Home Metabolism HMG-CoA Reductase inhibitor Mevastatin For research use only.

Mevastatin

Synonyms: ML-236B,Compactin

Mevastatin (ML-236B,Compactin) is a competitive inhibitor of HMG-Coenzyme A (HMG-CoA) reductase with a binding affinity 10,000 times greater than the HMG-CoA substrate itself.

Mevastatin Chemical Structure

Mevastatin Chemical Structure

CAS No. 73573-88-3

Purity & Quality Control

Mevastatin Related Products

Signaling Pathway

HMG-CoA Reductase Signaling Pathways

HMG-CoA Reductase Signaling Pathway

Biological Activity

Description Mevastatin (ML-236B,Compactin) is a competitive inhibitor of HMG-Coenzyme A (HMG-CoA) reductase with a binding affinity 10,000 times greater than the HMG-CoA substrate itself.
Targets
HMG-CoA reductase [1]
In vitro
In vitro

Mevastatin is a cholesterol-lowering agent isolated from Penicillium citinium. It reduces cholesterol synthesis to 50% of control at 0.01 pg/mL (26 nM). [1] It is structurally similar to the HMG, a substituent of the endogenous substrate of HMG-CoA reductase. Mevastatin is a prodrug that is activated in vivo via hydrolysis of the lactone ring. The hydrolyzed lactone ring mimics the tetrahedral intermediate produced by the reductase allowing the agent to bind with 10,000 times greater affinity than its natural substrate. The bicyclic portion of mevastatin binds to the coenzyme A portion of the active site. Mevastatin increases levels of eNOS mRNA and protein, reduces infarct size, and improves neurological deficits in a dose- and time-dependent manner.[2]
In Vivo
In vivo

At doses of 5 and 20 mg/kg, mevastatin produces reduction of serum cholesterol levels at 3 hours after oral administration. It lowers the levels of serum cholesterol by approximately 30 % at a dose of 20 mg/kg. [1] Mevastatin lowers hepatic production of cholesterol by competitively inhibiting HMG-CoA reductase. Cholesterol levels are reduced only after 28 days of treatment and does not correlate with infarct reduction. Baseline absolute cerebral blood flow is 30% higher after 14-day high-dose treatment. [2]
Animal Research Animal Models Wistar-Imamichi male rats
Dosages 5 mg/kg, 20 mg/kg
Administration orally

Chemical Information & Solubility

Molecular Weight 390.51 Formula

C23H34O5
CAS No. 73573-88-3 SDF Download Mevastatin SDF
Smiles CCC(C)C(=O)OC1CCC=C2C1C(C(C=C2)C)CCC3CC(CC(=O)O3)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 78 mg/mL ( (199.73 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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