URB754 |
| カタログ番号GC41599 |
URB754 は、200 nM の IC50 を持つエンドカンナビノイド不活化酵素モノアシルグリセロール リパーゼ (MGL) の強力な阻害剤です 。
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Cas No.: 86672-58-4
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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