货号	规格	价格	上海	北京	珠海	重庆	武汉
S89302-5mg	≥98%	￥3500.00 S89302-5mg ￥3500.00 3-5天	0 货期：3-5天	-	-	-	-
S89302-10mg	≥98%	￥5500.00 S89302-10mg ￥5500.00 3-5天	0 货期：3-5天	-	-	-	-
S89302-25mg	≥98%	￥9870.00 S89302-25mg ￥9870.00 3-5天	0 货期：3-5天	-	-	-	-
S89302-100mg	≥98%	￥22800.00 S89302-100mg ￥22800.00 3-5天	0 货期：3-5天	-	-	-	-

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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

靶点：

PAR4

体外研究：

BMS-986120 对 HEK293 细胞上表达的 PAR4 具有高结合亲和力，并抑制 PAR4 诱导的钙动员，IC50 为 0.56 nM

体内研究：

在猴子中，BMS-986120 (1 mg/kg) 不抑制由 PAR1-AP、ADP 和胶原蛋白诱导的 PA，支持选择性。BMS-986120 (0.2、0.5、1 mg/kg) 分别使 TW 降低 35±5、49±4 和 83±4%。KBT 和 MBT 的最大增加量分别仅为 2.2 倍和 1.8 倍

动物实验：

Monkeys Individual anesthetized monkeys are given orally of BMS-986120 (BMS: 0.2, 0.5,1 mg/kg) or vehicle (n=8/group) 2 hour before a combination of thrombosis, BT and ex vivo biomarker experiments. Aspirin alone (ASA, 4 mg/kg/h IV) or in combination with BMS-986120 (0.5, 1 mg/kg) is also studied (n=8/group). Thrombus weight (TW) reduction, BT increase over vehicle in kidney (KBT) and mesenteric artery (MBT), and platelet aggregation (PA) inhibition are determined. Peak PA responses to activation peptides selective for PAR4 (PAR4-AP, 12.5 μM) and PAR1 (PAR1-AP, 18 μM), ADP (20 μM), and collagen (5 μg/mL) are determined by whole blood aggregometry.

参考文献：

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).

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.947 ml	9.735 ml	19.471 ml
5 mM	0.389 ml	1.947 ml	3.894 ml
10 mM	0.195 ml	0.974 ml	1.947 ml
50 mM	0.039 ml	0.195 ml	0.389 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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