产品
编 号：F136610
分子式：C20H22N2O4
分子量：354.4
分子式：C20H22N2O4
分子量：354.4
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1357160-72-5
产品详情
生物活性：
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).
体内研究：
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 (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.
体外研究：
URB937 is actively extruded from the CNS by the ATP-binding cassette (ABC) membrane transporter, Abcg2.
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).
体内研究：
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 (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.
体外研究：
URB937 is actively extruded from the CNS by the ATP-binding cassette (ABC) membrane transporter, Abcg2.
产品资料
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