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JNJ-42165279
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JNJ-42165279图片
CAS NO:1346528-50-4
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
JNJ-42165279 是一种 FAAH 抑制剂,对 hFAAH 和 rFAAH 的 IC50 分别为 70 ± 8 nM 和 313 ± 28 nM。
Cas No.1346528-50-4
别名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
化学名N-(4-chloro-3-pyridinyl)-4-[(2,2-difluoro-1,3-benzodioxol-5-yl)methyl]-1-piperazinecarboxamide
Canonical SMILESClC1=CC=NC=C1NC(N2CCN(CC3=CC=C(OC(F)(F)O4)C4=C3)CC2)=O
分子式C18H17ClF2N4O3
分子量410.8
溶解度≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

JNJ-42165279 is a potent and irreversible inhibitor of fatty acid amide hydrolase (FAAH) [1]. JNJ-42165279 covalently inactivates the FAAH enzyme [1]. JNJ-42165279 is highly selective with regard to other enzymes, ion channels, transporters, and receptors. The fatty acid amide hydrolase interrupt the actions through degrading various endogenous lipid signaling molecules. FAAH degrades several fatty acid ethanolamides rapidly, such as FAAH’s primary substrate, AEA (N-arachidonyl ethanolamide or anandamide), PEA (N-palmitoyl ethanolamide), and OEA (N-oleoyl ethanolamide) [1].

In vitro: JNJ-42165279 inhibited recombinant human and rat FAAH with the IC50s of 70 ± 8 nM and 313 ± 28 nM, respectively [1]. JNJ-42165279 (10 μM) exhibited high selectivity against a panel of receptors, enzymes, transporters, and ion-channels. JNJ-42165279 (10 μM) showed no inhibitory effects against CYPS (1A2, 2C8, 2C9, 2C19, 2D6, 3A4) or hERG [1].

In vivo: In the rat spinal nerve ligation (SNL or Chung) model of neuropathic pain, JNJ-42165279 exhibited analgesic properties. JNJ-42165279 dose-dependently reversed the robust tactile allodynia. The ED90 was 22 mg/kg, which corresponds to a plasma concentration of 2.5 μM at 30 min [1].

References:
[1] Keith J M, Jones W M, Tichenor M, et al.  Preclinical characterization of the FAAH inhibitor JNJ-42165279[J]. ACS medicinal chemistry letters, 2015, 6(12): 1204-1208.