Simvastatin

SKU: orb1310385

Description

Simvastatin is an orally active HMG-CoA reductase inhibitor (Ki=0.2 nM) used in research to study cholesterol biosynthesis inhibition. It is applied in hypolipidemic, cardiovascular disease, and atherosclerosis research, utilizing both in vitro enzyme assays and in vivo animal models.

Research Area

Cell Biology

Key Properties

• CAS Number: 79902-63-9
• MW: 418.58
• Purity: >98%
• Formula: C₂₅H₃₈O₅
• SMILES: O(C(C(CC)(C)C)=O)[C@@H]1[C@]2(C(C=C[C@H](C)[C@@H]2CC[C@@H]3C[C@@H](O)CC(=O)O3)=C[C@H](C)C1)[H]
• Target: HMG-CoA reductase
• Solubility: Soluble in DMSO (up to 25 mg/ml) or in Ethanol (up to 35 mg/ml).

Bioactivity

• Target IC50:
  L6 cells:229 nM|Hepatocyte cells:1.3 nM|MEF cells:36.7 μM|HEK293 cells:11 μM|Hs 68 cells:26.4 μM|A549 cells:16.3 μM|HMG-CoA reductase:0.1-0.2 nM (Ki)
• In Vivo:
  METHODS: To study in vivo activity, Simvastatin (60 mg/kg, aqueous 2% DMSO+30% PEG 400+5% Tween 80) was administered by gavage to C57BL/6J mice once daily for six weeks on a CF diet. RESULTS: Simvastatin treatment reduced serum cholesterol levels by 18%, and retinal cholesterol and lipoprotein cholesterol levels by 24% and 21%, respectively. METHODS: To assay antitumor activity in vivo, Simvastatin (5-50 mg/kg in methylcellulose) was administered to BALB/c nu/nu mice by gavage once daily for three days. Subsequently, colorectal cancer cells COLO205 were subcutaneously inoculated into the right side of the mice. RESULTS: Simvastatin inhibited tumor growth in a xenograft mouse model by inducing tumor cell apoptosis and inhibiting tumor angiogenesis.
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• In Vitro:
  METHODS: BCa cells 5637, EJ and T24 were treated with Simvastatin (0.5-40 µM) for 48 h. Cell viability was measured by MTT assay. RESULTS: Simvastatin significantly inhibited the survival of the three BCa cells in a dose-dependent manner. METHODS: Human fibroblast SAEC and four tumor cells MCF7, HepG2, NCH, NCI were treated with Simvastatin (20 µM) for 72 h. Apoptosis was detected by TUNEL. RESULTS: Simvastatin induced apoptosis in different types of human tumor cells, but not in SAEC cells.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Mevinolin

Compound Identifiers

PubChem CID

54454