CAS 287714-41-4 Circulatory system medication for Anti-atherosclerosis Rosuvastatin Powder

CAS 287714-41-4 Circulatory system medication for Anti-atherosclerosis Rosuvastatin Powder

The Introductction of Rosuvastatin:

Rosuvastatin, sold under the trade name Crestor, is astatin that is used in combination with exercise, diet control and weight loss to treat hypercholesterolemia and other related conditions, as well as to prevent cardiovascular disease.

The Application & Function of Rosuvastatin:

1. Hypolipidemic effect
Rovastatin has an obvious effect on lowering blood lipids. Generally, statins can reduce the level of low density lipoprotein cholesterol (LDL-C) by 17% to 54%. The phase ii clinical trial results of rovastatin showed that when the dose was 80 mg, rovastatin reduced LDL-C by 65%, which is the best effect among statins. Rovastatin increases the number of LDL receptors. In human hepatocellular tumor, rovastatin raised the mRNA volume of LDL receptor about 10 times more than pravastatin.
2. Selective effect on hepatocytes
Cholesterol from hepatocytes is the main cause of blood cholesterol formation, while cholesterol from non-hepatocytes is necessary for normal cells. The main site of action of rovastatin is the liver. From the perspective of inhibiting sterol synthesis, the selectivity of rovastatin to rat liver was higher than that to peripheral tissues, and higher than pravastatin or simvastatin to liver tissues. Rovastatin is absorbed into liver cells through an active absorption process and is 1000 times more potent in inhibiting cholesterol in rat liver cells than in fibroblasts.
3. Anti-atherosclerosis effect
Rovastatin can reduce blood lipid, lipid infiltration and foam cell formation, which is beneficial to delay atherosclerosis. The drug can also inhibit smooth muscle cell proliferation and promote cell apoptosis by blocking the hydroxymethylglutaric acid pathway, especially the formation of isoprenoid metabolites, thus stabilizing atherosclerosis plaque and delaying the occurrence and development of atherosclerosis.

Application:

Although rovastatin has the common pharmacophore dihydroxyheptanoic acid part of statins, the rest of its molecular structure is different from other similar drugs, among which the presence of polar methylsulfonyl amino makes it present a low lipophilic. This means that its passive diffusion ability is low and it is difficult to enter non-hepatocytes. However, it can be absorbed by liver cells in large quantities through selective organic anion transport process, and has the characteristics of selective distribution and use for HMG-COA reductase in liver. At the same time, the relatively water-soluble nature of its structure enables it to avoid the defect that requires extensive metabolism of cytochrome P450 before elimination, and greatly reduces the chance of interaction with other drugs.

The COA of Rosuvastatin