BMS-986120 是first-in-class、具有口服活性的蛋白酶激活受体 4 (PAR4) 的可逆拮抗剂，在人类和猴子血液中的 IC50 值分别为 9.5 nM 和 2.1 nM。BMS-986120 具有有效选择性的抗血小板作用。
| 生物活性 |
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. |
|---|---|
| 体外研究 |
BMS-986120 has high binding affinity to PAR4 expressed on HEK293 cells and inhibition of PAR4-induced calcium mobilization with an IC50 of 0.56 nM. |
| 体内研究 |
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.
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| 分子式 |
C23N5O5S2H23
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| 分子量 |
513.59
|
| CAS号 |
1478712-37-6
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
| 临床试验 |
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纯度： 98%
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