1. Metabolic Enzyme/Protease Neuronal Signaling
  2. FAAH MAGL
  3. AKU-005

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.

For research use only. We do not sell to patients.

AKU-005 Chemical Structure

AKU-005 Chemical Structure

CAS No. : 1515855-85-2

Size Stock
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Solid
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Description

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[1][2].

In Vivo

AKU-005 (0.5 mg/kg; i.p.) shows anti-hyperalgesic and anti-inflammatory effects in rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 150-175 g, Male Sprague Dawley rats (NTG 10 mg/kg; i.p.)[1]
Dosage: 0.5 mg/kg
Administration: I.p.; 3 h after NTG (nitroglycerin)
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.
Molecular Weight

347.41

Formula

C20H21N5O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C=NC=N1)N2CCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8784 mL 14.3922 mL 28.7844 mL
5 mM 0.5757 mL 2.8784 mL 5.7569 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 5 mg/mL (14.39 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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AKU-005
Cat. No.:
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