| CAS NO: | 1346528-50-4 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 410.8 |
| Cas No. | 1346528-50-4 |
| Formula | C18H17ClF2N4O3 |
| Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
| Chemical Name | N-(4-chloro-3-pyridinyl)-4-[(2,2-difluoro-1,3-benzodioxol-5-yl)methyl]-1-piperazinecarboxamide |
| Canonical SMILES | ClC1=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。 |
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.
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