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Simvastatin

(Synonyms: MK 733)

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Based on 83 publication(s) in Google Scholar

Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a K_i of 0.2 nM.

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Pureté: 99.56%
CAS No.: 79902-63-9
Formule: C₂₅H₃₈O₅
Masse moléculaire:418.57

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Simvastatin Chemical Structure

CAS No.: 79902-63-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (83)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
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Activité biologique

Description

Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a K_i of 0.2 nM.

IC₅₀ & Target

Ki: 0.2 nM (HMG-CoA reductase)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	16.3 μM Compound: 11	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 23570542]
HEK293	IC₅₀	11 μM Compound: Simvastatin	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate	[PMID: 22587986]
HEK293	IC₅₀	4.4 μM Compound: Simvastatin	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate	[PMID: 22587986]
HEK293	IC₅₀	6 μM Compound: Simvastatin	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate	[PMID: 22587986]
HEK293	IC₅₀	9.7 μM Compound: Simvastatin lactone	TP_TRANSPORTER: inhibition of estradiol-17beta-glucuronide uptake(estradiol-17beta-glucuronide:0.02uM) in OATP1B1-expressing HEK293 cells TP_TRANSPORTER: inhibition of estradiol-17beta-glucuronide uptake(estradiol-17beta-glucuronide:0.02uM) in OATP1B1-expressing HEK293 cells	[PMID: 15616150]
Hepatocyte	IC₅₀	1.3 nM Compound: sim, simvastatin	Inhibition of cholesterol synthesis in rat liver hepatocytes after 4 hrs Inhibition of cholesterol synthesis in rat liver hepatocytes after 4 hrs	[PMID: 17560788]
Hepatocyte	IC₅₀	1.3 nM Compound: Simvastatin	Inhibition of cholesterol synthesis in rat hepatocyte Inhibition of cholesterol synthesis in rat hepatocyte	[PMID: 17574412]
Hepatocyte	IC₅₀	1.3 nM Compound: simvastatin	Inhibition of cholesterol synthesis in rat hepatocyte Inhibition of cholesterol synthesis in rat hepatocyte	[PMID: 18155906]
Hepatocyte	IC₅₀	4 nM Compound: simvastatin	Inhibition of cholesterol synthesis in rat hepatocytes Inhibition of cholesterol synthesis in rat hepatocytes	[PMID: 17574411]
Hepatocyte	IC₅₀	6.2 nM Compound: simvastatin	Inhibition of cholesterol synthesis in rat hepatocytes assessed as incorporation of [14C]acetate into cholesterol Inhibition of cholesterol synthesis in rat hepatocytes assessed as incorporation of [14C]acetate into cholesterol	[PMID: 18412317]
HepG2	IC₅₀	40 nM Compound: Simvastatin	In vitro inhibitory activity was evaluated on cholesterol biosynthesis in HepG2 cells In vitro inhibitory activity was evaluated on cholesterol biosynthesis in HepG2 cells	[PMID: 14741258]
Hs68	IC₅₀	26.4 μM Compound: 11	Cytotoxicity against human HS68 cells after 72 hrs by MTT assay Cytotoxicity against human HS68 cells after 72 hrs by MTT assay	[PMID: 23570542]
Ishikawa	IC₅₀	~ 17 μM Compound: Simvastatin	Antiproliferative activity against human Ishikawa cells assessed as reduction in cell viability Antiproliferative activity against human Ishikawa cells assessed as reduction in cell viability	[PMID: 38911148]
L6	IC₅₀	150 nM Compound: simvastatin	Inhibition of cholesterol synthesis in rat L6 myocyte Inhibition of cholesterol synthesis in rat L6 myocyte	[PMID: 18155906]
L6	IC₅₀	229 nM Compound: sim, simvastatin	Inhibition of cholesterol synthesis in rat L6 cells after 3 hrs Inhibition of cholesterol synthesis in rat L6 cells after 3 hrs	[PMID: 17560788]
L6	IC₅₀	27 nM Compound: simvastatin	Inhibition of cholesterol synthesis in rat L6 cells assessed as incorporation of [14C]acetate into cholesterol Inhibition of cholesterol synthesis in rat L6 cells assessed as incorporation of [14C]acetate into cholesterol	[PMID: 18412317]
MDCK	IC₅₀	10 μM Compound: Simvastatin lactone	TP_TRANSPORTER: inhibition of calcein-AM efflux in MDR1-expressing MDCK cells TP_TRANSPORTER: inhibition of calcein-AM efflux in MDR1-expressing MDCK cells	[PMID: 15616150]
MDCK	IC₅₀	25 μM Compound: Simvastatin lactone	TP_TRANSPORTER: inhibition of calcein-AM efflux in MRP2-expressing MDCK cells TP_TRANSPORTER: inhibition of calcein-AM efflux in MRP2-expressing MDCK cells	[PMID: 15616150]
MEF	IC₅₀	36.7 μM Compound: 11	Cytotoxicity against mouse MEF cells after 72 hrs by MTT assay Cytotoxicity against mouse MEF cells after 72 hrs by MTT assay	[PMID: 23570542]
NIH-3T3-G185	IC₅₀	26.1 μM Compound: Simvastatin	TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	56.8 μM Compound: Simvastatin	TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
Ventricular myocyte	IC₅₀	150 nM Compound: Simvastatin	Inhibition of cholesterol synthesis in rat myocyte Inhibition of cholesterol synthesis in rat myocyte	[PMID: 17574412]

In Vitro

Simvastatin is an inactive drug precursor that has no drug activity itself and must be metabolized into its hydroxy acid form in the liver to function. In vitro experiments, it can be activated by sodium hydroxide (NaOH).

1. Dissolve 2 mg of Simvastatin in 50 μL of 100% ethanol (clear solution);
2. Add 75 μL of 0.1 N NaOH to the above solution and heat at 50 °C (clear solution);
3. Adjust the pH to 7.2 with HCl, then add water to make it 250 μL (clear solution).
Simvastatin suppresses cholesterol synthesis in mouse L-M cell, rat H4II E cell, and human Hep G2 cell with IC₅₀s of 19.3 nM, 13.3 nM and 15.6 nM, respectively^[1].
Simvastatin causes a dose-dependent increase in serine 473 phosphorylation of Akt within 30 minutes, with maximal phosphorylation occurring at 1.0 μM^[2].
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 shows anti-in ammatory effects, reduces anti-CD3/anti-CD28 antibody-stimulated proliferation of PB-derived mononuclear cells and synovial uid cells from rheumatoid arthritis blood, as well as IFN-γ release at 10 μM^[3].
Simvastatin (10 μM) also blocks cell-mediated macrophage TNF-γ release induced via cognate interactions by appr 30%^[3].
Simvastatin (5 μM) significantly reduces the expression of ABCA1 in astrocytes and neuroblastoma cells, the expression of apolipoprotein E in astrocytes, and increases cyclin-dependent kinase 5 and glycogen synthase kinase 3β expression in SK-N-SH cells^[7].
Simvastatin has the ability to inhibit exosome release^[10].
Simvastatin (32 and 64 μM; 24, 48, and 72 h) inhibits tumor cell growth, arrests in the G0/G1 phase^[11].
Simvastatin (32 and 64 μM; 48 h) induces apoptosis in HepG2 and Huh7 cells^[11].

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

Cell Proliferation Assay^[11]

Cell Line:

HepG2 and Huh7 cells
Concentration:

32 and 64 μM
Incubation Time:

24, 48, and 72 hours
Result:

Inhibited tumor cell growth as compared to controls (ctrl, p<0.05).

Apoptosis Analysis^[11]

Cell Line:

HepG2 and Huh7 cells
Concentration:

32 and 64 μM
Incubation Time:

48 hours
Result:

Increased early apoptosis from 9.2% in non-treated ctrl cells to 18.2% (32 μM) and 19.8% (64 μM), respectively, increased late apoptosis from 35.0% in ctrl cells to 56.9% (32 μM) and 48.0% (64 μM), respectively, in HepG2 cells.

Cell Cycle Analysis^[11]

Cell Line:

HepG2 and Huh7 cells
Concentration:

32 and 64 μM
Incubation Time:

24, 48, and 72 hours
Result:

Exhibited downregulation of CDK1, CDK2, CDK4 and cyclins D1 and E as compared to ctrl tumor cells.

In Vivo

Simvastatin suppresses the conversion of radiolabeled acetate to cholesterol with an IC₅₀ of 0.2 mg/kg via p.o. administration^[1]. Simvastatin (4 mg/day, p.o. for 13 weeks) returns the cholesterol-induced increases in total cholesterol, LDL-cholesterol and HDL-cholesterol to normal level in rabbits fed an atherogenci cholesterol-rich diet^[4].
Simvastatin (6 mg/kg) increases LDL receptor-dependent binding and the number of hepatic LDL receptors in rabbits fed a diet containing 0.25% cholesterol^[5].
Simvastatin (20 mg/kg/day) causes 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 in cynomolgus monkeys fed an atherogenic diet^[6].
Simvastatin (oral gavage; 15 and 30 mg/kg; once daily; 14 d) treatment attenuats oxidative damage, TNF-a and IL-6 levels, and restores itochondrial enzyme complex activities^[12].

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

Animal Model:

Male wistar rats with oxidative damage by Intrastriatal 6-OHDA administration^[12]
Dosage:

15 and 30 mg/kg
Administration:

Oral gavage; 15 and 30 mg/kg; once daily; 14 days
Result:

Attenuated oxidative damage (reduced MDA, nitrite levels and restoration of reduced GSH) , attenuated TNF-a and IL-6 levels, and restored itochondrial enzyme complex activities as compared to 6-OHDA group.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 79902-63-9
Appearance Solid
Masse moléculaire 418.57
Formule C₂₅H₃₈O₅
Color White to off-white
SMILES

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

MK 733
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (83)

All In Vivo Efficacy StudyWBCell Proliferation/Viability Assay

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Journal Impact Factor

Nature

A metabolic alarmin from keratinocytes potentiates systemic humoral immunity. [Abstract]

2026 Apr;652(8108):209-219. PMID: 41781621
Cancer Commun (Lond)

Lipid metabolism reprograming by SREBP1-PCSK9 targeting sensitizes pancreatic cancer to immunochemotherapy. [Abstract]

2025 Aug;45(8):1010-1037. PMID: 40439109

Simvastatin purchased from MedChemExpress. Usage Cited in: Cancer Commun (Lond). 2025 Aug;45(8):1010-1037. [Abstract]

Denifanstat (10 mg/kg; i.g.; every day; from day7 to day20); Lovastatin(10 mg/kg; i.g.; every day; from day7 to day20); Simvastatin (50 mg/kg; i.g.; every day; from day7 to day20). Tumor growth curve of each group (4 mice/group). ns, not significant; * P < 0.05, **P < 0.01, ***P < 0.001.
Blood

Oncogenic role of the SOX9-DHCR24-cholesterol biosynthesis axis in IGH-BCL2+ diffuse large B-cell lymphomas. [Abstract]

2022 Jan 6;139(1):73-86. PMID: 34624089
Cancer Res

USP20-Driven Cholesterol Metabolism Links Inflammatory Signaling to Malignancy and Stromal Co-evolution in Pancreatic Cancer. [Abstract]

2025 Nov 6. PMID: 41196022
Nat Commun

TNF inhibitors target a mevalonate metabolite/TRPM2/calcium signaling axis in neutrophils to dampen vasculitis in Behçet's disease. [Abstract]

2024 Oct 26;15(1):9261. PMID: 39461948
Adv Sci (Weinh)

Cancer Cell-Intrinsic Cholesterol Induces Lipid-Associated Macrophage Differentiation via SP1 Palmitoylation to Promote Prostate Cancer Progression. [Abstract]

2026 Apr;13(19):e08588. PMID: 41603134
Adv Sci (Weinh)

Short-Term Statin Therapy Induces Hepatic Insulin Resistance Through HNF4α/PAQR9/PPM1α Axis Regulated AKT Phosphorylation. [Abstract]

2024 Jul 5:e2403451. PMID: 38970167
Exp Hematol Oncol

Chiglitazar diminishes the warburg effect through PPARγ/mTOR/PKM2 and increases the sensitivity of imatinib in chronic myeloid leukemia. [Abstract]

2024 Dec 18;13(1):121. PMID: 39696470
Chem Eng J

478, 15 December 2023, 147465
Chem Eng J

2022: 141111.
Biomaterials

A self-driven bioinspired nanovehicle by leukocyte membrane-hitchhiking for early detection and treatment of atherosclerosis. [Abstract]

2020 Aug;250:119963. PMID: 32334199
Sci Adv

Clonal cooperation through soluble metabolite exchange facilitates metastatic outgrowth by modulating Allee effect. [Abstract]

2023 Sep 15;9(37):eadh4184. PMID: 37713487
Sci Adv

Regulation of PD-L1 through direct binding of cholesterol to CRAC motifs. [Abstract]

2022 Aug 26;8(34):eabq4722. PMID: 36026448
J Control Release

Formulation of simvastatin within high density lipoprotein enables potent tumour radiosensitisation. [Abstract]

2022 Apr 21;346:98-109. PMID: 35447296
J Exp Med

The STING pathway drives noninflammatory neurodegeneration in NGLY1 deficiency. [Abstract]

2025 Oct 6;222(10):e20242296. PMID: 40644312
J Exp Med

ASC deglutathionylation is a checkpoint for NLRP3 inflammasome activation. [Abstract]

2021 Sep 6;218(9):e20202637. PMID: 34342641
Pharmacol Res

High expression of RUNX1 in colorectal cancer subtype accelerates malignancy by inhibiting HMGCR. [Abstract]

2024 Jul 4:107293. PMID: 38971271
Clin Cancer Res

CDK9 inhibition by dinaciclib is a therapeutic vulnerability in epithelioid hemangioendothelioma. [Abstract]

2024 Sep 13;30(18):4179-4189. PMID: 39052240
Clin Cancer Res

Gene Expression Signatures Identify Novel Therapeutics for Metastatic Pancreatic Neuroendocrine Tumors. [Abstract]

2020 Apr 15;26(8):2011-2021. PMID: 31937620
Cancer Lett

Myeloid-derived suppressor cells deficient in cholesterol biosynthesis promote tumor immune evasion. [Abstract]

2023 Jun 28:564:216208. PMID: 37150500
Cell Death Dis

VIRMA/IGF2BP3-mediated ANLN upregulation promotes intrahepatic cholangiocarcinoma growth by forming a positive feedback loop with RhoA/YAP1/TEAD1 signaling pathway. [Abstract]

2026 Jan 9;17(1):20. PMID: 41513610
Cell Death Dis

Combined metformin and simvastatin therapy inhibits SREBP2 maturation and alters energy metabolism in glioma. [Abstract]

2024 Nov 9;15(11):809. PMID: 39521788
Sci China Life Sci

NPC1-regulated dynamic of clathrin-coated pits is essential for viral entry. [Abstract]

2022 Feb;65(2):341-361. PMID: 34047913
Int J Biol Macromol

Integrative analysis using machine learning and RNA sequencing identifies TGFBI as a therapeutic target in HIV-associated osteonecrosis of the femoral head. [Abstract]

2025 Jun 27:145620. PMID: 40582670
Phytomedicine

Sparstolonin B and Curcumin alleviate atherogenesis by modulating T helper 17-stromal cell interactions associated with interleukin-17 receptor A (IL-17RA) - transforming growth factor-β-activated kinase 1 (TAK1) - nuclear factor-kappa B (NF-κB) signaling. [Abstract]

2025 Dec:149:157578. PMID: 41308385
Phytomedicine

Citri Reticulatae Pericarpium-Reynoutria japonica Houtt. herb pair suppresses breast cancer liver metastasis by targeting ECM1-mediated cholesterol biosynthesis pathway. [Abstract]

2023 Jul 25:116:154896. PMID: 37247588
Free Radic Biol Med

GSH exhaustion via inhibition of xCT-GSH-GPX4 pathway synergistically enhanced DSF/Cu-induced cuproptosis in myelodysplastic syndromes. [Abstract]

2024 Jun 10:S0891-5849(24)00521-5. PMID: 38866192
Chemosphere

Toxicogenomic assessment of hydroxylated metabolites of PBDEs on cetaceans: An in vitro study. [Abstract]

2024 Oct:366:143350. PMID: 39326706
Food Res Int

Encapsulation of oleanolic acid into cyclodextrin metal-organic frameworks by co-crystallization: Preparation, structure characterization and its effect on a zebrafish larva NAFLD model. [Abstract]

2025 Mar:204:115936. PMID: 39986782
Sci Total Environ

Cellular internalization and release of polystyrene microplastics and nanoplastics. [Abstract]

2021 Jul 20:779:146523. PMID: 34030247
Biomed Pharmacother

Fangchinoline suppresses melanoma metastasis by inducing senescence of circulating tumor cells. [Abstract]

2025 Nov 14:193:118770. PMID: 41242135
J Transl Med

Cholesterol overload in macrophages drives metabolic dysfunction-associated steatohepatitis via inhibiting 7-dehydrocholesterol reductase in mice. [Abstract]

2024 Nov 29;22(1):1085. PMID: 39614331
Biomed Pharmacother

Overcoming PLK1 inhibitor resistance by targeting mevalonate pathway to impair AXL-TWIST axis in colorectal cancer. [Abstract]

2021 Dec:144:112347. PMID: 34700228
Cell Rep

Mechanotransduction in response to ECM stiffening impairs cGAS immune signaling in tumor cells. [Abstract]

2023 Oct 5;42(10):113213. PMID: 37804510
Cell Biosci

Cholesterol confers resistance to Apatinib-mediated ferroptosis in gastric cancer. [Abstract]

2025 Jul 4;15(1):95. PMID: 40615893
Cancer Cell Int

Taurochenodeoxycholic acid suppresses the progression of glioblastoma via HMGCS1/HMGCR/GPX4 signaling pathway in vitro and in vivo. [Abstract]

2025 Apr 22;25(1):160. PMID: 40264142
Int J Mol Med

Simvastatin inhibits the adipogenesis of bone marrow‑derived mesenchymal stem cells through the downregulation of chemerin/CMKLR1 signaling. [Abstract]

2020 Aug;46(2):751-761. PMID: 32468037
Chin Med

Explore the potential mechanism of Huachansu injection against osteosarcoma via metabolomics, network pharmacology and bioinformatics. [Abstract]

2025 Aug 5;20(1):120. PMID: 40764575
Biochem Pharmacol

Insight into the structure, function and the tumor suppression effect of gasdermin E. [Abstract]

2024 Jun 7:116348. PMID: 38852642
Clin Pharmacol Ther

Advancing Predictions of Oral Drug Absorption, CYP3A4 Induction, and Transporter-Mediated Interactions Using a Human Primary Intestinal 3D Model (EpiIntestinal™). [Abstract]

2025 Jul 14. PMID: 40657937
Pharmaceutics

Drug-Induced Reorganisation of Lipid Metabolism Limits the Therapeutic Efficacy of Ponatinib in Glioma Stem Cells. [Abstract]

2024 May 29;16(6):728. PMID: 38931850
Cells

Lipophilic Statins Eliminate Senescent Endothelial Cells by inducing Anoikis-Related Cell Death. [Abstract]

2023 Dec 14;12(24):2836. PMID: 38132158
Cells

Statins Modulate Microenvironmental Cues Driving Macrophage Polarization in Simulated Periodontal Inflammation. [Abstract]

2023 Jul 29;12(15):1961. PMID: 37566040
Stem Cell Reports

Cholinergic neuron-to-glioblastoma synapses in a human iPSC-derived co-culture model. [Abstract]

2025 Jun 4:102534. PMID: 40541171
Commun Biol

Mevalonate pathway inhibition reduces bladder cancer metastasis by modulating RhoB protein stability and integrin β1 localization. [Abstract]

2024 Nov 9;7(1):1476. PMID: 39521858
Life Sci

Cordycepin reprogramming lipid metabolism to block metastasis and EMT via ERO1A/mTOR/SREBP1 axis in cholangiocarcinoma. [Abstract]

2023 Aug 15:327:121698. PMID: 37080351
Inflammation

Simvastatin Alleviates ConA-Induced Autoimmune Hepatitis by Inhibiting CD4+ T Cell Activation via Calcium-NFATC3 Pathway. [Abstract]

2026 Jan 30;49(1):72. PMID: 41618046
Front Bioeng Biotechnol

Application of 3D Hepatic Plate-Like Liver Model for Statin-Induced Hepatotoxicity Evaluation. [Abstract]

2022 Mar 17;10:826093. PMID: 35372314
Eur J Pharmacol

Simvastatin potentiates the cell-killing activity of imatinib in imatinib-resistant chronic myeloid leukemia cells mainly through PI3K/AKT pathway attenuation and Myc downregulation. [Abstract]

2021 Dec 15:913:174633. PMID: 34843676
J Dairy Sci

Regulation of cholesterol metabolism during high fatty acid-induced lipid deposition in calf hepatocytes. [Abstract]

2023 Aug;106(8):5835-5852. PMID: 37419743
Cancers (Basel)

Antitumor Activity of Simvastatin in Preclinical Models of Mantle Cell Lymphoma. [Abstract]

2022 Nov 15;14(22):5601. PMID: 36428695

Simvastatin purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2022 Nov 15;14(22):5601. [Abstract]

Simvastatin (0-40 µM; 48 h) inhibits growth of REC-1 and Z-138 cells with IC₅₀ values of 4.97 µM and 3.78 µM, respectively.
FASEB J

Simvastatin Targets PKM2 to Alter Metabolic Reprogramming in Hepatic Stellate Cells and Mitigate Liver Fibrosis. [Abstract]

2026 Feb 28;40(4):e71500. PMID: 41718472
J Biol Chem

Inhibition of cholesterol biosynthesis overcomes enzalutamide resistance in castration-resistant prostate cancer (CRPC). [Abstract]

2018 Sep 14;293(37):14328-14341. PMID: 30089652

Simvastatin purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2018 Sep 14;293(37):14328-14341. [Abstract]

C4-2R cells are treated with Simvastatin, MDV3100 or combination of the two drugs at the indicated concentrations for 48 hours, followed by Immunoblotting (IB) against cleaved PARP.
Brain Res Bull

Delayed simvastatin treatment improves neurological recovery after cryogenic traumatic brain injury through downregulation of ELOVL1 by inhibiting mTOR signaling. [Abstract]

2024 Sep 5:111072. PMID: 39243948
Med Oncol

Enhanced LDL uptake and PPARα signaling support OSCC cell survival under glutamine deprivation. [Abstract]

2025 Jul 14;42(8):332. PMID: 40660028
Exp Cell Res

A new mechanism in steroid-induced osteonecrosis of the femoral head and the protective role of simvastatin. [Abstract]

2025 Mar 1;446(1):114471. PMID: 39978720
Cell Cycle

Cholesterol depletion sensitizes gallbladder cancer to cisplatin by impairing DNA damage response. [Abstract]

2019 Dec;18(23):3337-3350. PMID: 31599189
Front Oncol

Synergistic Effect of Statins and Abiraterone Acetate on the Growth Inhibition of Neuroblastoma via Targeting Androgen Receptor. [Abstract]

2021 May 10:11:595285. PMID: 34041015
Naunyn Schmiedebergs Arch Pharmacol

Anti-adipogenesis and anti-obesity potential of alliin mediated by modulating glycolipid metabolism via activating PPARγ signaling. [Abstract]

2024 Nov;397(11):8707-8723. PMID: 38829385
Mol Immunol

Liposome-mediated simvastatin in vaccine adjuvants: Its application and mechanism. [Abstract]

2026 Feb:190:72-85. PMID: 41539277
J Chromatogr B Analyt Technol Biomed Life Sci

Integrated HPLC, pharmacodynamics, and immunoprofiling to explore active components and mechanism of Zhi Bai Heye Fang on glycolipid metabolic disorders in mice. [Abstract]

2024 Dec 28:1252:124446. PMID: 39754817
J Orthop Surg Res

Circ-STC2 promotes the ferroptosis of nucleus pulposus cells via targeting miR-486-3p/TFR2 axis. [Abstract]

2023 Jul 21;18(1):518. PMID: 37480032
Animals (Basel)

Simvastatin Improves the High-Fat-Diet-Induced Metabolic Disorder in Juvenile Chinese Giant Salamander (Andrias davidianus) Through Inhibiting Endoplasmic Reticulum Stress and Enhancing Mitochondrial Function. [Abstract]

2026 Jan 2;16(1):134. PMID: 41514821
Immun Inflamm Dis

Fluvastatin Promotes Treg Cell Production in Allogeneic Immune Reaction and Suppresses Inflammatory Response. [Abstract]

2025 Feb;13(2):e70165. PMID: 40007079
Clin Res Hepatol Gastroenterol

Simvastatin ameliorates total liver ischemia/reperfusion injury via KLF2-mediated mechanism in rats. [Abstract]

2019 Apr;43(2):171-178. PMID: 30274910

Simvastatin purchased from MedChemExpress. Usage Cited in: Clin Res Hepatol Gastroenterol. 2019 Apr;43(2):171-178. [Abstract]

Simvastatin pretreatment maintains the expression of KLF2 and its protective target genes (eNOS and TM). Westernblot analysis of KLF2, phosphorylation eNOS and total eNOS in liver tissue. β-actin is normalized as the loading control.
FEBS Open Bio

Cholesterol-regulated cellular stiffness may enhance evasion of NK cell-mediated cytotoxicity in gastric cancer stem cells. [Abstract]

2024 May;14(5):855-866. PMID: 38494433
Biochem Biophys Rep

Co-loaded simvastatin-ginsenoside Rh2 liposomes enhance cellular immune responses as vaccine adjuvants. [Abstract]

2025 Jul 15:43:102159. PMID: 40697522
Biochem Biophys Res Commun

Combinatorial screening of a panel of FDA-approved drugs identifies several candidates with anti-Ebola activities. [Abstract]

2020 Feb 19;522(4):862-868. PMID: 31806372
Drugs R D

Simvastatin Preferentially Targets FLT3/ITD Acute Myeloid Leukemia by Inhibiting MEK/ERK and p38-MAPK Signaling Pathways. [Abstract]

2023 Dec;23(4):439-451. PMID: 37847357
Res Sq

2026 Apr 21.
eGastroenterology

Phosphoinositide kinase PIKfyve inhibitor apilimod blocks hepatitis E virus infection. [Abstract]

2026 Mar 31;4(1):e100348. PMID: 41948149
bioRxiv

2026 Feb 20.
SSRN

2025 Dec 2.
SSRN

2025 Apr 29.
Patent

US20250025542A1.
Uppsala University

2024 Jul 12.
Patent

US20230145200A1.
Dis Markers

Simvastatin Improves Myocardial Ischemia Reperfusion Injury through KLF-Regulated Alleviation of Inflammation. [Abstract]

2022 Jan 11:2022:7878602. PMID: 35059045
University of New Hampshire

2021 Oct.
Research Square Preprint

2020 Sep.
Evid Based Complement Alternat Med

Combination of Astragalus membranaceous and Angelica sinensis Ameliorates Vascular Endothelial Cell Dysfunction by Inhibiting Oxidative Stress. [Abstract]

2020 Sep 18;2020:6031782. PMID: 33293989
Oncotarget

Exosomes impact survival to radiation exposure in cell line models of nervous system cancer. [Abstract]

2018 Nov 16;9(90):36083-36101. PMID: 30546829
Oxid Med Cell Longev

Pretreatment Donors after Circulatory Death with Simvastatin Alleviates Liver Ischemia Reperfusion Injury through a KLF2-Dependent Mechanism in Rat. [Abstract]

2017:2017:3861914. PMID: 29348789

Simvastatin purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2017:2017:3861914. [Abstract]

Simvastatin pretreatment maintains the expression of KLF2 and its protective target genes

Solvant et solubilité

In Vitro:

Ethanol : 100 mg/mL (238.91 mM; Need ultrasonic)

DMSO : ≥ 50 mg/mL (119.45 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3891 mL

11.9454 mL

23.8909 mL

5 mM

0.4778 mL

2.3891 mL

4.7782 mL

10 mM

0.2389 mL

1.1945 mL

2.3891 mL

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. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 (5.97 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.

Protocol 2

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

Solubility: 2.5 mg/mL (5.97 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

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

Solubility: ≥ 2.5 mg/mL (5.97 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 EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 5

Add each solvent one by one: 10% EtOH 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.97 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 50% PEG300 50% Saline

Solubility: 10 mg/mL (23.89 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (290 KB)
SDS (537 KB)
- English - EN (537 KB)
- Français - FR (537 KB)
- Deutsch - DE (537 KB)
- Norwegian - NO (537 KB)
- Español - ES (537 KB)
- Swedish - SV (537 KB)
- Italian - IT (537 KB)
- Portuguese - PT (537 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Slater, E.E., et al. Mechanism of action and biological profile of HMG CoA reductase inhibitors. A new therapeutic alternative. Drugs, 1988. 36 Suppl 3: p. 72-82. [Content Brief]

[2]. Kureishi, Y., et al. The HMG-CoA reductase inhibitor simvastatin activates the protein kinase Akt and promotes angiogenesis in normocholesterolemic animals. Nat Med, 2000. 6(9): p. 1004-10. [Content Brief]

[3]. Leung BP, et al. A novel anti-inflammatory role for simvastatin in inflammatory arthritis. J Immunol. 2003 Feb 1;170(3):1524-30. [Content Brief]

[4]. Kobayashi M, et al. Preventive effect of MK-733 (simvastatin), an inhibitor of HMG-CoA reductase, on hypercholesterolemia and atherosclerosis induced by cholesterol feeding in rabbits. Jpn J Pharmacol. 1989 Jan;49(1):125-33. [Content Brief]

[5]. Ishida F, et al. Comparative effects of simvastatin (MK-733) and CS-514 on hypercholesterolemia induced by cholesterol feeding in rabbits. Biochim Biophys Acta. 1990 Feb 23;1042(3):365-73. [Content Brief]

[6]. Sukhova GK, et al. Statins reduce inflammation in atheroma of nonhuman primates independent of effects on serum cholesterol. Arterioscler Thromb Vasc Biol. 2002 Sep 1;22(9):1452-8. [Content Brief]

[7]. Weijiang Dong, et al. Differential effects of simvastatin and CS-514 on expression of Alzheimer’s disease-related genes in human astrocytes and neuronal cells. J Lipid Res. 2009 Oct; 50(10): 2095-2102.

[8]. Liu Z, et al. Pretreatment Donors after Circulatory Death with Simvastatin Alleviates Liver Ischemia Reperfusion Injury through a KLF2-Dependent Mechanism in Rat. Oxid Med Cell Longev. 2017;2017:3861914. [Content Brief]

[9]. Ifergan I, et al. Statins reduce human blood-brain barrier permeability and restrict leukocyte migration: relevance to multiple sclerosis. Ann Neurol. 2006 Jul;60(1):45-55. [Content Brief]

[10]. Zhang H, et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020;35(1):1322-1330. [Content Brief]

[11]. Borna Relja, et al. Simvastatin inhibits cell growth and induces apoptosis and G0/G1 cell cycle arrest in hepatic cancer cells. Int J Mol Med. 2010 Nov;26(5):735-41. [Content Brief]

[12]. Anil Kumar, et al. Neuroprotective potential of atorvastatin and simvastatin (HMG-CoA reductase inhibitors) against 6-hydroxydopamine (6-OHDA) induced Parkinson-like symptoms. Brain Res. 2012 Aug 30;1471:13-22. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. 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 / Ethanol	1 mM	2.3891 mL	11.9454 mL	23.8909 mL	59.7272 mL
	5 mM	0.4778 mL	2.3891 mL	4.7782 mL	11.9454 mL
	10 mM	0.2389 mL	1.1945 mL	2.3891 mL	5.9727 mL
	15 mM	0.1593 mL	0.7964 mL	1.5927 mL	3.9818 mL
	20 mM	0.1195 mL	0.5973 mL	1.1945 mL	2.9864 mL
	25 mM	0.0956 mL	0.4778 mL	0.9556 mL	2.3891 mL
	30 mM	0.0796 mL	0.3982 mL	0.7964 mL	1.9909 mL
	40 mM	0.0597 mL	0.2986 mL	0.5973 mL	1.4932 mL
	50 mM	0.0478 mL	0.2389 mL	0.4778 mL	1.1945 mL
	60 mM	0.0398 mL	0.1991 mL	0.3982 mL	0.9955 mL
	80 mM	0.0299 mL	0.1493 mL	0.2986 mL	0.7466 mL
	100 mM	0.0239 mL	0.1195 mL	0.2389 mL	0.5973 mL

Keywords

Simvastatin

83 Cited Publications

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Simvastatin

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

Publications Citing Use of MedChemExpress (MCE) Simvastatin

Activité biologique

Chemical Information

Publications (83)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Simvastatin

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

Publications Citing Use of MedChemExpress (MCE) Simvastatin

Activité biologique

Chemical Information

Publications (83)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Simvastatin Related Classifications

Cat. No.: HY-17502