| 货号 | 75780-1mg |
| 描述 | 20-HETE is a major biologically active cytochrome P450 (CYP450) metabolite of arachidonic acid in the kidney and liver. It regulates renal vascular and tubular functions as well as vascular tone in the cerebral circulation.1,2,3,4,5 HET0016 is an inhibitor of 20-HETE formation in human renal microsomes with an IC50 of 8.9 nM, selectively inhibiting CYP4A and 4F isoforms.6,7 HET0016 inhibits CYP2C9, CYP2D6, and CYP3A4, enzymes important in drug metabolism, significantly less effectively with IC50s in the µM range. The IC50 values for inhibition of cyclooxygenase and epoxyeicosatrienoic acids (EETs) formation are 2.3 and 2.8 µM, respectively.6 |
| 别名 | N-hydroxy-N-(4-n-butyl-2-methylphenyl)Formamidine; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Omata, K.,Abraham, N.G. and Schwartzman, M.L. Renal cytochrome P-450-arachidonic acid metabolism: Localization and hormonal regulation in SHR. American Journal of Physiology.Renal, Fluid and Electrolyte Physiology 262, F591-F599 (1992). 2.Zou, A.P.,Imig, J.D.,Kaldunski, M., et al. Inhibition of renal vascular 20-HETE production impairs autoregulation of renal blood flow. American Journal of Physiology.Renal, Fluid and Electrolyte Physiology 35, F275-F282 (1994). 3.Lin, F.,Rios, A.,Falck, J.R., et al. 20-Hydroxyeicosatetraenoic acid is formed in response to EGF and is a mitogen in rat proximal tubule. American Journal of Physiology.Renal, Fluid and Electrolyte Physiology 38, F806-F816 (1995). 4.Imig, J.D.,Zou, A.P.,de Montellano, P.R.O., et al. Cytochrome P-450 inhibitors alter afferent arteriolar responses to elevations in pressure. American Journal of Physiology.Heart and Circulatory Physiology 35, H1879-H1885 (1994). 5.Gebremedhin, D.,Lange, A.R.,Lowry, T.F., et al. Production of 20-HETE and its role in autoregulation of cerebral blood flow. Circulation Research 87, 60-65 (2000). 6.Miyata, N.,Taniguchi, K.,Seki, T., et al. HET0016, a potent and selective inhibitor of 20-HETE synthesizing enzyme. British Journal of Pharmacology 133, 325-329 (2001). 7.Kehl, F.,Cambj-Sapunar, L.,Maier, K., et al. 20-HETE contributes to the acute fall in cerebral blood flow after subarachnoid hemorrhage in the rat. American Journal of Physiology.Heart and Circulatory Physiology 282, H1556-H1565 (2002). | |
| 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 | 206.3 |
| 分子式 | C12H18N2O |
| CAS号 | 339068-25-6 |
| 稳定性 | ≥ 2 years |
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