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AP 18
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AP 18图片
CAS NO:55224-94-7
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
AP 18 是一种有效的选择性 TRPA1 抑制剂,可通过 50 μM C\u200b\u200binnamaldehyde 阻断 TRPA1 的活化,对人和小鼠 TRPA1 的 IC50 分别为 3.1 μM 和 4.5 μM。
Cas No.55224-94-7
别名4-(4-氯苯基)-3-甲基丁-3-烯-2-肟
化学名(2E,3Z)-4-(4-chlorophenyl)-3-methylbut-3-en-2-one oxime
Canonical SMILESClC1=CC=C(C=C1)/C=C(C)\C(C)=N\O
分子式C11H12ClNO
分子量209.67
溶解度20 mg/ml in enathol; 30 mg/ml in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
文献引用
产品描述

AP-18 is a selective channel blocker which can reversibly inhibit TRPA1 of human and mouse with IC50 of 3.1 μM and 4.5 μM, respectively.

TRPV1 belongs to the transient receptor potential family of cation channels and is activated by low pH, heat, and capsaicin. Originally known as a noxious cold-activated ion channel, TRPA1 is expressed in the same sensory neurons as TRPV1 and is activated directly by a variety of chemicals via covalent modification, and indirectly through G-protein coupled receptors.

In odontoblasts, AP18 is effective to inhibit the increase in intracellular Ca2+ concentration induced by allyl isothiocyanate and cinnamaldehyde (the TRPA1 agonists) 1.

In vivo, AP-18 blocks the transient receptor potential ankyrin 1 receptors and can reduce chronic pain associated with arthritis. This product is also capable to induce cinnamaldehyde-induced nociception and to block cold- and mustard oil-induced activation of mouse TRPA1 but not capsaicin-induced activation 2. In addition, AP18 treatment reversed CFA-induced mechanical hyperalgesia in mice 2. Thus, TRPA1 is essential for sensitization of nociception.

References:
1. Egbuniwe O, Grover S, Duggal AK, et al. TRPA1 and TRPV4 activation in human odontoblasts stimulates ATP release. Journal of dental research. 2014;93(9):911-917.
2. Petrus M, Peier AM, Bandell M, et al. A role of TRPA1 in mechanical hyperalgesia is revealed by pharmacological inhibition. Molecular pain. 2007;3:40.