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V0162

Chemical Structure : V0162

CAS No.: 147780-50-5

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

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 322.47
    Formula C20H22N2S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

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

    References

    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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