URB754
MGL抑制剂；6-甲基-2-[(4-甲基苯基)氨基]-4H-3,1-benzoxazine-4-one
URB754
MGL抑制剂；6-甲基-2-[(4-甲基苯基)氨基]-4H-3,1-benzoxazine-4-one
URB754
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产品编号： CUR822000
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CAS号： 86672-58-4
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分子式：C16H14N2O2
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分子量：266.29
英文别名：
6-Methyl-2-[(4-methylphenyl)amino]-4H-3,1-benzoxazine-4-one
熔点：
201-203°C
可溶性：
DMSO
性状：
Off-White Solid
储存条件：
Refrigerator
参考文献：
Makara, J.K., et al.: Nat. Neurosci., 8, 1139 (2005)
URB754 is a potent, noncompetitive inhibitor of MGL, exhibiting an IC50 of 200 nM for the recombinant rat brain enzyme. It inhibits rat brain fatty acyl amide hydrolase (FAAH) less effectively with an IC50 of 32 µM and binds weakly to the rat 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.
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