| 货号 | 10009134-1mg |
| 描述 | EpETrE metabolizes 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 DiHETrEs thereby diminishing their activity.2 Inhibitors of sEH may therefore have clinical utility for treating hypertension and systemic inflammation.3,4 PHOME is a fluorogenic substrate for human sEH which displays good aqueous stability and solubility making it ideal for high throughput screening (HTS) programs. Hydrolysis of the substrate yields a highly fluorescent product that can be monitored at excitation and emission wavelengths of 330 and 465 nm, respectively. This fluorescent assay has a sensitivity that is 100 times greater than previously used spectrophotometric assays.5 NOTE: This substrate should only be used with the pure EH. If this substrate is used with crude enzyme preparations it is critical that all esterase activity is removed or inhibited, such as with organophosphate or a trifluoroketone inhibitor, and that glutathione is depleted and/or glutathione S-transferase is inhibited. |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Fleming, I. Cytochrome P450 epoxygenases as EDHF synthase(s). Pharmacological Research 49, 525-533 (2004). 2.Morisseau, C.,Goodrow, M.H.,Newman, J.W., et al. Structural refinement of inhibitors of urea-based soluble epoxide hydrolases. Biochemical Pharmacology 63, 1599-1608 (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. Hypertension 46(2), 975-981 (2005). 4.Schmelzer, K.R.,Kubala, L.,Newman, J.W., et al. Soluble epoxide hydrolase is a therapeutic target for acute inflammation. Proceedings of the National Academy of Sciences of the United States of America 102(28), 9772-9777 (2005). 5.Wolf, N.M.,Morisseau, C.,Jones, P.D., et al. Development of a high-throughput screen for soluble epoxide hydrolase inhibition. Analytical Biochemistry 355, 71-80 (2006). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 373.4 |
| 分子式 | C23H19NO4 |
| CAS号 | 1028430-42-3 |
| 稳定性 | ≥ 2 years |
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