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首页-小分子抑制剂&激动剂-GPCR-mAChR-V0162
V0162

Chemical Structure : V0162

CAS No.: 147780-50-5

V0162 (V 0162;V-0162;(R)-Mequitazine;VO-162)

货号: PC-61048Not For Human Use, Lab Use Only.

V0162 ((R)-Mequitazine) is a high affinity and long-acting antagonist of human M3 muscarinic acetylcholine receptor with pKi of 9.03-9.21.

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

    生物&药学活性

    V0162 ((R)-Mequitazine) is a high affinity and long-acting antagonist of human M3 muscarinic acetylcholine receptor with pKi of 9.03-9.21.
    V0162 acts an inverse agonist for hM3R-mediated reporter gene activation (pIC50=7.56), with much the same efficacy as atropine, ipratropium and tiotropium.
    V0162 antagonizes acetylcholine-mediated contractions in a human bronchial preparation.

    物理化学性质&存储条件

    分子量 322.47
    分子式 C20H22N2S
    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

    10-[(3R)-1-azabicyclo[2.2.2]oct-3-ylmethyl]-10H-phenothiazine

    参考文献

    1. Devillier P, et al. Respir Res. 2015 Jun 8;16:68.

    2. Heusler P, et al. Pharmacol Res. 2015 Oct;100:117-26.

    3. Mastrodicasa MA, et al. Expert Opin Investig Drugs. 2017 Feb;26(2):161-174.

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