Name: URB754
Rating: 5 (10 reviews)

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HIT ID:HIT212029475
Cas No:86672-58-4
常用名:URB754
IUPAC:6-methyl-2-[(4-methylphenyl)amino]-4H-3,1-benzoxazin-4-one
IUPAC:6-methyl-2-[(4-methylphenyl)amino]-4H-3,1-benzoxazin-4-one
InChI key:GFWNGVKCDGYFKG-UHFFFAOYSA-N

分子式:C16H14N2O2
分子量:266.3
氢键供体数 (HBD):1
氢键受体数 (HBA):4
LogP:2.22
SMILES:Cc1ccc(Nc2nc3ccc(C)cc3c(=O)o2)cc1
SMILES:Cc1ccc(Nc2nc3ccc(C)cc3c(=O)o2)cc1

URB754 is a potent and noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 value of 200 nM for the recombinant rat brain enzyme. However, it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 μM. There is evidence that the MAGL inhibitory activity of URB754 may be attributed to the impurity bis(methylthio)mercurane (IC50 = 11.9 nM for rat recombinant MAGL) that is found in commercial preparations. URB754 inhibits rat brain fatty acyl amide hydrolase (FAAH) with an IC50 value of 32 μM and binds weakly to the rat central cannabinoid (CB1) receptor with an IC50 value of 3.8 μM. It does not inhibit COX-1 or COX-2 at concentrations up to 100 μM. Inhibition of MAGL hydrolysis of 2-arachidonoyl glycerol (2-AG) is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.

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