URB-754A potent and selective inhibitor of MAG lipase which selectively raises levels of 2AG

URB-754 (CAS 86672-58-4)

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Synonym: 6-Methyl-2-(p-tolylamino)-4H-benzo[d][1,3]oxazin-4-one; 6-methyl-2-((4-methylphenyl)amino)-4h-3,1-benzoxazin-4-one
Application: A potent and selective inhibitor of MAG lipase which selectively raises levels of 2AG
CAS Number: 86672-58-4
Purity: ≥98%
Molecular Weight: 266.3
Molecular Formula: C16H14N2O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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URB-754 was originally described as a potent and selective inhibitor of MAG lipase which selectively raises levels of 2-arachidonoylglycerol (2AG). Subsequent studies have shown that that URB-754 does not inhibit recombinant MAG Lipase and that the original activity was due to a contaminant, bis(methylthio)mercurane, in another commercial source. URB-754 is an inhibitor of FAAH.


References

1. Makara, J.K., et al. 2005. Nat. Neurosci. 8: 1139-1141. PMID: 16116451
2. Saario, S.M., et al. 2006. Chem. Biol. 13: 811-814. PMID: 16931330
3. Vandevoorde, S., et al. 2007. Brit. J. Pharmacol. 150: 186-191. PMID: 17143303

Physical State :
Solid
Solubility :
Soluble in DMSO (15 mg/mL), and DMF. Insoluble in water.
Storage :
Store at -20° C
Melting Point :
≥ 260° C (lit.)
Boiling Point :
~434.0° C at 760 mmHg (Predicted)
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.63
IC50 :
monoacylglycerol lipase (MAGL): IC50 = 200 nM (rat); brain fatty acyl amide hydrolase (FAAH) : IC50 = 32 µM (rat); central cannabinoid (CB1) receptor : IC50 = 3.8 µM (rat)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
848487
SMILES :
CC1=CC=C(C=C1)NC2=NC3=C(C=C(C=C3)C)C(=O)O2

Download SDS (MSDS)

Certificate of Analysis

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