l General Information |
Product Name | Lovastatin |
General deion | Lovastatin is a cholesterol lowering drug and competitive inhibitor of HMG-CoA reductase, a rate limiting enzyme in cholesterol synthesis. |
Synonym | 2-Methyl-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1-naphthalenyl ester butanoic acid, 6-α-Methylcompactin, Lovastatin, Monacolin K |
Purity | ≥98%(HPLC) | CAS Number | 75330-75-5 |
Formula | C24H36O5 | Molecular Weight | 404.54 |
Suitability | BioReagent, suitable for cell culture, etc. |
l Physical and Chemical Information |
Appearance | White or Off-white solid |
Solubility(25℃) | DMSO | ~8mg/mL |
Ethanol | ~5mg/mL |
Water | Insoluble |
l Biological Information |
Biochem/Physiol Actions | The primary cause of cardiovascular disease is atherosclerotic plaque formation. Sustained elevations of cholesterol in the blood increase the risk of cardiovascular disease. Lovastatin lowers hepatic cholesterol synthesis by competitively inhibiting HMG-CoA reductase, the enzyme that catalyzes the rate-limiting step in the cholesterol biosynthesis pathway via the mevalonic acid pathway. Decreased hepatic cholesterol levels causes increased uptake of low density lipoprotein (LDL) cholesterol and reduces cholesterol levels in the circulation. At therapeutic doses, lovastatin decreases serum LDL cholesterol by 29-32%, increases high density lipoprotein (HDL) cholesterol by 4.6-7.3%, and decrease triglyceride levels by 2-12%. HDL cholesterol is thought to confer protective effects against CV disease, whereas high LDL and triglyceride levels are associated with higher risk of disease. Lovastatin is a lactone metabolite isolated from the fungus Aspergillus terreus with cholesterol-lowering and potential antineoplastic activities. Lovastatin is hydrolyzed to the active beta-hydroxyacid form, which competitively inhibits 3-hydroxyl-3-methylgutarylcoenzyme A (HMG-CoA) reductase, an enzyme involved in cholesterol biosynthesis. In addition, this agent may induce tumor cell apoptosis and inhibit tumor cell invasiveness, possibly by inhibiting protein farnesylation and protein geranylgeranylation, and may arrest cells in the G1 phase of the cell cycle. The latter effect sensitizes tumor cells to the cytotoxic effects of ionizing radiation. |
Application | 1. Compounds that inhibit HMG-CoA reductases. They have been shown to directly lower cholesterol synthesis. 2. Substances used to lower plasma cholesterol levels. |
l Packaging & Storage |
Packaging | 250mg; 1g |
Storage temp. | 0-5℃ |
l Precautions and Disclaimer |
This product is for R&D use only, not for drug, household, or other uses. |
l References |
1. http://www.drugbank.ca/drugs/DB00227 2. https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&ns=NCI_Thesaurus&code=C620 3. https://www.ncbi.nlm.nih.gov/mesh/68019161 4. https://www.ncbi.nlm.nih.gov/mesh/68000924 |