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Cerivastatin

Name: Cerivastatin
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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 No.: 145599-86-6
Formule: C₂₆H₃₄FNO₅
Masse moléculaire:459.55

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

Data Sheet (274 KB)

Cerivastatin Chemical Structure

CAS No.: 145599-86-6

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

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
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Activité biologique

Description

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.

Cell Proliferation Assay^[1]

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]

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]

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]

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.

Related Protocols :

Cell Viability Determination by MTT Colorimetric Assay

Chemical Information

CAS No. 145599-86-6
Masse moléculaire 459.55
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (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)
Instruction de manipulation (2659 KB)

Références

[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

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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.

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Cerivastatin

2 Cited Publications

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Cerivastatin

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