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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].
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].
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 1,950 | 5日内发货 | |
25 mg | ¥ 10,700 | 10-14周 | |
50 mg | ¥ 13,900 | 10-14周 | |
100 mg | ¥ 21,800 | 10-14周 |
产品描述 | 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]. |
靶点活性 | PAR4 (human):9.5 nM, PAR4 (monkey):2.1 nM |
体外活性 | 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]. |
体内活性 | 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]. |
分子量 | 513.59 |
分子式 | C23H23N5O5S2 |
CAS No. | 1478712-37-6 |
密度 | 1.57 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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