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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-GR127935
GR127935

Chemical Structure : GR127935

CAS No.: 148672-13-3

GR127935 (GR-127935)

货号: PC-61865Not For Human Use, Lab Use Only.

GR127935 is a potent and selective 5-HT1B/1D receptor antagonist with pKi of 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptor.

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

    生物&药学活性

    GR127935 is a potent and selective 5-HT1B/1D receptor antagonist with pKi of 8.5 for both guinea pig 5-HT1D and rat 5-HT1B receptor.
    GR127935 displays >100-fold selectivity over 5HT1A, 5-HT2A, 5-HT2C receptors and other receptor types.
    GR127935 blocks porcine carotid vascular response to sumatriptan in vivo; orally bioavailable and centrally active.

    物理化学性质&存储条件

    分子量 497.587
    分子式 C29H31N5O3
    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

    N-[4-methoxy-3-(4-methylpiperazin-1-yl)phenyl]-4-[2-methyl-4-(5-methyl-1,2,4-oxadiazol-3-yl)phenyl]benzamide

    参考文献

    1. Clitherow JW, et al. J Med Chem. 1994 Jul 22;37(15):2253-7.

    2. Knobelman DA, et al. J Pharmacol Exp Ther. 2001 Sep;298(3):1083-91.

    3. De Vries P, et al. Br J Pharmacol. 1996 May;118(1):85-92.

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