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 IC 50 values of 13.8 nM and 1.7 nM, respectively. AR9281 can be used for the research of inflammation, hypertension and type 2 diabetes
In Vitro
AR-9281 (APAU) has inhibitory activity for human sEH (HsEH) and murine sEH (MsEH) with IC 50 values of 13.8 nM and 1.7 nM, respectively. 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 Ca 2+ dysregulation and SERCA remodeling in hyperglycemic rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: T2DM rat modelDosage: 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 Ca 2+ effector system. Had less downregulation of sarco(endo)plasmic reticulum Ca 2+ ATPase (SERCA) and lowed expression of hypertrophic markers.
