|N-(哒嗪-3-基)-4-(3-((5(三氟甲基)吡啶-2-基)氧基)亚苄基)哌啶-1-甲酰胺|CsnPharm

CAS No.: 1020315-31-4

N-(Pyridazin-3-yl)-4-(3-((5-(trifluoromethyl)pyridin-2-yl)oxy)benzylidene)piperidine-1-carboxamide Catalog No. CSN16926

Synonyms: PF-4457845

PF-04457845 selectively inhibits FAAH with an IC50 of 7.2 nM. It has anti-inflammatory effects and is used as analgesic.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Fatty acid amide hydrolase (FAAH) is an integral membrane serine hydrolase that degrades the fatty acid amide family of signaling lipids, including the endocannabinoid anandamide^[3]. PF-04457845 selectively inhibits FAAH with an IC₅₀ of 7.2 nM^[3]. Men aged 18–55 years with cannabis dependence were treated with PF-04457845 (4 mg per day), and they showed reduced symptoms of cannabis withdrawal, lower self-reported cannabis use and lower urinary THC-COOH concentrations, compared with placebo group^[4]. Osteoarthritis patients administrated with 4 mg q.d. PF-04457845 showed decreased FAAH activity by >96% and significantly increased 4 endogenous substrates (fatty acid amides). PF-04457845 was well tolerated in osteoarthritis patients, and there was no evidence of cannabinoid-type adverse events, but failed to induce effective analgesia^[5].
作用机制PF-04457845 inhibits FAAH by a covalent, irreversible mechanism involving carbamylation of the active-site serine nucleophile of FAAH.
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
NCT01618656	Cannabis Dependence	Phase 2	Active, not recruiting	December 2018	United States, Connecticut ... more >> Yale University School of Medicine New Haven, Connecticut, United States, 06511 Collapse <<
NCT01665573	Fear Conditioning	Phase 2	Active, not recruiting	May 2019	United States, Connecticut ... more >> VA Connecticut Healthcare System West Haven, Connecticut, United States, 06516 Collapse <<
NCT00836082	Acute Pain Ch... more >>ronic Pain Collapse <<	Phase 1	Completed	-	Singapore ... more >> Pfizer Investigational Site Singapore, Singapore, 188770 Collapse <<

更多
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
- 2.1957 mL
- 10.9786 mL
- 21.9572 mL
- 5 mM
- 0.4391 mL
- 2.1957 mL
- 4.3914 mL
- 10 mM
- 0.2196 mL
- 1.0979 mL
- 2.1957 mL

技术信息

CAS号

1020315-31-4

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H20F3N5O2

运输

蓝冰

分子量

455.43

别名

PF-4457845

溶解度

DMSO	90.0 mg/mL (197.6 mM)
Water	Insoluble
Ethanol	4.0 mg/mL (8.8 mM)

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01618656	Cannabis Dependence	Phase 2	Active, not recruiting	December 2018	United States, Connecticut ... more >> Yale University School of Medicine New Haven, Connecticut, United States, 06511 Collapse <<
NCT01665573	Fear Conditioning	Phase 2	Active, not recruiting	May 2019	United States, Connecticut ... more >> VA Connecticut Healthcare System West Haven, Connecticut, United States, 06516 Collapse <<
NCT00836082	Acute Pain Ch... more >>ronic Pain Collapse <<	Phase 1	Completed	-	Singapore ... more >> Pfizer Investigational Site Singapore, Singapore, 188770 Collapse <<
NCT02134080	Tourette Syndrome	Phase 1	Terminated(no more funding ava... more >>ilable) Collapse <<	-	United States, Connecticut ... more >> Connecticut Mental Health Center New Haven, Connecticut, United States, 06519 Collapse <<
NCT00918164	Healthy Volunteers	Phase 1	Completed	-	Singapore ... more >> Pfizer Investigational Site Singapore, Singapore, 188770 Collapse <<
NCT03386487	Cannabis Use Disorder	Phase 2	Not yet recruiting	December 2022	-
NCT02216097	-	-	Terminated(The study stopped b... more >>ased on Pfizer portfolio prioritization and not due to safety and/or efficacy concern or change in benefitrisk assessment of PF-04457845.) Collapse <<	-	-
NCT01092845	Healthy Sleep	Phase 1	Completed	-	United States, New York ... more >> Pfizer Investigational Site New York, New York, United States, 10019 Collapse <<
NCT02216097	Post-Traumatic Stress Disorder	Phase 2	Terminated(The study stopped b... more >>ased on Pfizer portfolio prioritization and not due to safety and/or efficacy concern or change in benefitrisk assessment of PF-04457845.) Collapse <<	-	United States, New York ... more >> Clinical and Translational Science Institute (CTSI) New York, New York, United States, 10016 NYU CTSI Research Pharmacy (Drug Shipment Address) New York, New York, United States, 10016 NYU School of Medicine New York, New York, United States, 10016 Collapse <<
NCT01002625	Sleep Healthy... more >> Volunteers Collapse <<	Phase 1	Terminated(See termination rea... more >>son in detailed description.) Collapse <<	-	United States, New York ... more >> Pfizer Investigational Site New York, New York, United States, 10019 Collapse <<
NCT00981357	Osteoarthritis, Knee	Phase 2	Completed	-	United States, Florida ... more >> Arthritis & Rheumatic Care Center Miami, Florida, United States, 33143 Miami Research Associates Miami, Florida, United States, 33143 United States, Kansas Vince and Associates Clinical Research Overland Park, Kansas, United States, 66211 Vince and Associates Clinical Research Overland Park, Kansas, United States, 66212 United States, Texas CEDRA Clinical Research, LLC San Antonio, Texas, United States, 78217 Canada, Quebec Diex Research Inc. Sherbrooke, Quebec, Canada, J1H 1Z1 Sweden Centrum for klinisk provning Goteborg, Sweden, 405 30 Collapse <<

N-(Pyridazin-3-yl)-4-(3-((5-(trifluoromethyl)pyridin-2-yl)oxy)benzylidene)piperidine-1-carboxamide Catalog No. CSN16926

靶点选择性

请登录您的专属账户

确认信息