产品描述
| 溶解性 | Soluble in DMSO (~14 mg/ml), DMF (~10 mg/ml), 1:1 DMF:PBS(pH 7.2) (500 ug/ml), 1:2 DMSO:PBS(pH 7.2) (500 ug/ml), water (500 ug/ml) at 25 °C, and ethanol (5 mg/ml). |
| 存贮条件 | 储存温度-20°C |
| 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 |
