货号 | 19640-1mg |
描述 | Aliskiren is a nonpeptide renin inhibitor (IC50 = 0.6 nM) that selectively binds to the S3 sub-pocket of renin, preventing the conversion of angiotensinogen to angiotensin I, thereby blocking eventual conversion to angiotensin II.1,2 Thus, by blocking renin, aliskiren was designed to prevent angiotensin II-mediated arterial vasoconstriction and aldosterone production.1,3 Aliskiren is orally bioavailable and, in combination with valsartan (Item No. 14178), was shown to reduce blood pressure in db/dbmice.4 |
别名 | CGP 60536;SPP 100; |
供应商 | Cayman |
应用文献 | |
1.Rhuel, R.,Rasetti, V.,Maibaum, J., et al. Structure-based drug design: The discovery of novel nonpeptide orally active inhibitors of human renin. Chemistry & Biology 7(7), 493-504 (2000). 2.Holsworth, D.D.,Powell, N.A.,Downing, D.M., et al. Discovery of novel non-peptidic ketopiperazine-based renin inhibitors. Bioorganic & Medicinal Chemistry 13, 2657-2664 (2005). 3.Zaman, M.A.,Oparil, S., and Calhoun, D.A. Drugs targeting the renin-angiotensin-aldosterone system. Nature Reviews.Drug Discovery 1, 621-636 (2002). 4.Tesch, G.H., and Lim, A.K.H. Recent insights into diabetic renal injury from the db/db mouse model of type 2 diabetic nephropathy. American Journal of Physiology.Renal Physiology 300, F301-F310 (2011). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥95% |
计算分子量 | 609.8 |
分子式 | C30H53N3O6 • 1/2C4H4O4 |
CAS号 | 173334-58-2 |
稳定性 | ≥ 2 years |
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