JNJ-42165279 |
| カタログ番号GC10133 |
JNJ-42165279 は、hFAAH および rFAAH の IC50 がそれぞれ 70 ± 8 nM および 313 ± 28 nM の FAAH 阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1346528-50-4
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 1346528-50-4 | SDF | |
| 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 | ||
| Formula | C18H17ClF2N4O3 | M.Wt | 410.8 |
| 溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4343 mL | 12.1714 mL | 24.3427 mL |
| 5 mM | 0.4869 mL | 2.4343 mL | 4.8685 mL |
| 10 mM | 0.2434 mL | 1.2171 mL | 2.4343 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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