| 产品描述： | URB937 is an orally active and peripherally restricted FAAH inhibitor (IC50=26.8 nM) and increases anandamide levels. URB937 fails to affect FAAH activity in the brain (not penetrate the blood-brain barrier) |
| 靶点： |
IC50: 26.8 nM (FAAH) |
| 体外研究： |
URB937 is actively extruded from the CNS by the ATP-binding cassette (ABC) membrane transporter, Abcg2 |
| 体内研究： |
URB937 (1 mg/kg, i.p.) administrated in mice increases anandamide levels in peripheral tissues, but not forebrain or hypothalamus[1].URB937 (1 mg/kg, s.c.) suppresses pain responses elicited by i.p. injections of acetic acid. URB937 in male rats (an oral dose 3 mg/kg, F = 36%) is absorbed at a moderate rate and displays a peak plasma concentration (Cmax) of 159.47 ng/ml, which was achieved one hour after administration. URB937 exhibits T1/2 of 60 min by an oral dose of 3 mg/kg. URB937 produces a high degree of antinociception in female mice and rats in models of visceral and inflammatory pain. Moreover, the compound displayed a restricted access to placental and fetal tissues in pregnant mice and rats. URB937 (1 mg/kg, every 2 days for 30 days) attenuates radiation-induced lung injury and increased endocannabinoid concentration in lung tissue. Animal Model: Swiss Webster mice. Dosage: 1 mg/kg. Administration: S.C. Result: Suppressesd pain responses elicited by i.p. injections of acetic acid. Animal Model: Adult Sprague Dawley male and female rats (250-300 g). Dosage: 0.3, 1, 3, 10 mg/kg (Pharmacokinetic Analysis). Administration: Single oral dose. Result: Inhibited liver FAAH activity with a median effective dose (ED50) of 0.9 mg/kg.Inhibits FAAH in peripheral tissues and identify a possible biomarker for target engagement. |
| 参考文献： |
1. Jason R Clapper, et al. Anandamide suppresses pain initiation through a peripheral endocannabinoid mechanism. Nat Neurosci. 2010 Oct;13(10):1265-70. 2. Valentina Vozella, et al. Pharmacokinetics, pharmacodynamics and safety studies on URB937, a peripherally restricted fatty acid amide hydrolase (FAAH) inhibitor, in rats. J Pharm Pharmacol. 2019 Dec;71(12):1762-1773. 3. G Moreno-Sanz, et al. Pharmacological characterization of the peripheral FAAH inhibitor URB937 in female rodents: interaction with the Abcg2 transporter in the blood-placenta barrier. Br J Pharmacol. 2012 Dec;167(8):1620-8. 4. Rui Li, et al. The Fatty Acid Amide Hydrolase Inhibitor URB937 Ameliorates Radiation-Induced Lung Injury in a Mouse Model. Inflammation. 2017 Aug;40(4):1254-1263. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.822 ml |
14.108 ml |
28.217 ml |
| 5 mM |
0.564 ml |
2.822 ml |
5.643 ml |
| 10 mM |
0.282 ml |
1.411 ml |
2.822 ml |
| 50 mM |
0.056 ml |
0.282 ml |
0.564 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京