Simvastatin
Catalog No.S1792 Synonyms: MK-0733
Molecular Weight(MW): 418.57
Simvastatin is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays.
6 Customer Reviews
-
Statin-Related Inhibition of Dehydroepiandrosterone Sulfate (DHEAS) Uptake by SLCO2B1 in Prostate Cancer (PC) Cells. B, Uptake of DHEAS in PC cells with 2.5 µM DHEAS and different concentrations of statins when incubated for 60 minutes. Statistical analysis was performed by comparing each condition with the DHEAS 2.5 µM and no statin state except when indicated. C, Uptake of DHEAS in PC cells before (scrambled short hairpin RNA) and after (short hairpin RNA 2B1) SLCO2B1 is knocked down when incubated with 2.5 μM DHEAS and 100 μM atorvastatin for 10 and 60 minutes. Statistical analysis was performed by comparing each condition with scrambled short hairpin RNA after 10 minutes with DHEAS except when indicated. P = .02 for the comparison between scrambled short hairpin RNA with 10 vs 60 minutes of DHEAS incubation for LNCaP and .01 for 22RV1. Other P values are indicated in the figure. Bars indicate means and error bars indicate standard deviation.
JAMA Oncol, 2015, 1(4):495-504. . Simvastatin purchased from Selleck.
-
Pharmacological inhibition of HMGR by simvastatin (250 nM) for 72 h, atorvastatin (10 μM) for 48 h or pitavastatin (1 μM) for 72 h. ***P<0.001; **P<0.01. Error bars = Mean ± SEM (n=3).
Haematologica, 2018, doi: 10.3324/haematol.2018.204701. Simvastatin purchased from Selleck.
-
Representative images of p-Akt and p-GSK-3β expressions by western blot in the subgranular zone (SGZ) of the hippocampus.
Cell Physiol Biochem, 2018, 46(2):618-632. Simvastatin purchased from Selleck.
-
HCMECs were incubated with simvastatin at a range of concentrations for 6 hr. Intracellular signaling responses were assessed by Western blotting for phosphorylation of ERK5 and ERK1/2 using phospho-specific antibodies. Unprenylation of Rap1A was measured as a control for simvastatin activity. Total protein was measured for ERK5, ERK1/2, and Rap1.
J Cell Physiol, 2018, 233(1):186-200. Simvastatin purchased from Selleck.
-
Simvastatin obstructed autophagic flux induced by SAHA in MDA-MB-231. MDA-MB-231 cells that stable expressing (A) tfLC3 or (B) mRFP-LC3 were analyzed by confocal microscopy. MDA-MB-231 cells were treated with SAHA (1 μmol/l) and/or Simvastatin (1 μmol/l) for 16 h. Representative fluorescence images are shown.
Eur J Pharmacol, 2018, 813:161-171. Simvastatin purchased from Selleck.
-
Graph showing retention of 99mTc-RGD measured by longitudinal SPECT imaging (~30 MBq, acquired from 70-90 mins post injection under isoflurane anaesthesia). Retention was significantly higher in the simvastatin treated ischemic limb compared to the vehicle treated ischemic limb on Days 3 and 8 post ligation (n=7 (n=3 blocked), *P<0.05, **P<0.01, 1-way ANOVA with post hoc Tuckey’s test, data shown as %ID/g ± SEM).
Nucl Med Biol, 2017, 46:25-31. Simvastatin purchased from Selleck.
Purity & Quality Control
Choose Selective HMG-CoA Reductase Inhibitors
Biological Activity
| Description | Simvastatin is a competitive inhibitor of HMG-CoA reductase with Ki of 0.1-0.2 nM in cell-free assays. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Targets |
|
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| In vitro |
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. [1] 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. Simvastatin (1.0 μM) enhances phosphorylation of the endogenous Akt substrate endothelial nitric oxide synthase (eNOS), inhibits serum-free media undergo apoptosis and accelerates vascular structure formation. [2] Simvastatin displays anti-inflammatory effects in vitro. Simvastatin (10 μM) reduces anti-CD3/anti-CD28 antibody-stimulated proliferation of PB-derived mononuclear cells and synovial fluid cells from rheumatoid arthritis blood, as well as IFN-γ release. Simvastatin (10 μM) suppresses cell-mediated macrophage TNF-γ release induced via cognate interactions by ~30%. [3] |
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Cell Data |
|
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| Assay |
|
|||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
| In vivo | Simvastatin orally administration inhibits the conversion of radiolabeled acetate to cholesterol with IC50 of 0.2 mg/kg. [1] 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. [4] 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. [5] Simvastatin influences inflammation independent of its effect on plasma cholesterol level. In cynomolgus monkeys consumed an atherogenic diet, Simvastatin (20 mg/kg/day) induces a 1.3-fold less macrophage content in lesions, and 2-fold less vascular cell adhesion molecule-1, interleukin-1beta, and tissue factor expression, companied by a 2.1-fold increases in lesional smooth muscle cell and collagen content. [6] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 83 mg/mL (198.29 mM) |
|---|---|---|
| Ethanol | 83 mg/mL (198.29 mM) | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 2% DMSO+30% PEG 300+5% Tween80+ddH2O For best results, use promptly after mixing. |
10mg/mL |
* 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 | 418.57 |
|---|---|
| Formula | C25H38O5 |
| CAS No. | 79902-63-9 |
| Storage | powder |
| in solvent | |
| Synonyms | MK-0733 |
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT03571802 | Not yet recruiting | Drug: Simvastatin | Obesity|Hyperlipidemias | National University Hospital Singapore | September 1 2018 | Phase 4 |
| NCT03387670 | Recruiting | Drug: Simvastatin|Drug: Placebo | Secondary Progressive Multiple Sclerosis (SPMS) | University College London|University of Edinburgh|Queen Mary University of London|London School of Hygiene and Tropical Medicine|University of Leeds|The Leeds Teaching Hospitals NHS Trust|Imperial College Healthcare NHS Trust | March 28 2018 | Phase 3 |
| NCT03329118 | Unknown status | Drug: SHR3824 Simvastatin | Type 2 Diabetes | Jiangsu HengRui Medicine Co. Ltd. | November 24 2017 | Phase 1 |
| NCT03660293 | Completed | Drug: Atorvastatin|Drug: Captopril|Drug: L-carnitine | Diabetes Mellitus Type 1 | Tanta University | April 1 2017 | Not Applicable |
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.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.
Frequently Asked Questions
-
Question 1:
Can you please advise if Simvastatin has been tested effectively for in vivo use in mice? What solvent can be used to deliver Simvastatin in vivo?
-
Answer:
This compound is an oral drug and a lot of studies report its use in mice. According to this paper (http://atvb.ahajournals.org/content/21/1/115.full), 0.5% Methyl-cellulose can be used as the vehicle.
-
Question 2:
If any specific protocols exist for in vitro use, specifically any steps required to activate the compound?
-
Answer:
This product is supplied in an inactive form and requires treatment with NaOH in EtOH followed by neutralization to pH 7.2 for activation. Please find the details from the following reference: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2739764/.
