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4-Quinolone-3-Carboxamide CB2 Ligand
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 CB2 Ligand图片
CAS NO:1314230-69-7
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
Cas No.1314230-69-7
别名4Q3C CB2 Ligand
化学名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=CC=C2OC)C1=O)N[C@@]34CC5C[C@H](C4)C[C@H](C3)C5
分子式C26H34N2O3
分子量422.6
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: 0.6 nM

4-Quinolone-3-Carboxamide CB2 Ligand is a ligand of the CB2 receptor.

Cannabinoids (CBs) and their synthetic analogs exhibit biochemical and pharmacological effects via interacting with the central CB1 and peripheral CB2 receptors. The CB2 receptor has emerged as a pharmacological target for treating osteoporosis, and for eliciting antinociceptive effects in various pain models .

In vitro: Previous study found that 4-Quinolone-3-carboxamide CB2 Ligand was a selective, high-affinity ligand of the CB2 receptor, displaying an in vitro Ki values of 0.6 nM for CB2 and over 10,000 nM for CB1 [1].

In vivo: In animal study, it was found that 4-quinolone-3-carboxamide CB2 Ligand at a dose of 6 mg/kg showed antinociceptive activity in a formalin test of nocifensive response in mice. Moreover, such analgesic affect could not be significantly reversed by the CB2 antagonist AM630 treatment, which suggested that 4-quinolone-3-carboxamide CB2 Ligand might behave as an inverse agonist [1].

Clinical trial: So far, no clinical study has been conducted for 4-quinolone-3-carboxamide CB2 Ligand.

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).