AZ465 | TRPA1 inhibitor | Probechem Biochemicals

Chemical Structure : AZ465

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AZ465 (AZ-465)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	419.53
分子式	C24H29N5O2
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	(R)- N-(1-(4-cyanophenyl)-3,3-dimethyl-1-oxobutan-2-yl)-4-(6-methylpyridin-2-yl)piperazine-1-carboxamide

参考文献

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

AZ465 (AZ-465)

生物&药学活性

物理化学性质&存储条件

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AZ465 (AZ-465)

生物&药学活性

物理化学性质&存储条件

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