BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 ( PAR4 ) antagonist, with IC 50 s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Product Description
BMS-986120 is a first-in-class oral and reversible protease-activated receptor 4 ( PAR4 ) antagonist, with IC 50 s of 9.5 nM and 2.1 nM in human and monkey blood, respectively. BMS-986120 has potent and selective antiplatelet effects
In Vitro
BMS-986120 has high binding affinity to PAR4 expressed on HEK293 cells and inhibition of PAR4-induced calcium mobilization with an IC 50 of 0.56 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
In monkeys, BMS (1 mg/kg) does not inhibit PA induced by PAR1-AP, ADP and collagen, supporting selectivity. BMS (0.2, 0.5, 1 mg/kg) reduces TW by 35±5, 49±4, and 83±4%, respectively. Maximum KBT and MBT increases are only 2.2-fold and 1.8-fold, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only.
