Description
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 . 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 . Clinical trial: Up to now, 4-Quinolone-3-Carboxamide Furan CB2 Agonist is still in the preclinical development stage.
Product information
CAS Number: 1314230-75-5
Molecular Weight: 488.62
Formula: C30H36N2O4
Chemical Name: N-[(3R,5S)-adamantan-1-yl]-6-(furan-2-yl)-8-methoxy-4-oxo-1-pentyl-1,4-dihydroquinoline-3-carboxamide
Smiles: COC1=CC(=CC2=C1N(CCCCC)C=C(C2=O)C(=O)N[C@]12CC3C[C@H](C1)C[C@H](C2)C3)C1=CC=CO1
InChiKey: NXZZNXUALWSJSD-ZMMUGYPNSA-N
InChi: InChI=1S/C30H36N2O4/c1-3-4-5-8-32-18-24(29(34)31-30-15-19-10-20(16-30)12-21(11-19)17-30)28(33)23-13-22(25-7-6-9-36-25)14-26(35-2)27(23)32/h6-7,9,13-14,18-21H,3-5,8,10-12,15-17H2,1-2H3,(H,31,34)/t19-,20+,21?,30-
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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