JNJ-42165279
Based on 1 Customer Validation
JNJ-42165279 is an orally active FAAH inhibitor, with IC50 values of 70 nM for hFAAH and 313 nM for rFAAH. JNJ-42165279 can be used in research related to the field of neuropathic pain.
For research use only. We do not sell to patients.
- Purity: 99.95%
- CAS No.: 1346528-50-4
- Formula: C18H17ClF2N4O3
- Molecular Weight:410.80
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Spinal nerve ligation (SNL)-induced chronic tactile allodynia in Sprague-Dawley rats[2]
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Dosage:60 mg/kg
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Administration:Oral gavage (p.o.), single dose
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Result:Reversed tactile allodynia, with a maximum pain relief of 59% observed at 30 minutes, maintained for at least 2 hours.
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Animal Model:Embryo-fetal development model in Sprague-Dawley rats[2]
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Dosage:10, 30, 100 mg/kg
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Administration:Oral gavage (p.o.), once daily for 11 days
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Result:induced fetal lens fiber hypertrophy and degeneration, with nuclear cataracts observed in some rats (100 mg/kg).
Chemical Information
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CAS No. 1346528-50-4
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Appearance Solid
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Molecular Weight 410.80
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Formula C18H17ClF2N4O3
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Color White to off-white
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SMILES
O=C(N1CCN(CC2=CC=C(OC(F)(F)O3)C3=C2)CC1)NC4=C(Cl)C=CN=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : ≥ 100 mg/mL (243.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (7.30 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (7.30 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Keith JM, et al. Preclinical Characterization of the FAAH Inhibitor JNJ-42165279. ACS Med Chem Lett. 2015 Nov 2;6(12):1204-8. [Content Brief]
[2]. van Heerden M, et al. Exacerbation of Background Nuclear Cataracts in Sprague-Dawley Rats in Embryo-Fetal Development Studies With JNJ-42165279, a Fatty Acid Amide Hydrolase Inhibitor. Toxicol Pathol. 2021 Aug;49(6):1193-1205. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4343 mL | 12.1714 mL | 24.3427 mL | 60.8569 mL |
| 5 mM | 0.4869 mL | 2.4343 mL | 4.8685 mL | 12.1714 mL | |
| 10 mM | 0.2434 mL | 1.2171 mL | 2.4343 mL | 6.0857 mL | |
| 15 mM | 0.1623 mL | 0.8114 mL | 1.6228 mL | 4.0571 mL | |
| 20 mM | 0.1217 mL | 0.6086 mL | 1.2171 mL | 3.0428 mL | |
| 25 mM | 0.0974 mL | 0.4869 mL | 0.9737 mL | 2.4343 mL | |
| 30 mM | 0.0811 mL | 0.4057 mL | 0.8114 mL | 2.0286 mL | |
| 40 mM | 0.0609 mL | 0.3043 mL | 0.6086 mL | 1.5214 mL | |
| 50 mM | 0.0487 mL | 0.2434 mL | 0.4869 mL | 1.2171 mL | |
| 60 mM | 0.0406 mL | 0.2029 mL | 0.4057 mL | 1.0143 mL | |
| 80 mM | 0.0304 mL | 0.1521 mL | 0.3043 mL | 0.7607 mL | |
| 100 mM | 0.0243 mL | 0.1217 mL | 0.2434 mL | 0.6086 mL |