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Photochromic TrpA1 Channel Activator, Optovin-Calbiochem
半岛bd体育手机客户端 编号: | 4083717 |
规格: | A rhodanine-derived, reversible, photoactivated, TrpA1-selective channel activator. |
包装规格: | 10 MG |
半岛bd体育手机客户端 类别: | 进口试剂 |
品牌: | Sigma-Aldrich |
优惠价: | 立即咨询 |
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别名
Photochromic TrpA1 Channel Activator, Optovin-Calbiochem
(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
基本信息
Empirical Formula【经验(实验)分子式】 | C15H13N3OS2 |
Molecular weight | 315.41 |
General description【一般描述】 | A rhodanine derivative that acts as a reversible, photoactivated (λmax = 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 (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. Its in vivo efficacy is demonstrated in light-induced zebrafish motor activity (EC50/ECmax = 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【生化/生理作用】 | Primary Target TrpA1 |
Warning【警告】 | Toxicity: Standard Handling (A) |
Other Notes【其他说明】 | Kokel, D., et al. 2013, Nat. Chem. Biol.9, 257. |
Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
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性质
Quality Level【质量水平】 | 100 |
Assay【测定】 | ≥95% (HPLC) |
form【形式】 | powder |
potency【效能】 | 2 μM EC50 |
manufacturer/tradename | Calbiochem® |
storage condition【储存条件】 | OK to freeze protect from light |
color【颜色】 | yellow |
solubility【溶解性】 | DMSO: 100 mg/mL |
storage temp.【储存温度】 | 2-8℃ |
packaging【包装】 | Packaged under inert gas |
安全信息
Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
WGK | WGK 3 |