Photochromic TrpA1 Channel Activator, Optovin-Calbiochem

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一般描述

A rhodanine derivative that acts as a reversible, photoactivated (λ_{max= 415 nm), and highly TrpA1-selective channel activator, presumably by a light-activated cysteine alkylation mechanism via the α,β-unsaturated alkene group of Optovin rhodanine moiety, and enables light-induced primary murine DRG calcium response in a TrpA1-dependent and HC-030031- (Cat. No. 648485) blockable manner, allowing light-induced activation only in hTrpA1-expressing, but not TrpV1- or TrpM8-expressing, HEK293T transfectants. Itsin vivoefficacy is demonstrated in light-induced zebrafish motor activity (EC50/ECmax= 2 ?M/3 ?M; with >1.6 ?W/min 387-405 nm excitation) and low power 405 nm laser-induced head shake/twitch response in mice (0.3 ?mol Optovin/20 uL DMSO/ear applied atopically before laser illumination). Exhibits little or no inhibitory activity toward hERG or a panel of 50 human and rodent CNS receptors, channels, and transporters.
A rhodanine derivative that acts as a reversible, photoactivated (λmax= 415 nm), and highly TrpA1-selective channel activator and enables light-induced primary murine DRG calcium response in a TrpA1-dependent and HC-030031- (Cat. No. 648485) blockable manner, allowing light-induced activation only in hTrpA1-expressing, but not TrpV1- or TrpM8-expressing, HEK293T transfectants. Itsin vivoefficacy is demonstrated in light-induced zebrafish motor activity (EC50/ECmax= 2 ?M/3 ?M) and low power 405 nm laser-induced head twitch response in mice (0.3 ?mol Optovin/20 uL DMSO/ear applied atopically). Exhibits little or no inhibitory activity toward hERG or a panel of 50 human and rodent CNS receptors, channels, and transporters.}

生化/生理作用

Primary Target
TrpA1

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

其他说明

Kokel, D., et al. 2013,Nat. Chem. Biol.9,257.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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