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AR-9281

Cat. No. M30879
AR-9281 Structure
Synonym:

APAU

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Biological Activity

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.

Chemical Information
Molecular Weight 319.44
Formula C18H29N3O2
CAS Number 913548-29-5
Form Solid
Solubility (25°C) DMSO 25 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Fangyu Du, et al. Eur J Med Chem. Discovery of memantyl urea derivatives as potent soluble epoxide hydrolase inhibitors against lipopolysaccharide-induced sepsis

[2] Yong Du, et al. EJNMMI Res. PET imaging of soluble epoxide hydrolase in non-human primate brain with [18F]FNDP

[3] Sanda Despa, et al. J Am Heart Assoc. Cardioprotection by controlling hyperamylinemia in a "humanized" diabetic rat model

[4] Kathleen Guglielmino, et al. Am J Physiol Heart Circ Physiol. Pharmacological inhibition of soluble epoxide hydrolase provides cardioprotection in hyperglycemic rats

[5] Sampath-Kumar Anandan, et al. Bioorg Med Chem Lett. 1-(1-acetyl-piperidin-4-yl)-3-adamantan-1-yl-urea (AR9281) as a potent, selective, and orally available soluble epoxide hydrolase inhibitor with efficacy in rodent models of hypertension and dysglycemia

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Keywords: AR-9281, APAU supplier, Epoxide Hydrolase, inhibitors, activators

 
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