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4-Quinolone-3-Carboxamide Furan CB2 Agonist
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。
4-Quinolone-3-Carboxamide Furan CB2 Agonist图片
CAS NO:1314230-75-5
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
4-Quinolone-3-Carboxamide Furan CB2 Agonist 是一种有效的选择性 CB2(大麻素 2 型)受体激动剂,Ki 为 8.5 nM。
Cas No.1314230-75-5
别名4Q3C CB2 Agonist
化学名6-(2-furanyl)-1,4-dihydro-8-methoxy-4-oxo-1-pentyl-N-tricyclo[3.3.1.13,7]dec-1-yl-3-quinolinecarboxamide
Canonical SMILESO=C(C1=CN(CCCCC)C2=C(C=C(C3=CC=CO3)C=C2OC)C1=O)N[C@@]45CC6C[C@H](C5)C[C@H](C4)C6
分子式C30H36N2O4
分子量488.6
溶解度≤30mg/ml in ethanol;3mg/ml in DMSO;3mg/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

Ki: 8.5 nM

4-Quinolone-3-Carboxamide Furan CB2 Agonist is a high-affinity ligand of CB2.

The endocannabinoid system consists of endogenous cannabinoids (endocannabinoids), cannabinoid receptors (primarily CB1 and CB2), and the enzymes that synthesize and degrade endocannabinoids.

In vitro: Previous study found that 4-Quinolone-3-Carboxamide Furan CB2 Agonist (4g) was devoid of any potential “indirect” agonist activity at cannabinoid receptors, exerted by prolonging the lifespan of endocannabinoids because 4g at up to a 10 μM concentration did not inhibit anandamide or 2-AG degradation by FAAH or MAGL, respectively. In cytotosicity study, 4g was tested at 1 μM and the results showed that it exhibited very low or no cytotoxicity, the cell viability being above 95% after a 72 h treatment [1].

In vivo: In animal study, 4g was found to have antinociceptive activity in the formalin test in mice. Moreover, 4g was very potent with maximal effect being reached at the 1 mg/kg dose and efficacious also on the first phase of the nocifensive response. The effect of 4g could be strongly reduced by the addition of AM630, a CB2-selective antagonist/inverse agonist, therefore demonstrating that 4g might act as a potent and selective CB2 agonist [1].

Clinical trial: Up to now, 4-Quinolone-3-Carboxamide Furan CB2 Agonist is still in the preclinical development stage.

Reference:
[1] S.  Pasquini, M. De Rosa, V. Pedani, et al. Investigations on the 4-quinolone-3-carboxylic acid motif. 4. Identification of new potent and selective ligands for the cannabinoid type 2 receptor with diverse substitution patterns and antihyperalgesic effects in mice. Journal of Medicinal Chemistry 54, 5444-5453 (2011).