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AZ465

Chemical Structure : AZ465

CAS No.: 1373046-67-3

AZ465 (AZ-465)

Catalog No.: PC-49702Not For Human Use, Lab Use Only.

AZ465 (AZ-465) is a potent selective TRPA1 inhibitor, potently inhibitor Zn2+ (100 μM)- and O-chlorobenzylidene malononitrile (CS) (10 nM)-induced TRPA1 activation with IC50 of 85 nM and 20 nM, respectively.

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    Biological Activity

    AZ465 (AZ-465) is a potent selective TRPA1 inhibitor, potently inhibitor Zn2+ (100 μM)- and O-chlorobenzylidene malononitrile (CS) (10 nM)-induced TRPA1 activation with IC50 of 85 nM and 20 nM, respectively.
    AZ465 displays a high degree of selectivity for TRPA1, with no effect on the responses of human TRPV1- and TRPM8-expressing cells to capsaicin or menthol, respectively.
    AZ465 binds reversibly in the transmembrane region of human TRPA1.
    AZ465 inhibits cinnamaldehyde-induced TRPA1 activation in hTRPA1 and mouse/human chimeric TRPA1 channels, but not in mTRPA1.
    AZ465 (30 μM) reversibly inhibits cinnamaldehyde-activated TRPA1 currents in whole-cell patch-clamp experiments.
    |AZ465 (10 and 50 μM) produced a significant inhibition of CS-evoked CGRP release in human dental pulp.

    Physicochemical Properties

    M.Wt 419.53
    Formula C24H29N5O2
    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

    (R)- N-(1-(4-cyanophenyl)-3,3-dimethyl-1-oxobutan-2-yl)-4-(6-methylpyridin-2-yl)piperazine-1-carboxamide

    References

    1. Eva Nyman, et al. J Pain Res. 2013;6:59-70. doi: 10.2147/JPR.S37567.

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