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CAS No.: 681136-29-8

JNJ-1661010 Catalog No. CSN16558

Synonyms: Takeda-25

JNJ-1661010 is a selective inhibitor of FAAH with IC50 of 10 nM (rat) and 12 nM (human).

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400-920-2911

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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 amides (FAA) are a diverse group of lipid mediators including arachidonoyl ethanolamide (AEA), oleoyl ethanolamide (OEA), palmitoyl ethanolamide (PEA) and N-arachidonoyl glycine. FAAs are hydrolyzed by several different enzymes with different substrate preferences. The metabolizing enzymes that hydrolyze FAA include fatty acid amide hydrolase (FAAH), and N-acylethanolamine-hydrolyzing acid amidase^[3]. JNJ-1661010 is a selective inhibitor of FAAH with IC₅₀ of 10 nM (rat) and 12 nM (human)^[3]. The level of FAAH activity in the rat brain was decreased by at least 85% for up to 4 h after intraperitoneal dosing of 20 mg/kg JNJ-1661010, and only 25% of FAAH activity had returned by 24 h postdose, compared to control levels^[3]. Treatment of wild-type mice with 10 mg/kg JNJ-1661010, intraperitoneally four times a day, resulted in prominent exacerbation of bleomycin-induced fibrosis and dermal thickening, myofibroblast counts and hydroxyproline content are significantly increased compared with sham-treated, bleomycin-challenged mice^[4].
作用机制The acyl piperazinyl fragment of JNJ-1661010 forms a covalent bond with the FAAH.
参考文献

[1] Karbarz MJ, Luo L, et al. Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. Anesth Analg. 2009 Jan;108(1):316-29.
[2] Keith JM, Apodaca R, et al. Thiadiazolopiperazinyl ureas as inhibitors of fatty acid amide hydrolase. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4838-43.
[3] Karbarz MJ, Luo L, Chang L, Tham CS, Palmer JA, Wilson SJ, Wennerholm ML, Brown SM, Scott BP, Apodaca RL, Keith JM, Wu J, Breitenbucher JG, Chaplan SR, Webb M. Biochemical and biological properties of 4-(3-phenyl-[1,2,4] thiadiazol-5-yl)-piperazine-1-carboxylic acid phenylamide, a mechanism-based inhibitor of fatty acid amide hydrolase. Anesth Analg. 2009 Jan;108(1):316-29. doi: 10.1213/ane.0b013e31818c7cbd. PMID: 19095868.
[4] Palumbo-Zerr K, Horn A, Distler A, Zerr P, Dees C, Beyer C, Selvi E, Cravatt BF, Distler O, Schett G, Distler JH. Inactivation of fatty acid amide hydrolase exacerbates experimental fibrosis by enhanced endocannabinoid-mediated activation of CB1. Ann Rheum Dis. 2012 Dec;71(12):2051-4. doi: 10.1136/annrheumdis-2012-201823. Epub 2012 Aug 22. PMID: 22915616.

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
- 2.7363 mL
- 13.6817 mL
- 27.3634 mL
- 5 mM
- 0.5473 mL
- 2.7363 mL
- 5.4727 mL
- 10 mM
- 0.2736 mL
- 1.3682 mL
- 2.7363 mL

技术信息

CAS号

681136-29-8

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H19N5OS

运输

蓝冰

分子量

365.45

别名

Takeda-25

溶解度

DMSO	36.0 mg/mL (98.5 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

5% DMSO+95% Corn oil

5 mg/mL

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