4-Quinolone-3-Carboxamide Furan CB2 Agonist

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4-Quinolone-3-Carboxamide Furan CB2 Agonist manufacturers

4-Quinolone-3-Carboxamide Furan CB2 Agonist Basic information
Product Name:4-Quinolone-3-Carboxamide Furan CB2 Agonist
Synonyms:4-Quinolone-3-Carboxamide Furan CB2 Agonist;N-(1-adamantyl)-6-(furan-2-yl)-8-methoxy-4-oxo-1-pentylquinoline-3-carboxamide;3-Quinolinecarboxamide, 6-(2-furanyl)-1,4-dihydro-8-methoxy-4-oxo-1-pentyl-N-tricyclo[3.3.1.13,7]dec-1-yl-;CB2 receptor agonist 2
CAS:1314230-75-5
MF:C30H36N2O4
MW:488.62
EINECS:
Product Categories:
Mol File:1314230-75-5.mol
4-Quinolone-3-Carboxamide Furan CB2 Agonist Structure
4-Quinolone-3-Carboxamide Furan CB2 Agonist Chemical Properties
storage temp. Store at -20°C
solubility ≤30mg/ml in ethanol;3mg/ml in DMSO;3mg/ml in dimethyl formamide
form crystalline solid
color White to light yellow
Safety Information
MSDS Information
4-Quinolone-3-Carboxamide Furan CB2 Agonist Usage And Synthesis
UsesCB2 receptor agonist 2 is a potent and selective agonist for the CB2 (cannabinoid type 2) receptor with a Ki of 8.5 nM. CB2 receptor agonist 2 has high affinity and selectivity for CB2[1].
Biological Activityki: 8.5 nm4-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 vitroprevious 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 vivoin 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].
IC 50CB2: 8.5 nM (Ki)
references[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).
4-Quinolone-3-Carboxamide Furan CB2 Agonist Preparation Products And Raw materials
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