| Description | BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 (PAR4) antagonist. With IC50s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects[1][2]. |
| In vitro | BMS-986120 has high binding affinity to PAR4 expressed on HEK293 cells. And it inhibition of PAR4-induced calcium mobilization with an IC50 of 0.56 nM[3]. |
| In vivo | BMS (0.2, 0.5, 1 mg/kg) reduces TW by 35±5, 49±4, and 83±4%, respectively. In monkeys, BMS (1 mg/kg) does not inhibit PA induced by PAR1-AP, ADP and collagen, supporting selectivity. Maximum KBT and MBT increases are only 2.2-fold and 1.8-fold, respectively[1]. |
| Target activity | PAR4 (human):9.5 nM, PAR4 (monkey):2.1 nM |
| molecular weight | 513.59 |
| Molecular formula | C23H23N5O5S2 |
| CAS | 1478712-37-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| References | 1. Pancras C Wong, et al. Abstract 175: A Novel Orally-Active Small-Molecule Antagonist of the Platelet Protease-Activated Receptor-4, BMS-986120, Inhibits Arterial Thrombosis With Limited Impact on Hemostasis in Cynomolgus Monkeys. Stroke. 2018;47:A175. 2. Wilson SJ, et al. PAR4 (Protease-Activated Receptor 4) Antagonism With BMS-986120 Inhibits Human Ex VivoThrombus Formation. Arterioscler Thromb Vasc Biol. 2018 Feb;38(2):448-456. 3. Wong PC, et al. Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding. Sci Transl Med. 2017 Jan 4;9(371). |