化学性质:
规格 | 5mg 10mg 25mg 50mg |
CAS | 55224-94-7 |
别名 | N/A |
化学名 | (2E,3Z)-4-(4-chlorophenyl)-3-methylbut-3-en-2-one oxime |
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°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
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.
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