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首页-小分子抑制剂&激动剂-GPCR-Neurotensin Receptor-SR 48692
SR 48692

Chemical Structure : SR 48692

CAS No.: 146362-70-1

SR 48692 (Meclinertant;SR48692;SR-48692)

货号: PC-60947Not For Human Use, Lab Use Only.

SR 48692 (Meclinertant) is a potent, selective and orally active nonpeptide antagonist of the neurotensin receptor with IC50 of 0.99 nM (guinea pig), without any intrinsic agonist activity.

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

    生物&药学活性

    SR 48692 (Meclinertant) is a potent, selective and orally active nonpeptide antagonist of the neurotensin receptor with IC50 of 0.99 nM (guinea pig), without any intrinsic agonist activity.
    SR 48692 (Meclinertant) blocks K(+)-evoked release of [3H]dopamine stimulated by neurotensin in guinea pig striatal slices with IC50 of 0.46 nM, competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization with pA2 of 8.13 in H29 cells.
    SR 48692 (Meclinertant) reverses the turning behavior induced by intrastriatal injection of neurotensin in mice.

    物理化学性质&存储条件

    分子量 587.073
    分子式 C32H31ClN4O5
    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

    (1r,3r,5r,7r)-2-(1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)-1H-pyrazole-3-carboxamido)adamantane-2-carboxylic acid

    参考文献

    1. Dubuc I, et al. Br J Pharmacol. 1994 Jun;112(2):352-4.

    2. Steinberg R, et al. Neuroscience. 1994 Apr;59(4):921-9.

    3. Brouard A, et al. Eur J Pharmacol. 1994 Mar 3;253(3):289-91.

    4. Gully D, et al. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):65-9.

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