• merck millipore,默克密理博,346003,Glucagon Receptor Antagonist II - CAS 191034-25-0 - Calbiochem
  • merck millipore,默克密理博,346003,Glucagon Receptor Antagonist II - CAS 191034-25-0 - Calbiochem

    产品名称:Glucagon Receptor Antagonist II - CAS 191034-25-0 - Calbiochem
    产品型号:346003
    The Glucagon Receptor Antagonist II, also referenced under CAS 191034-25-0, controls the biological activity of Glucagon Receptor.

    merck millipore,默克密理博,346003,Glucagon Receptor Antagonist II - CAS 191034-25-0 - Calbiochem

  • 产品介绍
  • merck millipore,默克密理博,346003,Glucagon Receptor Antagonist II - CAS 191034-25-0 - Calbiochem

    重要规格表

    经验配方 CAS号
    C₂₄H₂₀BrClN₂O191034-25-0
    描述
    概述 A cell-permeable triarylpyrrole compound that acts as a selective, non-competitive, high affinity glucagon receptor antagonist (IC50 = 3.7 nM, 63 nM, and 60 nM for inhibition of labeled glucagon binding to human, murine, and canine glucagon receptor, respectively). Exhibits diminished antagonistic properties in the presence of Mg2+ (by ≥ 20-fold) and exhibits poor affinity for the rat, guinea pig, and rabbit glucagon receptors (IC50 > 1 µM). Does not inhibit binding of glucagon-like peptide-1 (GLP-1) to the homologous GLP-1 receptor even at concentrations as high as 10 µM. Does not affect ligand binding of a panel of other GPCRs and only weakly affects p38 kinase activity (IC50 = 1.44 µM). Potently inhibits glucagon-induced GTPγS binding to Gαs (IC50 = 158 nM) and adenylate cyclase activation in hGLUR-CHO cells (Kb = 25 nM). Shown to be orally bioavailable in both mice and rats.
    产品目录编号 346003
    品牌系列 Calbiochem®
    同义词 2-(4-Pyridyl)-5-(4-chlorophenyl)-3-(5-bromo-2-propyloxyphenyl)pyrrole, L-168,049
    参考
    参考 Dallas-Yang, Q., et al. 2002. Anal. Biochem. 301, 156.
    Cascieri, M.A., et al. 1999. J. Biol. Chem. 274, 8694.
    de Laszlo, S.E., et al. 1999. Bioorg. Med. Chem. Lett. 9, 641.
    产品信息
    CAS号 191034-25-0
    具有ATP竞争性 N
    形式 Light beige solid
    Hill配方 C₂₄H₂₀BrClN₂O
    化学配方 C₂₄H₂₀BrClN₂O
    Molar Mass 467.8
    可逆 N
    结构配方图像
    生物信息
    主靶 Glucagon Receptor
    主靶IC50 3.7 nM, 63 nM, and 60 nM for inhibition of labeled glucagon binding to human, murine, and canine glucagon receptor, respectively
    纯度 ≥98% by HPLC
    理化信息
    细胞可渗透 Y
    溶解度 DMSO or EtOH
    储存和货运信息
    货运代码 Ambient Temperature Only
    毒性 Standard Handling
    储存 +2°C to +8°C
    避光 Protect from light
    无需冷冻 No
    特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
    包装信息
    惰性气体下包装 Packaged under inert gas

    merck millipore,默克密理博,346003,Glucagon Receptor Antagonist II - CAS 191034-25-0 - Calbiochem

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