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100mg |
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500mg |
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1g |
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2g |
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Other Sizes |
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Purity: ≥98%
Mevastatin (CS500; ML236B; Mevastatin; Compactin; ML-236B), an approved anti-hyperliperdemic drug of the statin class, is a potent and competitive inhibitor of HMG-Coenzyme A (HMG-CoA) reductase with anti-hyperlipidemic effects. It has a binding affinity of around 10,000-fold higher than the native ubstrate HMG-CoA. Mevastatin is a naturally occuring compound isolated from the mold Penicillium citrinum by Akira Endo in the 1970s, and is generally considered to be the first statin drug but it never made to the market due to undesired adverse effects.
ln Vitro |
Treatment with levofloxacin (0–128 μM; 5 days; Caco-2 cells) reduces cell number in a dose-dependent manner [1]. Treatment with mevastatin (32-128 μM; 24-72 hours; Caco-2 cells) causes cell cycle arrest in two stages: early G0/G1 and late G2/M [1]. Cyclin-dependent kinase (cdk) 4 and 6 as well as cyclin D1 were downregulated after 72 hours of mevastatin (32-128 μM) treatment in Caco-2 cells; in contrast, the levels of cdk 2 and cdk E protein stayed unaltered. Mevastatin dramatically increases p21 and p27, two cell cycle inhibitors [1]. Treatment with mevastatin (16-256 μM; Caco-2 cells) dose-dependently promotes apoptosis [1]. Mevastatin treatment of Neuro2a cells for 24 hours resulted in neurite outgrowth and increased expression of the neuronal marker protein NeuN. The important kinases ERK1/2, Akt/protein kinase B, and epidermal growth factor receptor (EGFR) are phosphorylated in response to mevastatin. Mevastatin-induced axonal development is inhibited by PI3K, EGFR, and mitogen-activated protein kinase cascade inhibition [4].
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ln Vivo |
In wild-type 129-SV/eVTAcBr male mice and eNOS-deficient male mice, mevastatin (2–20 mg/kg; administered daily via ALZET micro-osmotic pump) increases endothelial nitric oxide levels synthase (eNOS) mRNA and protein, reduces infarct size, and improves neurological deficits in a dose- and time-dependent manner [2]. Mevastatin (2.5 pmol/hour) administered locally promotes bone morphogenetic protein-2 (BMP-2) mRNA and receptor activator of NF-κB ligand (RANKL) mRNA expression in addition to boosting bone turnover. The transplanted bone mass in the MRL/MpJ mice [3].
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Cell Assay |
Cell Viability Assay[2]
Cell Types: Caco-2 cells Tested Concentrations: 0 µM, 8 µM, 16 µM, 32 µM, 64 µM, 128 µM Incubation Duration: 5 days Experimental Results: Caused a dose-dependent decrease in cell number. Cell Cycle Analysis[2] Cell Types: Caco-2 cells Tested Concentrations: 32 µM, 64 µM, 128 µM Incubation Duration: 24 hrs (hours), 48 hrs (hours), 72 hrs (hours) Experimental Results: Caused a dose-dependent increase of cells in G0/G1 and G2/ M phases of the cell cycle. Western Blot Analysis[2] Cell Types: Caco-2 cells Tested Concentrations: 32 µM, 64 µM, 128 µM Incubation Duration: 72 hrs (hours) Experimental Results: Resulted in a down-regulation of cyclin-dependent kinases (cdk ) 4 and cdk 6 as well as cyclin D1. |
Animal Protocol |
Animal/Disease Models: Wild-type 129-SV/eVTAcBr male mice and eNOS-deficient male mice (18-22 g) with the filament model[2]
Doses: 2 mg/kg or 20 mg/kg Route of Administration: Delivered via 7- or 14-day ALZET miniosmotic pumps implanted subcutaneously (sc); daily; for 7, 14, or 28 days Experimental Results: Increased levels of endothelial nitric oxide synthase (eNOS) mRNA and protein, decreased infarct size, and improved neurological deficits in a dose- and time- dependent manner. |
References |
[1]. Wächtershäuser A, et al. HMG-CoA reductase inhibitor mevastatin enhances the growth inhibitory effect of butyrate in the colorectal carcinoma cell line Caco-2. Carcinogenesis. 2001 Jul;22(7):1061-7.
[2]. Amin-Hanjani S, Stagliano NE, Yamada M, et al. Mevastatin, an HMG-CoA reductase inhibitor, reduces stroke damage and upregulates endothelial nitric oxide synthase in mice. Stroke. 2001 Apr;32(4):980-6. [3]. Sugazaki M, Hirotani H, Echigo S, et al. Effects of mevastatin on grafted bone in MRL/MpJ mice. Connect Tissue Res. 2010 Apr;51(2):105-12. [4]. Evangelopoulos ME, Weis J, Krüttgen A. Mevastatin-induced neurite outgrowth of neuroblastoma cells via activation of EGFR. J Neurosci Res. 2009 Jul;87(9):2138-44. |
Molecular Formula |
C23H34O5
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Molecular Weight |
390.51
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CAS # |
73573-88-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02441400 | Terminated | Device: EndoStim LES Stimulation System |
GERD | EndoStim Inc. | May 2013 |
Dose–response curve of Caco-2 cells incubated with increasing concentrations of mevastatin for 5 days. Means ± SD, n = 8. td> |
(A) Cell counts of Caco-2 cells incubated with butyrate (1 or 2 mM) alone or in combination with mevastatin (64 μM) for up to 5 days. Means ± SD, n = 8. (B) Cell counts of Caco-2 cells incubated with butyrate (1 or 2 mM) alone or in combination with mevalonate (2.5 mM), mevastatin (64 μM) or mevalonate (2.5 mM) plus mevastatin (64 μM) for 5 days. Means ± SD, n = 8, *P < 0.05, **P < 0.01. td> |
(A) Cell counts of HCT-116 cells incubated with butyrate (1 or 2 mM) alone or in combination with mevastatin (5 μM) for up to 72 h. Means ± SD, n = 8. (B) Cell counts of HCT-116 cells incubated with butyrate (1 or 2 mM) alone or in combination with mevalonate (2.5 mM), mevastatin (5 μM) or mevalonate (2.5 mM) plus mevastatin (5 μM) for 72 h. Means ± SD, n = 8, *P < 0.05, **P < 0.01. td> |