PHOTOCHROMIC TRPA1 CHANNEL ACTIVATOR OPTOVIN (C15-1304-303)

General description

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. Its in vivo efficacy is demonstrated in light-induced zebrafish motor activity (EC50/ECmax = 2 µM/3 µM; with >1.6 µW/min 387-405 nm excitation) and low power 405 nm laser-induced head shake/twitch response in mice (0.3 µmol 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 (λ_max = 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. Its in vivo efficacy is demonstrated in light-induced zebrafish motor activity (EC₅₀/EC_max = 2 µM/3 µM) and low power 405 nm laser-induced head twitch response in mice (0.3 µmol 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.

Biochem/physiol Actions

Primary Target
TrpA1

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

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

Legal Information

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

Molecular Weight: 315.41. Empirical Formula: C₁₅H₁₃N₃OS₂. Assay: ≥. 95% (HPLC). Quality Level: 100. form: powder. potency: 2 . μ. M EC₅₀. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, protect from light. color: yellow. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.