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AM4113
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。
AM4113图片
CAS NO:614726-85-1
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
AM4113 是从专利 WO2016184310A1 化合物 3 中提取的 caimabinoid 1 (CB1) 拮抗剂,在体内抑制 CB1,IC50 为 25.5 nM。
Cas No.614726-85-1
别名AM4113
化学名5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide
Canonical SMILESClC1=CC(Cl)=CC=C1N2C(C3=CC=C(Cl)C=C3)=C(C)C(C(N)=O)=N2
分子式C17H12Cl3N3O
分子量380.7
溶解度≤0.5mg/ml in ethanol;3mg/ml in DMSO;10mg/ml in dimethyl formamide
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

AM4113, a pyrazole analog structurally related to SR141716 and AM251, is a novel cannabinoid CB1 neutral antagonist. AM4113 suppressed food intake and food-reinforced behavior in rats.

In vitro: AM4113 was able to bind with high affinity to CB1 receptors, exhibiting 100-fold selectivity for CB1 against CB2 receptors. The Ki value for CB1 was 0.897 ± 0.44 nM, while the Ki value for hCB2 was 92 ± 6.9 nM [1].

In vivo: In rats, treatment with AM4113 (2.0 and 4.0 mg/kg) attenuated the AM411-induced locomotor suppression and analgesia. In addition, 4.0 mg/kg AM4113 alone significantly suppressed locomotor activity when compared with vehicle. AM4113 dose-dependently decreased lever pressing on an FR1 schedule. AM4113 produced conditioned taste avoidance and suppression of ingestive (hedonic) taste reactivity scores in a dose-dependent manner [1]. AM4113 didn’t induce signs of nausea [1].

Reference:
[1] Sink K S, McLaughlin P J, Wood J A T, et al.  The novel cannabinoid CB1 receptor neutral antagonist AM4113 suppresses food intake and food-reinforced behavior but does not induce signs of nausea in rats[J]. Neuropsychopharmacology, 2008, 33(4): 946-955.