ARN 077
Based on 1 Customer Validation
ARN 077 is a potent and selective N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 7 nM for human NAAA. ARN 077 significantly increases palmitoyl ethanolamine (PEA) levels within the CNS and has broad antinociceptive activity in mice and rats.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.82%
- No. CAS: 1373625-34-3
- Fòrmula: C16H21NO4
- Peso molecular:291.34
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Covalent Screening Library
HY-L036
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Heterocyclic Compound Library
HY-L138
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Metabolic Enzyme Compound Library
HY-L146
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Covalent Screening Library Plus
HY-L036P
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Immunology/Inflammation Compound Library
HY-L007
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Metabolism/Protease Compound Library
HY-L012
Actividad biológica
IC50: 7 nM (human NAAA)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.007 μM
Compound: 4, ARN077
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Inhibition of C-terminal His-6-tagged recombinant human spleen NAAA enzyme expressed in HEK293 cells
Inhibition of C-terminal His-6-tagged recombinant human spleen NAAA enzyme expressed in HEK293 cells
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[PMID: 23991897] |
| HEK293 | IC50 |
0.13 μM
Compound: 27, URB913/ARN077
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Inhibition of rat recombinant NAAA expressed in HEK293 cells using heptadecenoylethanolamide as substrate after 30 mins by LC/MS analysis
Inhibition of rat recombinant NAAA expressed in HEK293 cells using heptadecenoylethanolamide as substrate after 30 mins by LC/MS analysis
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[PMID: 22515328] |
| HEK293 | IC50 |
7.3 nM
Compound: ARN077
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Inhibition of human recombinant His6-tagged NAAA expressed in HEK293 cells using 10-cis-heptadecenoylethanolamide as substrate after 30 mins by UPLC/MS analysis
Inhibition of human recombinant His6-tagged NAAA expressed in HEK293 cells using 10-cis-heptadecenoylethanolamide as substrate after 30 mins by UPLC/MS analysis
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[PMID: 24900487] |
Chemical Information
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No. CAS 1373625-34-3
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Appearance Solid
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Peso molecular 291.34
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Fòrmula C16H21NO4
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Color White to off-white
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SMILES
O=C(OCCCCCC1=CC=CC=C1)N[C@@H]2[C@H](C)OC2=O
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Synonyms
URB913
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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 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 250 mg/mL (858.10 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.08 mg/mL (7.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (7.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Pureza y Documentación
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Ficha de datos (270 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Sasso O, et al. Antinociceptive effects of the N-acylethanolamine acid amidase inhibitor ARN077 in rodent pain models. Pain. 2013 Mar;154(3):350-60. [Content Brief]
[2]. Davis MP, et al. Cannabinoids in pain management: CB1, CB2 and non-classic receptor ligands. Expert Opin Investig Drugs. 2014 Aug;23(8):1123-40. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.4324 mL | 17.1621 mL | 34.3242 mL | 85.8104 mL |
| 5 mM | 0.6865 mL | 3.4324 mL | 6.8648 mL | 17.1621 mL | |
| 10 mM | 0.3432 mL | 1.7162 mL | 3.4324 mL | 8.5810 mL | |
| 15 mM | 0.2288 mL | 1.1441 mL | 2.2883 mL | 5.7207 mL | |
| 20 mM | 0.1716 mL | 0.8581 mL | 1.7162 mL | 4.2905 mL | |
| 25 mM | 0.1373 mL | 0.6865 mL | 1.3730 mL | 3.4324 mL | |
| 30 mM | 0.1144 mL | 0.5721 mL | 1.1441 mL | 2.8603 mL | |
| 40 mM | 0.0858 mL | 0.4291 mL | 0.8581 mL | 2.1453 mL | |
| 50 mM | 0.0686 mL | 0.3432 mL | 0.6865 mL | 1.7162 mL | |
| 60 mM | 0.0572 mL | 0.2860 mL | 0.5721 mL | 1.4302 mL | |
| 80 mM | 0.0429 mL | 0.2145 mL | 0.4291 mL | 1.0726 mL | |
| 100 mM | 0.0343 mL | 0.1716 mL | 0.3432 mL | 0.8581 mL |
ARN 077 Related Classifications
HY-120813 Related Classifications
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