JZL195
Based on 4 publication(s) in Google Scholar
JZL195 is a selective and efficacious dual fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) inhibitor with IC50s of 2 and 4 nM, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.75%
- No. CAS: 1210004-12-8
- Fòrmula: C24H23N3O5
- Peso molecular:433.46
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) JZL195
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Actividad biológica
IC50: 2 nM (FAAH), 4 nM (MAGL)[1]
JZL195 produces near-complete blockade of FP-Rh labeling of both mouse brain FAAH and MAGL at concentrations as low as 100 nM (IC50 values of 13 and 19 nM, respectively)[1].
JZL195 inhibits rat and human FAAH and MAGL enzymes with IC50 values in the range of ≈10-100 nM based on competitive ABPP assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice[1]
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Dosage:20 mg/kg
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Administration:Intraperitoneal injection
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Result:Produced a much greater antinociceptive response in the tail immersion assay compared with inhibitors of either FAAH or MAGL alone.
Chemical Information
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No. CAS 1210004-12-8
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Appearance Solid
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Peso molecular 433.46
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Fòrmula C24H23N3O5
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Color White to off-white
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SMILES
O=C(OC1=CC=C([N+]([O-])=O)C=C1)N(CC2)CCN2CC3=CC(OC4=CC=CC=C4)=CC=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Death Differ
FAAH served a key membrane-anchoring and stabilizing role for NLRP3 protein independently of the endocannabinoid system. [Abstract]2023 Jan;30(1):168-183. PMID: 36104448 -
Int J Mol Sci
Function of Presynaptic Inhibitory Cannabinoid CB1 Receptors in Spontaneously Hypertensive Rats and Its Modification by Enhanced Endocannabinoid Tone. [Abstract]2024 Jan 10;25(2):858. PMID: 38255931 -
Int J Mol Sci
Weak Hypotensive Effect of Chronic Administration of the Dual FAAH/MAGL Inhibitor JZL195 in Spontaneously Hypertensive Rats as Revealed by Area under the Curve Analysis. [Abstract]2023 Jun 30;24(13):10942. PMID: 37446125 -
iScience
Inhibition of cannabinoid degradation enhances hippocampal contextual fear memory and exhibits anxiolytic effects. [Abstract]2024 Jan 15;27(2):108919. PMID: 38318362
Solvente y solubilidad
DMSO : 50 mg/mL (115.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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: ≥ 2.5 mg/mL (5.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (398 KB)
- English - EN (398 KB)
- Français - FR (398 KB)
- Deutsch - DE (398 KB)
- Norwegian - NO (398 KB)
- Español - ES (398 KB)
- Swedish - SV (398 KB)
- Italian - IT (398 KB)
- Korean - KR (398 KB)
- Portuguese - PT (398 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Long JZ, et al. Dual blockade of FAAH and MAGL identifies behavioral processes regulated by endocannabinoid crosstalk in vivo. Proc Natl Acad Sci U S A. 2009 Dec 1;106(48):20270-5. [Content Brief]
[2]. Anderson WB, et al. Actions of the dual FAAH/MAGL inhibitor JZL195 in a murine inflammatory pain model. Neuropharmacology. 2014 Jun;81:224-30. [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 | 2.3070 mL | 11.5351 mL | 23.0702 mL | 57.6754 mL |
| 5 mM | 0.4614 mL | 2.3070 mL | 4.6140 mL | 11.5351 mL | |
| 10 mM | 0.2307 mL | 1.1535 mL | 2.3070 mL | 5.7675 mL | |
| 15 mM | 0.1538 mL | 0.7690 mL | 1.5380 mL | 3.8450 mL | |
| 20 mM | 0.1154 mL | 0.5768 mL | 1.1535 mL | 2.8838 mL | |
| 25 mM | 0.0923 mL | 0.4614 mL | 0.9228 mL | 2.3070 mL | |
| 30 mM | 0.0769 mL | 0.3845 mL | 0.7690 mL | 1.9225 mL | |
| 40 mM | 0.0577 mL | 0.2884 mL | 0.5768 mL | 1.4419 mL | |
| 50 mM | 0.0461 mL | 0.2307 mL | 0.4614 mL | 1.1535 mL | |
| 60 mM | 0.0385 mL | 0.1923 mL | 0.3845 mL | 0.9613 mL | |
| 80 mM | 0.0288 mL | 0.1442 mL | 0.2884 mL | 0.7209 mL | |
| 100 mM | 0.0231 mL | 0.1154 mL | 0.2307 mL | 0.5768 mL |
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