URB937
目录号: PL02302 纯度: ≥99%
CAS No. :1357160-72-5
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中文名称
URB937
中文别名
4-氨基-1-甲基-3-正丙基-1H-吡唑-5-甲酰胺
英文名称
URB937
英文别名
URB 937;3'-Carbamoyl-6-hydroxybiphenyl-3-yl cyclohexylcarbamate;Cyclohexylcarbamic acid 3′–carbamoyl–6–hydroxybiphenyl–3–yl ester;URB937;[3-(3-carbamoylphenyl)-4-hydroxyphenyl] N-cyclohexylcarbamate;3'-Carbamoyl-6-hydroxy-[1,1'-biphenyl]-3-yl cyclohexylcarbamate;GTPL11817;cyclohexylcarbamic acid 3'-carbamoyl-6-hydroxybiphenyl-3-yl ester;BDBM50437227;A936336;3'-(Aminocarbonyl)-6-hydroxy[1,1'-biphenyl]-3-yl N-cyclohexylcarbamate
Cas No.
1357160-72-5
分子式
C20H22N2O4
分子量
354.40
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
URB937 是口服有效的、外周限制的 FAAH 抑制剂,IC50 值为 26.8 nM,可增加 anandamide 水平。URB937 不能影响脑内 FAAH 水平 (无法透过血脑屏障)。
生物活性
URB937 is an orally active and peripherally restricted FAAH inhibitor (IC 50 =26.8 nM) and increases anandamide levels. URB937 fails to affect FAAH activity in the brain (not penetrate the blood-brain barrier).
性状
Solid
IC50 & Target[1][2]
IC50: 26.8 nM (FAAH).
体外研究(In Vitro)
URB937 is actively extruded from the CNS by the ATP-binding cassette (ABC) membrane transporter, Abcg2. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
URB937 (1 mg/kg, i.p.) administrated in mice increases anandamide levels in peripheral tissues, but not forebrain or hypothalamus.
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 (C max ) of 159.47 ng/ml, which was achieved one hour after administration. URB937 exhibits T 1/2 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 tissu
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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.
溶解度数据
In Vitro: DMSO : 250 mg/mL (705.42 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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