A potent and noncompetitive inhibitor of MAGL (IC50 = 200 nM for the recombinant rat brain enzyme); inhibits rat brain FAAH (IC50 = 32 µM); binds weakly to the rat CB1 receptor (IC50 = 3.8 µM); does not inhibit COX-1 or COX-2 at concentrations up to 100 µM

URB754 – 100 mg

Brand:
Cayman
CAS:
86672-58-4
Storage:
-20
UN-No:
Non-Hazardous - /

URB754 is a potent and noncompetitive inhibitor of monoacylglycerol lipase (MAGL), exhibiting an IC50 value of 200 nM for the recombinant rat brain enzyme.{13321} However, it does not inhibit human recombinant, rat brain, or mouse brain MAGL at concentrations up to 100 µM.{14400,16299} 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.{37077} 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.{13321} It does not inhibit COX-1 or COX-2 at concentrations up to 100 µM.{13321} 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.{13217}  

 

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SKU: 10007691 - 100 mg Category:

Description

A potent and noncompetitive inhibitor of MAGL (IC50 = 200 nM for the recombinant rat brain enzyme); inhibits rat brain FAAH (IC50 = 32 µM); binds weakly to the rat CB1 receptor (IC50 = 3.8 µM); does not inhibit COX-1 or COX-2 at concentrations up to 100 µM

Formal name: 6-methyl-2-[(4-methylphenyl)amino]-1-benzoxazin-4-one

Synonyms: 

Molecular weight: 266.3

CAS: 86672-58-4

Purity: >98%

Formulation: A crystalline solid

Application||Product Type|Biochemicals|Receptor Pharmacology||Product Type|Biochemicals|Small Molecule Inhibitors|Fatty Acid Metabolism||Product Type|Biochemicals|Small Molecule Inhibitors|Glycerolipid Lipases||Research Area|Lipid Biochemistry|Endocannabinoid/Endocannabinoid-like||Research Area|Lipid Biochemistry|Glycerolipids|Lipases||Research Area|Neuroscience|Cannabinoid Research|CB1 & CB2 Receptors||Research Area|Neuroscience|Cannabinoid Research|Endocannabinoids||Research Area|Neuroscience|Pain Research

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