Colivin

Chemical Structure : Colivin

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货号: PC-27644Not For Human Use, Lab Use Only.

Colivin is a potent, selective and orally bioactive TRPV3 inhibitor/antagonist, suppresses hTRPV3 activity with IC50 of 0.23 uM in Fluorescence-based Ca2+ influx assays, inhibits hTRPV3 and mTRPV3 equally.

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生物&药学活性

Colivin is a potent, selective and orally bioactive TRPV3 inhibitor/antagonist, suppresses hTRPV3 activity with IC50 of 0.23 uM in Fluorescence-based Ca2+ influx assays, inhibits hTRPV3 and mTRPV3 equally.
Colivin concentration-dependently suppresses 2-APB (100 μM)-induced outward and inward currents in HEK-293 cells transiently expressing hTRPV3 with IC50 values of 0.24 μM and 0.20 μM at +100 and −100 mV, respectively.
Colivin has IC50 values of 0.24 μM and 0.20 μM at +100 and −100 mV, respectively, in HEK-293 cells transiently expressing mTRPV3.
Colivin acts as a non-competitive inhibitor of TRPV3.
Colivin has no significant effect on Ca2+ influx mediated by hTRPV1, mTRPV2, hTRPV4, hTRPA1, and hTRPM8 at 10 uM.
Colivin binds to the vanilloid site of hTRPV3.
Colivin stabilizes TRPV3 in a non-conducting conformation.
Colivin (10 mg/kg, intragastric administration) ameliorates DSS-induced ulcerative colitis (UC) in mice.

物理化学性质&存储条件

分子量	480.43
分子式	C24H17D2F5N2O3
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	(3-(4'-fluoro-3-(hydroxymethyl-d2)-2'-(trifluoromethoxy)-[1,1'-biphenyl]-4-yl)pyrrolidin-1-yl)(5-fluoropyridin-2-yl)methanone

参考文献

1. Wang Y, et al. EMBO J. 2026 Aug 13. doi: 10.1038/s44318-026-00896-9.

Colivin

生物&药学活性

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Colivin

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