• 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);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： -20℃

• 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。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *