1. Metabolic Enzyme/Protease
  2. Epoxide Hydrolase
  3. AR-9281

AR9281 (APAU) is a potent, selective and orally active soluble epoxide hydrolase (s-EH) inhibitor. AR-9281 can inhibits human sEH (HsEH) and murine sEH (MsEH) with IC50 values of 13.8 nM and 1.7 nM, respectively. AR9281 can be used for the research of inflammation, hypertension and type 2 diabetes.

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

AR-9281 Chemical Structure

AR-9281 Chemical Structure

CAS No. : 913548-29-5

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 187 In-stock
Solution
10 mM * 1 mL in DMSO USD 187 In-stock
Solid
5 mg USD 170 In-stock
10 mg USD 272 In-stock
25 mg USD 540 In-stock
50 mg USD 810 In-stock
100 mg USD 1215 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AR9281 (APAU) is a potent, selective and orally active soluble epoxide hydrolase (s-EH) inhibitor. AR-9281 can inhibits human sEH (HsEH) and murine sEH (MsEH) with IC50 values of 13.8 nM and 1.7 nM, respectively. AR9281 can be used for the research of inflammation, hypertension and type 2 diabetes[1][2].

IC50 & Target

IC50: 13.8 nM (HsEH); 1.7 nM (MsEH)[1]

In Vitro

AR-9281 (APAU) has inhibitory activity for human sEH (HsEH) and murine sEH (MsEH) with IC50 values of 13.8 nM and 1.7 nM, respectively[1].

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

In Vivo

AR-9281 (APAU) (oral, 150-200 mg/dL, for 6 weeks) enhances the therapeutic effects of EETs, slows progression of hyperglycemia, protects the myocyte structure, and reduces Ca2+ dysregulation and SERCA remodeling in hyperglycemic rats[2].

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

Animal Model: T2DM rat model[2]
Dosage: 150-200 mg/dL
Administration: oral(drinking), for 6 weeks
Result: Attenuated the progressive increase of blood glucose concentration and preserved mitochondrial structure and myofibril morphology in cardiac myocytes.
Protected the intracellular Ca2+ effector system.
Had less downregulation of sarco(endo)plasmic reticulum Ca2+ ATPase (SERCA) and lowed expression of hypertrophic markers.
Molecular Weight

319.44

Formula

C18H29N3O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1(C2)CC3CC2CC(C3)C1)NC4CCN(C(C)=O)CC4

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 25 mg/mL (78.26 mM; Need ultrasonic; 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 3.1305 mL 15.6524 mL 31.3048 mL
5 mM 0.6261 mL 3.1305 mL 6.2610 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (6.51 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (6.51 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.
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

Purity: 99.43%

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, 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 3.1305 mL 15.6524 mL 31.3048 mL 78.2620 mL
5 mM 0.6261 mL 3.1305 mL 6.2610 mL 15.6524 mL
10 mM 0.3130 mL 1.5652 mL 3.1305 mL 7.8262 mL
15 mM 0.2087 mL 1.0435 mL 2.0870 mL 5.2175 mL
20 mM 0.1565 mL 0.7826 mL 1.5652 mL 3.9131 mL
25 mM 0.1252 mL 0.6261 mL 1.2522 mL 3.1305 mL
30 mM 0.1043 mL 0.5217 mL 1.0435 mL 2.6087 mL
40 mM 0.0783 mL 0.3913 mL 0.7826 mL 1.9565 mL
50 mM 0.0626 mL 0.3130 mL 0.6261 mL 1.5652 mL
60 mM 0.0522 mL 0.2609 mL 0.5217 mL 1.3044 mL
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AR-9281 Related Classifications

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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Product Name:
AR-9281
Cat. No.:
HY-111151
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