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首页-小分子抑制剂&激动剂-GPCR-Somatostatin Receptor-MK-1421
MK-1421

Chemical Structure : MK-1421

CAS No.: 1235995-16-0

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MK-1421 (MK1421;MK 1421)

货号: PC-61087Not For Human Use, Lab Use Only.

MK-1421 is a potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 2.3 nM, >2,500-fold selectivity over SSTR1/2/4/5 (IC50>5 uM).

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

    生物&药学活性

    MK-1421 is a potent, selective, orally active somatostatin receptor SSTR3 antagonist with binding Ki of 2.3 nM, >2,500-fold selectivity over SSTR1/2/4/5 (IC50>5 uM).
    MK-1421 shows excellent efficacy in a mouse model of glucose excursion (oGTT) and demonstrates glucose-dependent release of insulin from relevant human tissue.

    物理化学性质&存储条件

    分子量 525.548
    分子式 C27H24FN9O2
    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

    5-((1R,3R)-1-(1-ethyl-1H-pyrazol-4-yl)-3-(4-(5-fluoropyridin-2-yl)-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)-3-methyl-1,3,4-oxadiazol-2(3H)-one

    参考文献

    1. Shah SK, et al. ACS Med Chem Lett. 2015 Mar 18;6(5):513-7.

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