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Cerivastatin

Name: Cerivastatin
Brand: MedChemExpress
SKU: HY-129458
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2 Cited Publications

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Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect.

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CAS. Nr.: 145599-86-6
Formel: C₂₆H₃₄FNO₅
Molecular Weight:459.55

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (274 KB)

Cerivastatin Chemical Structure

CAS. Nr.: 145599-86-6

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Protokoll (1)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Ki: 1.3 nM/L (HMG-CoA reductase)^[1]^[2]^[3]

Cellular Effect

Cell Line	Type	Value	Description	References
Hepatocyte	IC₅₀	1.7 nM Compound: cer, cerivastatin	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	1.7 nM Compound: cerivastatin	Inhibition of cholesterol synthesis in rat hepatocytes Inhibition of cholesterol synthesis in rat hepatocytes	[PMID: 18072721]
Hepatocyte	IC₅₀	1.7 nM Compound: cerivastatin	Inhibition of cholesterol synthesis in rat hepatocyte Inhibition of cholesterol synthesis in rat hepatocyte	[PMID: 18155906]
Hepatocyte	IC₅₀	2.3 nM Compound: cerivastatin	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	0.13 μM Compound: Cerivastatin	Cytotoxicity against human HepG2 cells assessed as reduction in nuclear size after 72 hrs by fluorescent image analysis Cytotoxicity against human HepG2 cells assessed as reduction in nuclear size after 72 hrs by fluorescent image analysis	[PMID: 27105029]
HepG2	IC₅₀	0.34 μM Compound: Cerivastatin	Cytotoxicity against human HepG2 cells assessed as increase in intracellular free calcium level after 72 hrs by fluorescent image analysis Cytotoxicity against human HepG2 cells assessed as increase in intracellular free calcium level after 72 hrs by fluorescent image analysis	[PMID: 27105029]
HepG2	IC₅₀	0.6 μM Compound: Cerivastatin	Cytotoxicity against human HepG2 cells assessed as reduction in mitochondrial membrane potential after 72 hrs by fluorescent image analysis Cytotoxicity against human HepG2 cells assessed as reduction in mitochondrial membrane potential after 72 hrs by fluorescent image analysis	[PMID: 27105029]
HepG2	IC₅₀	0.8 μM Compound: Cerivastatin	Cytotoxicity against human HepG2 cells assessed as increase in membrane permeability after 72 hrs by fluorescent image analysis Cytotoxicity against human HepG2 cells assessed as increase in membrane permeability after 72 hrs by fluorescent image analysis	[PMID: 27105029]
HepG2	IC₅₀	0.96 μM Compound: Cerivastatin	Cytotoxicity against human HepG2 cells assessed as reduction in cell number after 72 hrs by fluorescent image analysis Cytotoxicity against human HepG2 cells assessed as reduction in cell number after 72 hrs by fluorescent image analysis	[PMID: 27105029]
L6	IC₅₀	1.7 nM Compound: cerivastatin	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]
L6	IC₅₀	3 nM Compound: cerivastatin	Inhibition of cholesterol synthesis in rat L6 cells Inhibition of cholesterol synthesis in rat L6 cells	[PMID: 18072721]
L6	IC₅₀	7 nM Compound: cer, cerivastatin	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	7 nM Compound: cerivastatin	Inhibition of cholesterol synthesis in rat L6 myocyte Inhibition of cholesterol synthesis in rat L6 myocyte	[PMID: 18155906]

In Vitro

Cerivastatin (5-50 ng/mL; 3 days; MDA-MB-231 cells) treatment induces a dose-dependent decrease in cell proliferation of MDA-MB-231 cells (up to 40% inhibition at 25 ng/mL)^[1].
Cerivastatin (25 ng/mL; 18-36 hours; MDA-MB-231 cells) treatment induces an arrest of the cell cycle in G 1/S phase after 36 h treatment. This arrest is not observed for a shorter incubation time (18 h)^[1].
Cerivastatin (25 ng/mL; 18 hours; MDA-MB-231 cells) treatment induces a marked increase in the level of p21^Waf1/Cip1^[1].
Cerivastatin (25 ng/mL; 12 hours; MDA-MB-231 cells) treatment increases the p21 transcript in MDA-MB-231 cells^[1].
Cerivastatin (10-25 ng/mL; 18 hours) inhibits invasion of MDA-MB-231 cells through Matrigel^[1].
Cerivastatin (25 ng/mL; 18-36 hours) delocalizes RhoA and Ras from the membrane to the cytosol and induces morphological changes^[1].
Cerivastatin (25 ng/mL; 4-36 hours) induces inactivation of NFκB, in a RhoA inhibition-dependent manner, resulting in a decrease in urokinase and metalloproteinase-9 expression, and concomitantly increases IκB^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Cell Proliferation Assay^[1]

View Protocol

Cell Line:

MDA-MB-231 cells
Concentration:

5 ng/mL, 10 ng/mL, 25 ng/mL, 50 ng/mL
Incubation Time:

3 days
Result:

Induced a dose-dependent decrease in cell proliferation of MDA-MB-231 cells.

Cell Cycle Analysis^[1]

View Protocol

Cell Line:

MDA-MB-231 cells
Concentration:

25 ng/mL
Incubation Time:

18 hours, 36 hours
Result:

Induced a cell cycle block in G 1/S phase.

Western Blot Analysis^[1]

View Protocol

Cell Line:

MDA-MB-231 cells
Concentration:

25 ng/mL
Incubation Time:

18 hours
Result:

Induced a marked increase in the level of p21^Waf1/Cip1.

RT-PCR^[1]

View Protocol

Cell Line:

MDA-MB-231 cells
Concentration:

25 ng/mL
Incubation Time:

12 hours
Result:

Increased p21^Waf1/Cip1 mRNA levels.

In Vivo

Cerivastatin is well absorbed, reaching maximal plasma levels in 1-3 hours following oral dosing. In the circulation, Cerivastatin is highly bound to plasma proteins (99.5%), with an elimination half-life of 2-4 hours. Cerivastatin is metabolized predominantly in the liver to three polar metabolites. Two of these metabolites are active, but to a lesser extent compared to parent drug, and the third metabolite is inactive. Plasma concentrations of all metabolites are substantially lower than those of the parent drug. Elimination of metabolites is via the urine (20-25%) and feces (66-73%), while essentially no parent compound is excreted^[2].

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

Chemical Information

CAS. Nr. 145599-86-6
Molecular Weight 459.55
Formel C₂₆H₃₄FNO₅
SMILES

O=C(O)C[C@H](O)C[C@H](O)/C=C/C1=C(C2=CC=C(F)C=C2)C(COC)=C(C(C)C)N=C1C(C)C
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (2)

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Phytomedicine

Integrated identification and mechanism exploration of bioactive ingredients from Salvia miltiorrhiza to induce vascular normalization. [Abstract]

2025 Mar:138:156427. PMID: 39892310
bioRxiv

2024 October 04.

Protokoll

All Cell Biology

Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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)
Handling Instructions (2659 KB)

Verweise

[1]. Denoyelle C, et al. Cerivastatin, an inhibitor of HMG-CoA reductase, inhibits the signaling pathways involved in the invasiveness and metastatic properties of highly invasive breast cancer cell lines: an in vitro study. Carcinogenesis. 2001 Aug;22(8):1139 [Content Brief]

[2]. Stein E, et al. Cerivastatin, a New Potent Synthetic HMG Co-A Reductase Inhibitor: Effect of 0.2 mg Daily in Subjects With Primary Hypercholesterolemia. J Cardiovasc Pharmacol Ther. 1997 Jan;2(1):7-16. [Content Brief]

[3]. Furberg CD, et al. Withdrawal of cerivastatin from the world market. Curr Control Trials Cardiovasc Med. 2001;2(5):205-207. [Content Brief]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

Keywords

Cerivastatin

2 Cited Publications

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Cerivastatin

Publications Citing Use of MedChemExpress (MCE) Cerivastatin