MAGL inhibitor 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. 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. 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. It does not inhibit cyclooxygenase-1 (COX-1) or COX-2 at concentrations up to 100 µM. Inhibition of 2-AG hydrolysis is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.
To inquire quotation or to ask questions, please send email to sales@chemrenpharm.com to describe your needs. A representative will respond your email shortly. We offer big discount for orders of bulk quantities.
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M.Wt: 266.3
MF:C16H14N2O2
Appearance:a crystalline solid
Purity:>98%
Storage:at -20”ę 2 years
MAGL inhibitor 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. 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. 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. It does not inhibit cyclooxygenase-1 (COX-1) or COX-2 at concentrations up to 100 µM. Inhibition of 2-AG hydrolysis is associated with enhanced stress-induced analgesia and may represent a novel drug target in pain and stress management.
To inquire quotation or to ask questions, please send email to sales@chemrenpharm.com to describe your needs. A representative will respond your email shortly. We offer big discount for orders of bulk quantities.