Holiday Notification: Cayman Chemical will be closed Monday, May 28, 2012, in observance of the Memorial Day holiday.
More…
Please feel free to continue placing orders via our website or via fax at 734-971-3640. You may send an email to customer service at custserv@caymanchem.com , or to technical support at techserv@caymanchem.com which we will respond to the next business day. Cayman will resume regular business hours and shipping schedules on Tuesday, May 29, 2012. Thank you for your patience and understanding.
Epoxyeicosatrienoic acid (EpETrE) metabolites of arachidonic acid such as 11(12)-EpETrE and 14(15)-EpETrE have been identified as endothelium derived hyperpolarizing factors with vasodilator activity.1 Soluble epoxide hydrolase (sEH) catalyzes the conversion of EpETrEs to the corresponding dihydroxy eicosatrienoic acids (DiHETrEs) thereby diminishing their activity. AUDA is an inhibitor of sEH exhibiting IC50 values of 18 and 69 nM for the mouse and human enzymes, respectively.2 In angiotensin-infused rats, a dose of 25 mg/l AUDA administered in drinking water decreased mean arterial blood pressure from 161 ± 4 mmHg to 140 ± 5 mmHg. This hypotensive effect was accompanied by an increase in urinary epoxide-to-diol ratios.3 AUDA activates peroxisome proliferator-activated receptor α (PPARα) 3-fold at a concentration of 10 µM but exhibits no affect on PPARδ or PPARγ.4
1
Fleming, I. Cytochrome P450 epoxygenases as EDHF synthase(s). Pharmacol Res49525-533(2004).
2
Morisseau, C., Goodrow, M.H., Newman, J.W., et al. Structural refinement of inhibitors of urea-based soluble epoxide hydrolases. Biochem Pharmacol631599-1608(2002).
3
Imig, J.D., Zhao, X., Zaharis, C.Z., et al. An orally active epoxide hydrolase inhibitor lowers blood pressure and provides renal protection in salt-sensitive hypertension. Hypertension46(2)975-981(2005).
4
Fang, X., Hu, S., Watanabe, T., et al. Activation of peroxisome proliferator-activated receptor α by substituted urea-derived soluble epoxide hydrolase inhibitors. J Pharmacol Exp Ther314(1)260-270(2005).
Fleming, I. Cytochrome P450 epoxygenases as EDHF synthase(s). Pharmacol Res49525-533(2004).
Morisseau, C., Goodrow, M.H., Newman, J.W., et al. Structural refinement of inhibitors of urea-based soluble epoxide hydrolases. Biochem Pharmacol631599-1608(2002).
Fang, X., Hu, S., Watanabe, T., et al. Activation of peroxisome proliferator-activated receptor α by substituted urea-derived soluble epoxide hydrolase inhibitors. J Pharmacol Exp Ther314(1)260-270(2005).
Imig, J.D., Zhao, X., Zaharis, C.Z., et al. An orally active epoxide hydrolase inhibitor lowers blood pressure and provides renal protection in salt-sensitive hypertension. Hypertension46(2)975-981(2005).