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URB754
Cayman Chemical Item Number 10007691
Description
2-Arachidonoyl glycerol (2-AG) is an endogenous agonist of the central cannabinoid (CB1) receptor.1↗,2↗ It is present at relatively high levels in the central nervous system and is the most abundant molecular species of monoacylglycerol found in rat brain.2↗,3↗ Monoacylglycerol lipase (MGL) hydrolyzes 2-AG to arachidonic acid and glycerol, thereby terminating its biological actions.4↗ URB754 is reported to be a potent, noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 of 200 nM for the recombinant rat brain enzyme.5↗ However, data from other labs indicates that it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 µM.6↗,7↗ It inhibits rat brain fatty acyl amide hydrolase (FAAH) with an IC50 of 32 µM and binds weakly to the rat central cannabinoid (CB1) receptor with an IC50 of 3.8 µM.5↗ It does not inhibit cyclooxygenase-1 (COX-1) or COX-2 at concentrations up to 100 µM.5↗ Inhibition of 2-AG hydrolysis is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.8↗
Formal Name
6-methyl-2-[(4-methylphenyl)amino]-1-benzoxazin-4-one
CAS Number 86672-58-4
Molecular Formula C16H14N2O2
Formula Weight 266.3
Formulation A crystalline solid
Purity >98%
λmax 216, 247, 283, 348 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES Cc1ccc(cc1)Nc1nc2ccc(C)cc2c(=O)o1
InCHI Code 1S/C16H14N2O2/c1-10-3-6-12(7-4-10)17-16-18-14-8-5-11(2)9-13(14)15(19)20-16/h3-9H,1-2H3,(H,17,18)
InCHI Key GFWNGVKCDGYFKG-UHFFFAOYSA-N |