BMS-986120
目录号 : KM16559 CAS No. : 1478712-37-6 纯度 : 98%

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。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock

Other Forms of Rapamycin:

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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.

IC50&Target

IC50: 9.5 nM (PAR4, human), 2.1 nM (PAR4, monkey)

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.

分子式
C23N5O5S2H23
分子量
513.59
CAS号
1478712-37-6
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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工作液浓度 mg/ml;

DMSO母液配制方法 mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,

体内配方配制方法μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

配置后的溶液总体积

1. 首先保证母液是澄清的;
           2. 一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。