1. Metabolic Enzyme/Protease Anti-infection Autophagy Apoptosis
  2. HMG-CoA Reductase (HMGCR) Bacterial Autophagy Apoptosis Antibiotic
  3. Mevastatin

メバスタチン  (Synonyms: コンパクチン; Compactin; Mevastatin; ML236B)

製品番号: HY-17408 純度: 99.08%
COA 取扱説明書 Technical Support

Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G0/G1 phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment.

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CAS 番号 : 73573-88-3

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 67 在庫あり
Solution
10 mM * 1 mL in DMSO USD 67 在庫あり
Solid
50 mg $61 在庫あり
100 mg $99 在庫あり
500 mg $297 在庫あり
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カスタマーレビュー

Based on 7 publication(s) in Google Scholar

Other Forms of Mevastatin:

Top Publications Citing Use of Products

    Mevastatin purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2020 Jan 13;11(1):25.  [Abstract]

    Cell proliferation ability was evaluated using the MTS assay in SKOV3 cells treated as indicated (EV, empty vector; SIK2, expression vector encoding SIK2; C75, FASN inhibitor, 25 μM for 24 h; Mevastatin, HMGCR inhibitor, 1 μM for 24 h).

    Mevastatin purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2020 Sep;20(3):2855-2869.  [Abstract]

    Western blotting showing the location of mSREBP, SCD1 and β‑catenin in KYSE-150 cells treated with or without Mevastatin (10 µM) for 24 h.
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    • 参考文献

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    製品説明

    Mevastatin (Compactin) is a first HMG-CoA reductase inhibitor that belongs to the statins class. Mevastatin is a lipid-lowering agent, and induces apoptosis, arrests cancer cells in G0/G1 phase. Mevastatin also increases endothelial nitric oxide synthase (eNOS) mRNA and protein levels. Mevastatin has antitumor activity and has the potential for cardiovascular diseases treatment[1][2][3].

    IC50 & Target

    HMG-CoA reductase[1][2]
    Apoptosis[1]

    Cellular Effect
    Cell Line Type Value Description References
    DLD-1 IC50
    3.2 μM
    Compound: 26
    Cytotoxicity in human DLD-1 cells expressing APC mutant assessed as reduction in cell viability incubated for 96 hrs by Cell Titer-Glo assay
    Cytotoxicity in human DLD-1 cells expressing APC mutant assessed as reduction in cell viability incubated for 96 hrs by Cell Titer-Glo assay
    [PMID: 33445154]
    HCT-116 IC50
    18.6 μM
    Compound: 26
    Cytotoxicity in human HCT-116 cells expressing wild type APC assessed as reduction in cell viability incubated for 96 hrs by Cell Titer-Glo assay
    Cytotoxicity in human HCT-116 cells expressing wild type APC assessed as reduction in cell viability incubated for 96 hrs by Cell Titer-Glo assay
    [PMID: 33445154]
    HEK293 IC50
    159 μM
    Compound: 27
    Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
    Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay
    [PMID: 31260312]
    体外実験

    Mevastatin (0-128 μM; 5 days; Caco-2 cells) treatment causes a dose-dependent decrease in cell number[1].
    Mevastatin (32-128 μM; 24-72 hours; Caco-2 cells) treatment causes an early G0/G1 phase and a late G2/M phase cell cyclr arrest[1].
    Mevastatin (32-128 μM; 72 hours; Caco-2 cells) treatment causes a down-regulation of cyclin-dependent kinases (cdk) 4 and cdk 6 as well as cyclin D1, while cdk 2 and cyclin E protein levels remained unchanged. Cell cycle inhibitors p21 and p27 are significantly upregulated by Mevastatin[1].
    Mevastatin (16-256 μM; Caco-2 cells) treatment induces apoptosis in a dose-dependent manner[1].
    Treatment of Neuro2a cells with mevastatin for 24 hours induced neurite outgrowth associated with up-regulation of the neuronal marker protein NeuN. Mevastatin triggers phosphorylation of the key kinases epidermal growth factor receptor (EGFR), ERK1/2, and Akt/protein kinase B. Inhibition of EGFR, PI3K, and the mitogen-activated protein kinase cascade blocks Mevastatin-induced neurite outgrowth[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Viability Assay[2]

    Cell Line: Caco-2 cells
    Concentration: 0 µM, 8 µM, 16 µM, 32 µM, 64 µM, 128 µM
    Incubation Time: 5 days
    Result: Caused a dose-dependent decrease in cell number.

    Cell Cycle Analysis[2]

    Cell Line: Caco-2 cells
    Concentration: 32 µM, 64 µM, 128 µM
    Incubation Time: 24 hours, 48 hours, 72 hours
    Result: Caused a dose-dependent increase of cells in G0/G1 and G2/M phases of the cell cycle.

    Western Blot Analysis[2]

    Cell Line: Caco-2 cells
    Concentration: 32 µM, 64 µM, 128 µM
    Incubation Time: 72 hours
    Result: Resulted in a down-regulation of cyclin-dependent kinases (cdk) 4 and cdk 6 as well as cyclin D1.
    体内実験

    Mevastatin (2-20 mg/kg; delivered via ALZET miniosmotic pumps; daily; for 7, 14, or 28 days; wild-type 129-SV/eVTAcBr male mice and eNOS-deficient male mice) treatment increases levels of endothelial nitric oxide synthase (eNOS) mRNA and protein, reduces infarct size, and improves neurological deficits in a dose- and time-dependent manner[2].
    The topical infusion of Mevastatin (2.5 pmol/hr) increases bone mass (MRL/MpJ mouse) of isografted bone by increasing bone turnover and, at least in part, by promoting the expression of bone morphogenetic protein-2 (BMP-2) mRNA and receptor activator of NF-κB ligand (RANKL) mRNA[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Wild-type 129-SV/eVTAcBr male mice and eNOS-deficient male mice (18-22 g) with the filament model[2]
    Dosage: 2 mg/kg or 20 mg/kg
    Administration: Delivered via 7- or 14-day ALZET miniosmotic pumps implanted subcutaneously; daily; for 7, 14, or 28 days
    Result: Increased levels of endothelial nitric oxide synthase (eNOS) mRNA and protein, reduced infarct size, and improved neurological deficits in a dose- and time-dependent manner.
    分子量

    390.51

    分子式

    C23H34O5

    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CC[C@H](C)C(O[C@H]1CCC=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(O3)=O)[C@@]12[H])=O

    Structure Classification
    Initial Source

    Penicillium citrinum

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶剤 & 溶解度
    体外: 

    DMSO : 200 mg/mL (512.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5608 mL 12.8038 mL 25.6075 mL
    5 mM 0.5122 mL 2.5608 mL 5.1215 mL
    10 mM 0.2561 mL 1.2804 mL 2.5608 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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    • Dilution Calculator

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    一般には略語で表示されます:C1V1 = C2V2

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.08%

    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (protect from light). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5608 mL 12.8038 mL 25.6075 mL 64.0188 mL
    5 mM 0.5122 mL 2.5608 mL 5.1215 mL 12.8038 mL
    10 mM 0.2561 mL 1.2804 mL 2.5608 mL 6.4019 mL
    15 mM 0.1707 mL 0.8536 mL 1.7072 mL 4.2679 mL
    20 mM 0.1280 mL 0.6402 mL 1.2804 mL 3.2009 mL
    25 mM 0.1024 mL 0.5122 mL 1.0243 mL 2.5608 mL
    30 mM 0.0854 mL 0.4268 mL 0.8536 mL 2.1340 mL
    40 mM 0.0640 mL 0.3201 mL 0.6402 mL 1.6005 mL
    50 mM 0.0512 mL 0.2561 mL 0.5122 mL 1.2804 mL
    60 mM 0.0427 mL 0.2134 mL 0.4268 mL 1.0670 mL
    80 mM 0.0320 mL 0.1600 mL 0.3201 mL 0.8002 mL
    100 mM 0.0256 mL 0.1280 mL 0.2561 mL 0.6402 mL
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    一般には略語で表示されます:C1V1 = C2V2

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    製品名:
    Mevastatin
    製品番号:
    HY-17408
    数量:
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