Mevastatin

Catalog No.S4223 Synonyms: ML-236B

Mevastatin Chemical Structure

Molecular Weight(MW): 390.51

Mevastatin 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.

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Cited by 4 Publications

2 Customer Reviews

  • Sterol-starved HepG2 cells were treated with vehicle or mevastatin for 24 h before exposure to the indicated concentrations of MK-2206 for a further 14 h. Cells were then harvested and subjected to Western blot analysis. Upper panel shows one representative blot from six experiments. Lower panel: the immunoblots data were plotted relative to vehicle-treated cells. Error bars represent SD. One, two and three asterisks indicate p < 0.05, p < 0.01 and p < 0.001, respectively, compared with matched vehicle-treated cells.

    Atherosclerosis, 2018, 276:28-38. Mevastatin purchased from Selleck.

    SAHA and Statins on the proliferation of TNBC cells. TNBC or MCF-10A cells were treated with (D) Mevastatin, (E) Mevastatin + 0.5 μmol/l SAHA. Except for that a final concentration of 0.5 μmol/l SAHA was used in combination groups, serial 2-fold dilutions of each compound in a final concentration range of 32–0.03 μmol/l were used in experiments. Cell counting was assessed by using CCK8 reagent at 72 h after treatments. Dose-response curves were plotted as concentration (logarithmic scale) versus normalized response-variable slope using non-linear regression by software Prism 5.0 (Graphpad). Experiments were performed in triplicate, and data were presented as the mean±S.E.M.

    Eur J Pharmacol, 2017, 813:161-171. Mevastatin purchased from Selleck.

Purity & Quality Control

Choose Selective HMG-CoA Reductase Inhibitors

Biological Activity

Description Mevastatin 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

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 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]

Protocol

Animal Research:[1]
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  • Animal Models: Wistar-Imamichi male rats
  • Formulation: saline
  • Dosages: 5 mg/kg, 20 mg/kg
  • Administration: orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (199.73 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 390.51
Formula

C23H34O5

CAS No. 73573-88-3
Storage powder
in solvent
Synonyms ML-236B

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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.

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HMG-CoA Reductase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID