您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > JNJ-42165279
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
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

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt410.8
Cas No.1346528-50-4
FormulaC18H17ClF2N4O3
Solubility≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide
Chemical NameN-(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
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

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.