010).

3. Sivaraman, L., Gill, M., Nelson, D.M., et al. Structure dependence and species sensitivity of in vivo hepatobiliary toxicity with lysophosphatidic acid receptor 1 (LPA₁) antagonists. Toxicol. Appl. Pharmacol. 438, 115846 (2021).

4. Gaire, B.P., Sapkota, A., and Choi, J.W. BMS-986020, a specific LPA₁ antagonist, provides neuroprotection against ischemic stroke in mice. Antioxidants (Basel) 9(11), 1097 (2020).