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首页-小分子抑制剂&激动剂-GPCR-Protease-activated Receptor (PAR)-BMS-986141
BMS-986141

Chemical Structure : BMS-986141

CAS No.: 1478711-48-6

BMS-986141 (BMS986141)

货号: PC-20965Not For Human Use, Lab Use Only.

BMS-986141 is a potent, selective antagonist of protease-activated receptor 4 (PAR4) with IC50 of 0.4 nM, Kd of 0.1 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    BMS-986141 is a potent, selective antagonist of protease-activated receptor 4 (PAR4) with IC50 of 0.4 nM, Kd of 0.1 nM.
    BMS-986141 potently inhibits platelet aggregation induced with a PAR4 agonist peptide (25 μM) with IC50 of 2.2 nM.
    BMS-986141 shows no effect on platelet aggregation induced by a PAR1 antagonist peptide, adenosine diphosphate, collagen, or the thromboxane A2 receptor agonist U46619 up to 1 uM.
    BMS-986141 (0.5 and 1 mg/kg) demonstrated excellent antithrombotic efficacy and minimal bleeding time prolongation in monkey models relative to the clinically important antiplatelet agent clopidogrel.

    物理化学性质&存储条件

    分子量 561.63
    分子式 C27H23N5O5S2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    4-(4-(((6-methoxy-2-(2-methoxyimidazo[2,1-b][1,3,4]thiadiazol-6-yl)benzofuran-4-yl)oxy)methyl)thiazol-2-yl)-N,N-dimethylbenzamide

    参考文献

    1. E Scott Priestley, et al. J Med Chem. 2022 Jul 14;65(13):8843-8854.

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