CAS:546141-08-6URB-597

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Synonyms: KDS-4103

URB-597 is fatty acid amide hydrolase (FAAH, IC50 = 4.6 nM) inhibitor without effect on other cannabinoid-related targets.

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18817579266

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18817579266

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实验数据

技术信息

CAS号

546141-08-6

储存条件

分子式

C20H22N2O3

运输

蓝冰

分子量

338.40

别名

KDS-4103

溶解度

动物实验配方

5%DMSO+40%PEG300+5%Tween80+water

1 mg/mL

生物活性

描述Fatty acid amide hydrolase (FAAH), an integral membrane bound enzyme, are intracellular enzymes responsible for the hydrolysis of endogenous fatty acid ethanolamides (FAEs). URB-597 (KDS-4103) is FAAH inhibitor with IC50 of 4.6 nM without effect on other cannabinoid-related targets. Treatment with 10 μM URB-597 in microglial cells reduced the release of PGE2 to approximately 50% of control, and inhibited LPS stimulated TNF and NO release and iNOS expression. In vivo, URB-597 (0.3 mg/kg/day, intraperitoneal (i.p.) injection) treatment in chronic cerebral hypoperfusion model inhibited impaired autophagy degradation and the disruption of beclin-1/Bcl-2 complex and subsequently cut off BNIP3-cyt C- and parkin-required mitophagy, finally preventing the abnormal excessive autophagy and mitophagy.
作用机制Carbamoyl group in URB-597 may form two distinct hydrogen bonds with FAAH: one as an acceptor, with the hydroxyl group of Thr488, and the other as a donor, with the main chain carbonyl group of Leu192.