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

AR-9281  (Synonyms: APAU)

Cat. No.: HY-111151 Purity: 99.43%
COA Handling Instructions

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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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 187 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 187 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 170 In-stock
Estimated Time of Arrival: December 31
10 mg USD 272 In-stock
Estimated Time of Arrival: December 31
25 mg USD 540 In-stock
Estimated Time of Arrival: December 31
50 mg USD 810 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1215 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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].

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

Appearance

Solid

Formula

C18H29N3O2
CAS No.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (78.26 mM; Need ultrasonic)

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
10 mM 0.3130 mL 1.5652 mL 3.1305 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.51 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.43%

COA (253 KB) LCMS (260 KB)

Handling Instructions (2659 KB)
References
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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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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

AR-9281913548-29-5APAUAR9281AR 9281Epoxide Hydrolaseoralsoluble epoxide hydrolase (s-EH)HsEHMsEHinflammationhypertensiontype 2 diabetesInhibitorinhibitorinhibit

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