货号 | 10493-5mg |
描述 | The statins inhibit the enzyme HMG-CoA reductase, the rate-limiting enzyme of the mevalonate pathway of cholesterol synthesis, thus lowering blood cholesterol levels. Statins also have additional cardiovascular benefits that appear to be independent of their effects on cholesterol synthesis. Atorvastatin is an HMG-CoA reductase inhibitor (IC50 = 154 nM) that is effective in treating hypercholesterolemia and certain dyslipidemias.1,2,3 It may also be used to prevent coronary or stroke events in hypertensive patients with normal cholesterol levels.4 In addition to inhibiting cholesterol synthesis, atorvastatin reduces the production of low-density lipoprotein (LDL).5,6 It is metabolized by cytochrome P450 3A4 (CYP3A4), producing several metabolites that are important in the therapeutic actions attributed to atorvastatin.7 As a result, inhibitors or inducers of CYP3A4 modify plasma concentrations of atorvastatin and its metabolites, altering the effectiveness of treatment. |
别名 | Cardyl;Lipitor®; |
供应商 | Cayman |
应用文献 | |
1.Dart, A.,Jerums, G.,Nicholson, G., et al. A multicenter, double-blind, one-year study comparing safety and efficacy of atorvastatin versus simvastatin in patients with hypercholesterolemia. American Journal of Cardiology 80, 39-44 (1997). 2.The Diabetes Atorvastatin Lipid Intervention Study, G. The effect of aggressive versus standard lipid lowering by atorvastatin on diabetic dyslipidemia. The DALI study: A double-blind, randomized, placebo-controlled trial in patients with type 2 diabetes and diabetic dyslipidemia. Diabetes Care 24(8), 1335-1341 (2001). 3.van Dam, M.,Zwart, M.,de Beer, F., et al. Long term efficacy and safety of atorvastatin in the treatment of severe type III and combined dyslipidaemia. Heart 88, 234-238 (2002). 4.Sever, P.S.,Dahlöf, B.,Poulter, N.R., et al. Prevention of coronary and stroke events with atorvastatin in hypertensive patients who have average or lower-than-average cholesterol concentrations, in the Anglo-Scandinavian Cardiac Outcomes Trial-Lipid Lowering Arm (ASCOT-LLA): A multicentre randomised controlled trial. Lancet 361, 1149-1158 (2003). 5.Marais, A.D.,Naoumova, R.P.,Firth, J.C., et al. Decreased production of low density lipoprotein by atorvastatin after apheresis in homozygous familial hypercholesterolemia. Journal of Lipid Research 38, 2071-2078 (1997). 6.Naoumova, R.P.,Dunn, S.,Rallidis, L., et al. Prolonged inhibition of cholesterol synthesis explains the efficacy of atorvastatin. Journal of Lipid Research 38, 1496-1500 (1997). 7.Lennernäs, H. Clinical pharmacokinetics of atorvastatin. Clinical Pharmacokinetics 42(13), 1141-1160 (2003). | |
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 | 578.7 |
分子式 | C33H35FN2O5 • 1/2Ca |
CAS号 | 134523-03-8 |
稳定性 | ≥ 2 years |
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