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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Factor Xa-BAY 3389934
BAY 3389934

Chemical Structure : BAY 3389934

CAS No.: 2915316-40-2

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BAY 3389934 (BAY3389934)

货号: PC-24671Not For Human Use, Lab Use Only.

BAY 3389934 is a potent and highly selective, direct dual FIIa/Xa inhibitor with IC50 of 4.9/0.66 nM (in buffer) and 22/9.2 nM (in plasma) respectively.

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

    生物&药学活性

    BAY 3389934 is a potent and highly selective, direct dual FIIa/Xa inhibitor with IC50 of 4.9/0.66 nM (in buffer) and 22/9.2 nM (in plasma) respectively.
    BAY3389934 has IC50 values of 31 and 5.3 nM (FIIa/FXa) for rabbit and 26 and 16 nM (FIIa/FXa) for minipig plasma.
    BAY3389934 has EC200 values of 0.32 μM (PT) and 0.22 μM (aPTT) for in vitro anticoagulant activity.
    BAY3389934 (0.23 μM) doubled the CT value in the ROTEM (EXTEM) whole blood assay.
    BAY3389934  inhibits pre-existing thrombin by potent inhibition of TF-triggered ongoing, normalizes LPS-induced CT in human whole blood at 130 nM.
    BAY3389934 strongly reduced the hypercoagulatory state and protected from organ damage in a baboon model of Staphylococcus aureus sepsis.
    BAY3389934 showed high selectivity within the serine protease target family (Table 7), no significant off-target effects on a broad range of targets, including GPCRs, ion channels, nuclear hormone receptors, and other proteins and enzymes (>70 targets).

    物理化学性质&存储条件

    分子量 624.12
    分子式 C26H30ClN5O7S2
    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

    2-(1-methyl-1H-imidazol-2-yl)ethyl (S)-3-(5-chlorothiophene-2-carboxamido)-2-((2-ethyl-3-((S)-3-hydroxy-2-oxopyrrolidin-1-yl)phenyl)sulfonamido)propanoate

    参考文献

    1. Robert Silasi, et al. Blood (2024) 144 (Supplement 1): 3988.

    2. Patent WO2023031083 A1.

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