URB937

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

URB937 是 FAAH 的抑制剂，可增加 anandamide 水平（IC50：26.8 nM）。URB937 抑制 FAAH 活性并增加啮齿动物 CNS 外的 anandamide 水平。

URB937 is an inhibitor of FAAH and increases anandamide levels(IC50 : 26.8 nM).URB937 suppressed FAAH activity and increased anandamide levels outside the rodent CNS.?

URB937 is actively extruded from the CNS by the ATP-binding cassette (ABC) membrane transporter, Abcg2.

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.

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Metabolic Enzyme/Protease

FAAH

FAAH

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1357160-72-5

354.4

C20H22N2O4?

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (705.42 mM)

NC(=O)c1cccc(c1)-c1cc(OC(=O)NC2CCCCC2)ccc1O

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(-20℃)

With Ice Pack

≥ 2 years