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Lovastatin

Product #: TL0007
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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

 


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