|3'-氨甲酰基-[1,1'-联苯]-3-环己基氨基甲酸酯|CsnPharm

CAS No.: 546141-08-6

URB-597 Catalog No. CSN12175

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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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^[3]. 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^[4]. 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^[5].
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.
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00916201	Schizophrenia	Phase 1	Not yet recruiting	December 2020	Germany ... more >> Dep. of Psychiatry and Psychotherapy, Central Institute of Mental Health Not yet recruiting Mannheim, BW, Germany, 68159 Contact: F. Markus Leweke, MD +49 621 1703 ext 2321 leweke@cimh.de Contact: Cathrin Rohleder, PhD +49 621 1703 ext 2333 rohleder@cimh.de Sub-Investigator: J. Malte Bumb, MD Sub-Investigator: Cathrin Rohleder, PhD Sub-Investigator: Till van der List, MD Sub-Investigator: Juliane K. Mueller, MD Sub-Investigator: Frank Enning, MD Collapse <<

参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9551 mL
- 14.7754 mL
- 29.5508 mL
- 5 mM
- 0.5910 mL
- 2.9551 mL
- 5.9102 mL
- 10 mM
- 0.2955 mL
- 1.4775 mL
- 2.9551 mL

技术信息

CAS号

546141-08-6

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H22N2O3

运输

蓝冰

分子量

338.40

别名

KDS-4103

溶解度

DMSO	68.0 mg/mL (200.9 mM)
Water	Insoluble
Ethanol	5.0 mg/mL (14.8 mM)

动物实验配方

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

1 mg/mL

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