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Simvastatin (MK 733)

Cat. No. M3497

All AbMole products are for research use only, cannot be used for human consumption.

Simvastatin (MK 733) Structure
Synonym:

MK 733; MK-0733

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 40  USD40 In stock
50mg USD 70  USD70 In stock
100mg USD 120  USD120 In stock
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Quality Control & Documentation
Biological Activity

Simvastatin (MK-0733, MK 733) is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays. Simvastatin induces ferroptosis, mitophagy, autophagy and apoptosis. Simvastatin inhibits exosome release.

Prior to use in cell assays, Simvastatin needs to be activated by NaOH in EtOH treatment. Simvastatin inhibits cholesterol synthesis in mouse L-M cell (fibroblast), rat H4II E cell (liver), and human Hep G2 cell (liver) with IC50 of 19.3 nM, 13.3 nM and 15.6 nM, respectively. Simvastatin treatment leads to a dose-dependent increase in serine 473 phosphorylation of Akt within 30 minutes, with maximal phosphorylation occurring at 1.0 µM.

In vivo, Simvastatin orally administration inhibits the conversion of radiolabeled acetate to cholesterol with IC50 of 0.2 mg/kg. Simvastatin (4 mg/day) orally administration for 13 weeks to rabbits fed an atherogenci cholesterol-rich diet, returns the cholesterol-induced increases in total cholesterol, LDL-cholesterol and HDL-cholesterol to normal level. Simvastatin (6 mg/kg) produces an increase in LDL receptor-dependent binding and increases the number of hepatic LDL receptors in rabbits fed a diet containing 0.25% cholesterol.


Activation of simvastatin

Simvastatin needs to be activated by opening of the lactone ring before use in cell culture. Briefly, eight milligrams of simvastatin (0.019 mM) were dissolved in 0.2 ml of 100% ethanol, with subsequent addition of 0.3 ml of 0.1 N NaOH. The solution was heated at 50°C for 2 h in a sand bath and then neutralized with HCl to pH 7.2. The resulting solution was brought to a final volume (1 ml) with distilled water, and aliquots were stored at −80°C until use.

Product Citations
Customer Product Validations & Biological Datas
Source Pak J Pharm Sci (2016). Figure 1. Simvastatin (Abmole Bioscience)
Method HPLC chromatogram
Cell Lines
Concentrations 200μg/ml
Incubation Time
Results The results summarized in (table 1) obtained for pravastatin, rosuvastatin, pitavastatin, atorvastatin, fluvastatin, lovastatin and simvastatin were comparable with the corresponding labeled amounts.
Chemical Information
Molecular Weight 418.57
Formula C25H38O5
CAS Number 79902-63-9
Solubility (25°C) DMSO 80 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Jaqueline Aparecida Duarte, et al. The potential use of simvastatin for cancer treatment: A review

[2] Tanzeela A Fattah, et al. Synthetic Approaches Towards Antihypercholesterolemic Drug Simvastatin

[3] Nawal M Al-Rasheed, et al. Simvastatin Ameliorates Diabetic Cardiomyopathy by Attenuating Oxidative Stress and Inflammation in Rats

[4] L B Ramsey, et al. The clinical pharmacogenetics implementation consortium guideline for SLCO1B1 and simvastatin-induced myopathy: 2014 update

[5] Weijiang Dong, et al. J Lipid Res . Differential effects of simvastatin and pravastatin on expression of Alzheimer's disease-related genes in human astrocytes and neuronal cells

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Keywords: Simvastatin (MK 733), MK 733; MK-0733 supplier, Autophagy, inhibitors, activators

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