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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Mineralocorticoid Receptor (MLR)-PF-03882845
PF-03882845

Chemical Structure : PF-03882845

CAS No.: 1023650-66-9

PF-03882845 (PF03882845, PF-3882845)

货号: PC-61848Not For Human Use, Lab Use Only.

PF-03882845 (PF-3882845) is highly potent, selective, nonsteroidal, orally bioavailable Mineralocorticoid receptor (MR, MLR) antagonist with IC50 of 4.5 nM.

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

    生物&药学活性

    PF-03882845 (PF-3882845) is highly potent, selective, nonsteroidal, orally bioavailable Mineralocorticoid receptor (MR, MLR) antagonist with IC50 of 4.5 nM.
    PF-03882845 displays >500-fold selectivity versus PR and other related nuclear hormone receptors.
    PF-03882845 significantly increases urinary Na(+)/K(+) ratio in vivo.
    PF-03882845 prevents renal injury with reduced risk of hyperkalemia in an animal model of nephropathy.

    物理化学性质&存储条件

    分子量 419.91
    分子式 C24H22ClN3O2
    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

    (3S,3aR)-2-(3-chloro-4-cyanophenyl)-3-cyclopentyl-3,3a,4,5-tetrahydro-2H-benzo[g]indazole-7-carboxylic acid

    参考文献

    1. Casimiro-Garcia A, et al. J Med Chem. 2014 May 22;57(10):4273-88.

    2. Orena S, et al. Front Pharmacol. 2013 Oct 14;4:115.

    3. Eudy RJ, et al. J Transl Med. 2011 Oct 21;9:180.

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