Mevastatin

Catalog No.S4223 Batch:S422304

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Technical Data

Formula

C23H34O5
Molecular Weight 390.51 CAS No. 73573-88-3
Solubility (25°C)* In vitro DMSO 78 mg/mL (199.73 mM)
Ethanol 20 mg/mL (51.21 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 1.33mg/ml (3.41mM) Taking the 1 mL working solution as an example, add 50 μL of 26.6 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution
5% DMSO 95% Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 0.156mg/ml (0.40mM) Taking the 1 mL working solution as an example, add 50 μL of 3.12 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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 (from reference)

Animal Study:

[1]
  • Animal Models

    Wistar-Imamichi male rats

  • Dosages

    5 mg/kg, 20 mg/kg

  • Administration

    orally

References

  • https://pubmed.ncbi.nlm.nih.gov/1010803/
  • https://pubmed.ncbi.nlm.nih.gov/11283400/

Customer Product Validation

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.

Data from [ , , Atherosclerosis, 2018, 276:28-38 ]

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.

Data from [ , , Eur J Pharmacol, 2017, 813:161-171 ]

Selleck's Mevastatin Has Been Cited by 9 Publications

Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805] PubMed: 39581704
Systems immunology-based drug repurposing framework to target inflammation in atherosclerosis [ Nat Cardiovasc Res, 2023, 2(6):550-571] PubMed: 37771373
The cholesterol metabolite 25-hydroxycholesterol restrains the transcriptional regulator SREBP2 and limits intestinal IgA plasma cell differentiation [ Immunity, 2021, 54(10):2273-2287.e6] PubMed: 34644558
Simvastatin Suppresses Human Breast Cancer Cell Invasion by Decreasing the Expression of Pituitary Tumor-Transforming Gene 1 [ Front Pharmacol, 2020, 11:574068] PubMed: 33250768
Accumulation of 8,9-unsaturated sterols drives oligodendrocyte formation and remyelination [Hubler Z, et al. Nature, 2018, 560(7718):372-376] PubMed: 30046109
Simvastatin functions as a heat shock protein 90 inhibitor against triple-negative breast cancer [Kou X, et al. Cancer Sci, 2018, 109(10):3272-3284] PubMed: 30039622
MK-2206, an allosteric inhibitor of AKT, stimulates LDLR expression and LDL uptake: A potential hypocholesterolemic agent [Bjune K, et al. Atherosclerosis, 2018, 276:28-38] PubMed: 30025252
Triciribine increases LDLR expression and LDL uptake through stabilization of LDLR mRNA. [ Sci Rep, 2018, 8(1):16174] PubMed: 30385871
Vorinostat and Simvastatin have synergistic effects on triple-negative breast cancer cells via abrogating Rab7 prenylation. [Kou X, et al. Eur J Pharmacol, 2017, 813:161-171] PubMed: 28826913

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.