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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-Trpvicin
Trpvicin

Chemical Structure : Trpvicin

CAS No.: 2019994-90-0

Trpvicin

货号: PC-49411Not For Human Use, Lab Use Only.

Trpvicin is a potent and subtype-selective inhibitor of TRPV3 with IC50 of 0.41 and 0.22 uM for hTRPV3-WT and hTRPV3-G573S mutant, respectively.

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

生物&药学活性

Trpvicin is a potent and subtype-selective inhibitor of TRPV3 with IC50 of 0.41 and 0.22 uM for hTRPV3-WT and hTRPV3-G573S mutant, respectively.
Trpvicin displays no significant inhibitory activities against hTRPV1, mTRPV2 and hTRPV4-6.
Trpvicin inhibits the TRPV3 channel by stabilizing it in a closed state.
Trpvicin accesses additional binding sites inside the central cavity of the G573S mutant to remodel the channel symmetry and block the channel.
Trpvicin exhibits pharmacological potential in the inhibition of itch and hair loss in mouse models.

物理化学性质&存储条件

分子量 478.450
分子式 C20H17F3N6O3S
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

N-(5-(2-(2-cyanopropan-2-yl)pyridin-4-yl)-4-(trifluoromethyl)thiazol-2-yl)-4,6-dimethoxypyrimidine-5-carboxamide

参考文献

1. Fan J, et al. Nat Chem Biol. 2022 Oct 27. doi: 10.1038/s41589-022-01166-5.

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