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AM630
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。
AM630图片
CAS NO:164178-33-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议
100mg电议

产品介绍

CB2 receptor antagonist,selective and competitive

Cas No.164178-33-0
别名[6-碘-2-甲基-1-[2-(4-吗啉基)乙基]-1H-吲哚-3-基](4-甲氧基苯基)甲酮,AM 630;AM-630
化学名[6-iodo-2-methyl-1-(2-morpholin-4-ylethyl)indol-3-yl]-(4-methoxyphenyl)methanone
Canonical SMILESCC1=C(C2=C(N1CCN3CCOCC3)C=C(C=C2)I)C(=O)C4=CC=C(C=C4)OC
分子式C23H25IN2O3
分子量504.36
溶解度3mg/mL in DMSO; 10mg/mL in DMF; Sparingly soluble in aqueous buffers
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
产品描述

AM630 is a selective and competitive antagonist of cannabinoid receptors with Ki values of 5 μM and 31.2 nM for CB1 receptor and CB2 receptor, respectively [1].

In CB1-transfected CHO cells, AM630 significantly inhibited the production of cAMP stumilated by forskolin. In CB2-transfected cells, AM630 promoted forskolin to stimulate cyclic AMP production with EC50 value of 230.4 nM. AM630 also exerted to have inhibitory effect on the binding of GTPγS to membranes from CB2-transfected cells. Besides that, AM630 was found to activate the TRPA1 channels and subsequently desensitizing TRPA1 and TRPV1 channels in TG sensory neurons. Moreover, AM630 significantly weakened the thermal hyperalgesia induced by CAP (capsaicin) in WT mice [1, 2].

References:
1. Ross R A, Brockie H C, Stevenson L A, et al. Agonist-inverse agonist characterization at CB1 and CB2 cannabinoid receptors of L759633, L759656 and AM630. British journal of pharmacology, 1999, 126(3): 665-672.
2. Patil M, Patwardhan A, Salas M M, et al. Cannabinoid receptor antagonists AM251 and AM630 activate TRPA1 in sensory neurons. Neuropharmacology, 2011, 61(4): 778-788.