Topic
URB754
About: URB754 is a research topic. Over the lifetime, 2 publications have been published within this topic receiving 55 citations. The topic is also known as: urb-754.
Papers
TL;DR: It is shown that the MGL-inhibitory activity attributed to URB754 is in fact due to a chemical impurity present in the commercial sample, identified as bis(methylthio)mercurane.
Abstract: The compound URB754 was recently identified as a potent inhibitor of the endocannabinoid-deactivating enzyme monoacylglycerol lipase (MGL) by screening of a commercial chemical library. Based on HPLC/MS, NMR and EI/MS analyses, the present paper shows that the MGL-inhibitory activity attributed to URB754 is in fact due to a chemical impurity present in the commercial sample, identified as bis(methylthio)mercurane. Although this organomercurial compound is highly potent at inhibiting MGL (IC50 = 11.9 +/- 1.1 nM), its biological use is prohibited by its toxicity and target promiscuity.
23 citations
TL;DR: URB754 was not able to block the endocannabinoid-hydrolyzing enzymes and cannot serve as a lead structure for future development of MGL-specific inhibitors.
Related Topics (5)
Performance Metrics
| Year | Papers |
|---|---|
| 2007 | 1 |
| 2006 | 1 |