CAS NO: | 1314230-75-5 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
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 SMILES | O=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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: |