应用 |
A cell permeable carbamate and potent inhibitor of fatty acid amide hydrolase (FAHH) |
产品介绍 |
URB597是一种口服生物有效的FAAH抑制剂,IC50为4.6 nM,对其他大麻黄素相关靶点没有抑制活性。Phase 1。 |
备注 |
URB597 is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets. |
生化机理 |
FAAH Inhibitor II is a cell-permeable carbamate compound that acts as a potent, selective, and irreversible inhibitor of FAAH (fatty acid amide hydrolase; IC50 = 4.6 nM in brain membranes). Shown to block anandamide breakdown in rat cortical neurons (IC50 = 500 pM) and modulate anxiety in rats (ID50 = 0.15 mg/Kg). Does not affect the activities of several serine hydrolases (IC50 > 30 μM), including AChE (acetylcholinesterase), BCh (butyrylcholinesterase) and MGL (monoglyceride lipase). FAAH Inhibitor II does not interfere with the binding of anandamide to cannabinoid receptors CB1 and CB2 (IC50 > 100 μM), as well as several ion-channels and neurotransmitter transporters. |
别名 |
KDS-4103;N-环己基氨基甲酸 3'-(氨基甲酰基)[1,1'-联苯]-3-基酯;URB597; KDS-4103;URB 597; KDS 4103; KDS4103;Cyclohexylcarbamic acid 3′-carbamoyl-biphenyl-3-yl ester |