4-Quinolone-3-Carboxamide Furan CB2 Agonist

Selective CB2 agonist

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库存: 现货

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1mg

￥737.00

590.00

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5mg

￥3275.00

2620.00

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10mg

￥5750.00

4600.00

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25mg

￥12475.00

9980.00

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货号: ajci15942
CAS: 1314230-75-5
别名: 4Q3C CB2 Agonist
分子式: C30H36N2O4
分子量: 488.6
纯度: >98%
溶解度: ≤30mg/ml in ethanol;3mg/ml in DMSO;3mg/ml in dimethyl formamide
储存: Store at -20°C
库存: 现货

Background

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).