|N-(4-氯-3-吡啶基)-4-[(2,2-二氟-1,3-苯并二恶茂-5-基)甲基]-1-哌嗪甲酰胺|CsnPharm

CAS No.: 1346528-50-4

JNJ-42165279 Catalog No. CSN17723

Synonyms: JNJ-5279

JNJ-42165279 inhibits hFAAH and rFAAH with IC50 of 70 ± 8 nM and 313 ± 28 nM respectively.

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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^[2]. JNJ-42165279 inhibits hFAAH and rFAAH with IC₅₀ of 70 ± 8 nM and 313 ± 28 nM respectively^[3]. In rats, JNJ-42165279 reached a maximum plasma concentration of 4.2 μM after 1 h, falling to about 130 nM at 8 h and declining to below the LLQ by 16 h. Observed concentrations in the brain were somewhat rised relative to plasma at the Cmax (6.3 μM at 1 h), but those differences diminished by the 8 h time-point (167 nM)^[3]. In the multiple ascending dose (MAD) study, daily administration of JNJ-42165279 (10 mg, 25 mg, 75 mg) for 1 week increased the mean cerebrospinal fluid AEA and OEA concentrations by 45-77 fold and 6.6-7.4 fold, respectively, relative to predose values. Single doses of JNJ-42165279 in the range of 10-100 mg produced mean peak concentrations of AEA in plasma that were 5.5-10-fold higher than mean peak placebo values. ~10 mg of JNJ-42165279 resulted in saturation of brain FAAH occupancy^[4].
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
NCT01650597	Healthy Volunteers ... more >> Pharmacokinetics Collapse <<	Phase 1	Completed	-	Belgium ... more >> Merksem, Belgium Collapse <<
NCT01826786	Healthy	Phase 1	Completed	-	United States, California ... more >> La Jolla, California, United States Collapse <<
NCT02065739	Healthy	Phase 1	Completed	-	Belgium ... more >> Merksem, Belgium Collapse <<

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参考文献

[1] Keith JM, Jones WM, et al. Preclinical Characterization of the FAAH Inhibitor JNJ-42165279. ACS Med Chem Lett. 2015 Nov 2;6(12):1204-8.
[2] 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.
[3] Keith JM, Jones WM, Tichenor M, Liu J, Seierstad M, Palmer JA, Webb M, Karbarz M, Scott BP, Wilson SJ, Luo L, Wennerholm ML, Chang L, Rizzolio M, Rynberg R, Chaplan SR, Breitenbucher JG. Preclinical Characterization of the FAAH Inhibitor JNJ-42165279. ACS Med Chem Lett. 2015 Nov 2;6(12):1204-8. doi: 10.1021/acsmedchemlett.5b00353. PMID: 26713105; PMCID: PMC4677372.
[4] Postnov A, Schmidt ME, Pemberton DJ, de Hoon J, van Hecken A, van den Boer M, Zannikos P, van der Ark P, Palmer JA, Rassnick S, Celen S, Bormans G, van Laere K. Fatty Acid Amide Hydrolase Inhibition by JNJ-42165279: A Multiple-Ascending Dose and a Positron Emission Tomography Study in Healthy Volunteers. Clin Transl Sci. 2018 Jul;11(4):397-404. doi: 10.1111/cts.12548. Epub 2018 Mar 25. PMID: 29575526; PMCID: PMC6039207.

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
- 2.4343 mL
- 12.1713 mL
- 24.3426 mL
- 5 mM
- 0.4869 mL
- 2.4343 mL
- 4.8685 mL
- 10 mM
- 0.2434 mL
- 1.2171 mL
- 2.4343 mL

技术信息

CAS号

1346528-50-4

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H17ClF2N4O3

运输

蓝冰

分子量

410.80

别名

JNJ-5279

溶解度

DMSO	100.0 mg/mL (243.4 mM)

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01650597	Healthy Volunteers ... more >> Pharmacokinetics Collapse <<	Phase 1	Completed	-	Belgium ... more >> Merksem, Belgium Collapse <<
NCT01826786	Healthy	Phase 1	Completed	-	United States, California ... more >> La Jolla, California, United States Collapse <<
NCT02065739	Healthy	Phase 1	Completed	-	Belgium ... more >> Merksem, Belgium Collapse <<
NCT02169973	Healthy	Phase 1	Completed	-	Belgium ... more >> Leuven, Belgium Collapse <<
NCT02498392	Depressive Disorder ... more >> Anxiety Collapse <<	Phase 2	Active, not recruiting	February 18, 2019	-
NCT01964651	Healthy	Phase 1	Completed	-	Belgium ... more >> Merksem, Belgium Collapse <<
NCT03664232	Autism Spectrum Disorder	Phase 2	Recruiting	March 3, 2021	United States, Arizona ... more >> Southwest Autism Research and Resource Center Recruiting Phoenix, Arizona, United States, 85006 United States, New York Nathan Kline Institute Not yet recruiting Orangeburg, New York, United States, 10962 United States, Washington Seattle Children's Hospital Not yet recruiting Seattle, Washington, United States, 98105 Collapse <<
NCT02432703	Phobic Disorders	Phase 2	Completed	-	United States, California ... more >> La Jolla, California, United States United States, Connecticut Hartford, Connecticut, United States United States, Florida Orlando, Florida, United States United States, Illinois Chicago, Illinois, United States United States, Massachusetts Boston, Massachusetts, United States Natick, Massachusetts, United States United States, New York New York, New York, United States Rochester, New York, United States Staten Island, New York, United States United States, Pennsylvania Allentown, Pennsylvania, United States Reading, Pennsylvania, United States United States, Texas Dallas, Texas, United States United States, Utah Salt Lake City, Utah, United States Australia Adelaide, Australia Frankston, Australia Melbourne, Australia Perth, Australia Canada, Alberta Edmonton, Alberta, Canada Canada, Ontario Hamilton, Ontario, Canada Mississauga, Ontario, Canada Toronto, Ontario, Canada Collapse <<
NCT03564379	Healthy	Phase 1	Completed	-	United States, California ... more >> WCCT Global, LLC Cypress, California, United States, 90630 Collapse <<

JNJ-42165279 Catalog No. CSN17723

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