5.05206

Photochromic TrpA1 Channel Activator, Optovin

• 別名: Photochromic TrpA1 Channel Activator, Optovin, (E)-5-((2,5-dimethyl-1-(pyridin-3-yl)-1H-pyrrol-3-yl)methylene)-2-thioxothiazolidin-4-one, PDSP 22594, Transient Receptor Potential A1 Ion Channel Activator I, TrpA1 Channel Activator I
• 実験式（ヒル表記法）: C₁₅H₁₃N₃OS₂
• CAS番号: 348575-88-2
• 分子量: 315.41
• MDL番号: MFCD02219276
• UNSPSCコード: 41106609
• NACRES: NA.77

特性

• アッセイ: ≥95% (HPLC)
• 品質水準: 100
• フォーム: powder
• 有効性: 2 μM EC₅₀
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: yellow
• 溶解性: DMSO: 100 mg/mL
• 保管温度: 2-8°C
• SMILES記法: S1C(=S)NC(=O)C1=Cc2c([n](c(c2)C)c3cnccc3)C
• InChI: 1S/C15H13N3OS2/c1-9-6-11(7-13-14(19)17-15(20)21-13)10(2)18(9)12-4-3-5-16-8-12/h3-8H,1-2H3,(H,17,19,20)
• InChI Key: YISGMOZSGOGYOU-UHFFFAOYSA-N

詳細

詳細

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.}

生物化学的／生理学的作用

Primary Target
TrpA1

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable