AKU-005
Based on 1 Customer Validation
AKU-005 is a FAAH and MAGL dual inhibitor with IC50 values of 63, 389 nM for rat and human FAAH, respectively. AKU-005 has the potential for the research of trigeminal hyperalgesia.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.48%
- CAS. Nr.: 1515855-85-2
- Formel: C20H21N5O
- Molecular Weight:347.41
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
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| COS-7 | IC50 |
452 nM
Compound: AKU-005
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Inhibition of human recombinant FAAH expressed in COS7 cells using anandamide as substrate
Inhibition of human recombinant FAAH expressed in COS7 cells using anandamide as substrate
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[PMID: 25282655] |
| HEK293 | IC50 |
1.3 nM
Compound: AKU-005
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Inhibition of human recombinant MAGL expressed in HEK293 cells using 2-AG as substrate
Inhibition of human recombinant MAGL expressed in HEK293 cells using 2-AG as substrate
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[PMID: 25282655] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:150-175 g, Male Sprague Dawley rats (NTG 10 mg/kg; i.p.)[1]
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Dosage:0.5 mg/kg
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Administration:I.p.; 3 h after NTG (nitroglycerin)
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Result:Significantly prevented the NTG-induced increase in face-rubbing behavior, decreased the CGRP mRNA levels in the meninges, medulla, CSC, and TG ipsilateral, prevented an NTG-induced increase in IL-6 and TNF-alpha mRNA levels in all areas, except for TNF-alpha in the medulla.
Chemical Information
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CAS. Nr. 1515855-85-2
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Appearance Solid
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Molecular Weight 347.41
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Formel C20H21N5O
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Color White to off-white
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SMILES
O=C(N1C=NC=N1)N2CCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (287.84 mM; ultrasonic and warming and heat to 60°C; 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (14.39 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Reinheit & Dokumentation
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Data Sheet (275 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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Handling Instructions (2659 KB)
Verweise
[1]. Greco R, et al. Effects of the Dual FAAH/MAGL Inhibitor AKU-005 on Trigeminal Hyperalgesia in Male Rats. Cells. 2024 May 13;13(10):830. [Content Brief]
[2]. Aaltonen N, et al. Piperazine and piperidine triazole ureas as ultrapotent and highly selective inhibitors of monoacylglycerol lipase. Chem Biol. 2013 Mar 21;20(3):379-90. [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 | 2.8784 mL | 14.3922 mL | 28.7844 mL | 71.9611 mL |
| 5 mM | 0.5757 mL | 2.8784 mL | 5.7569 mL | 14.3922 mL | |
| 10 mM | 0.2878 mL | 1.4392 mL | 2.8784 mL | 7.1961 mL | |
| 15 mM | 0.1919 mL | 0.9595 mL | 1.9190 mL | 4.7974 mL | |
| 20 mM | 0.1439 mL | 0.7196 mL | 1.4392 mL | 3.5981 mL | |
| 25 mM | 0.1151 mL | 0.5757 mL | 1.1514 mL | 2.8784 mL | |
| 30 mM | 0.0959 mL | 0.4797 mL | 0.9595 mL | 2.3987 mL | |
| 40 mM | 0.0720 mL | 0.3598 mL | 0.7196 mL | 1.7990 mL | |
| 50 mM | 0.0576 mL | 0.2878 mL | 0.5757 mL | 1.4392 mL | |
| 60 mM | 0.0480 mL | 0.2399 mL | 0.4797 mL | 1.1994 mL | |
| 80 mM | 0.0360 mL | 0.1799 mL | 0.3598 mL | 0.8995 mL | |
| 100 mM | 0.0288 mL | 0.1439 mL | 0.2878 mL | 0.7196 mL |
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