URB937 是一种具有口服活性和外周受限的 FAAH 抑制剂 (IC50=26.8 nM)，可增加 anandamide 水平。
| Cas No. | 1357160-72-5 |
| 化学名 | N-cyclohexyl-carbamic acid, 3'-(aminocarbonyl)-6-hydroxy[1,1'-biphenyl]-3-yl ester |
| Canonical SMILES | NC(C1=CC(C2=C(O)C=CC(OC(NC3CCCCC3)=O)=C2)=CC=C1)=O |
| 分子式 | C20H22N2O4 |
| 分子量 | 354.4 |
| 溶解度 | 10mg/mL in ethanol, or 15mg/mL in DMSO, or 10mg/mL in DMF |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | URB937 is a potent fatty acid amide hydrolase (FAAH) inhibitor (IC50 = 26.8 nM, in vitro) that does not penetrate the blood-brain barrier, thus preventing arachidonoyl ethanolamide deactivation only in peripheral tissues.[1] Its ED50 value for FAAH inhibition in brain is 200-fold higher than the ED50 value for FAAH inhibition in liver when administered systemically in mice (40 mg/kg versus 0.2 mg/kg, respectively). Subcutaneous administration of URB937 reduces acetic acid-induced writhing in mice with an ED50 value of 0.1 mg/kg. A single 1 mg/kg injection of URB937 sufficiently attenuates behavioral responses elicited in mouse models of neuropathic and inflammatory pain. As a peripherally-specific FAAH inhibitor, URB937 may offer an alternative approach to pain therapy devoid of unwanted central effects. References:
[1]. Clapper, J.R., Moreno-Sanz, G., Russo, R., et al. Anandamide suppresses pain initiation through a peripheral endocannabinoid mechanism Nat. Neurosci. 13(10), 1265-1270 (2010). |
