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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Guanylate Cyclase-GSK2181236A
GSK2181236A

Chemical Structure : GSK2181236A

CAS No.: 1160426-89-0

GSK2181236A (GSK-2181236A; GSK2181236A)

货号: PC-70008Not For Human Use, Lab Use Only.

GSK2181236A is a potent, selective soluble guanylate cyclase (sGC) stimulator that increases sGC activity (cGMP formation) with EC50s of 27 and 25 nM for rat and human sGC, respectively.

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

    生物&药学活性

    GSK2181236A is a potent, selective soluble guanylate cyclase (sGC) stimulator that increases sGC activity (cGMP formation) with EC50s of 27 and 25 nM for rat and human sGC, respectively.
    GSK2181236A displays 23-fold selectivity for sGC over OATP1B1 and >197-fold selectivity over a panel of 38 proteins.
    GSK2181236A increases P-VASP levels in rat aortic smooth muscle cells with EC50 of 12.7 nM.
    GSK2181236A attenuates the development of cardiac hypertrophy in a blood pressure-independent fashion.

    物理化学性质&存储条件

    分子量 613.14
    分子式 C31H21F6N3O4
    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

    1-(6-(2-((3-methyl-4'-(trifluoromethoxy)-[1,1'-biphenyl]-4-yl)methoxy)phenyl)pyridin-2-yl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid

    参考文献

    1. Costell MH, et al. Front Pharmacol. 2012 Jul 5;3:128.

    2. Stasch JP, et al. Curr Opin Pharmacol. 2015 Apr;21:95-104.

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