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Cerivastatin

Catalog No. T14931 CAS 145599-86-6

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

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Cerivastatin, CAS 145599-86-6

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 2,120.00
50 mg	8-10 weeks	$ 2,780.00
100 mg	8-10 weeks	$ 3,700.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Description	Cerivastatin is a highly potent, well-tolerated, and orally active HMG-CoA reductase inhibitor (Ki: 1.3 nM/L). Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition with anti-cancer effect. Cerivastatin reduces low-density lipoprotein cholesterol levels.
Targets&IC50	HMG-CoA reductase:1.3 nM/L (Ki)
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). Cerivastatin (10-25 ng/mL; 18 hours) inhibits invasion of MDA-MB-231 cells through Matrigel. 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. Cerivastatin (25 ng/mL; 18-36 hours; MDA-MB-231 cells) treatment induces an arrest of the cell cycle in the G 1/S phase after 36 h treatment. Cerivastatin (25 ng/mL; 18-36 hours) delocalizes RhoA and Ras from the membrane to the cytosol and induces morphological changes. Cerivastatin (25 ng/mL; 18 hours; MDA-MB-231 cells) treatment induces a marked increase in the level of p21Waf1/Cip1. Cerivastatin (25 ng/mL; 12 hours; MDA-MB-231 cells) treatment increases the p21 transcript in MDA-MB-231 cells. This arrest is not observed for a shorter incubation time (18 h) [1].
In vivo	Cerivastatin is highly bound to plasma proteins (99.5%), with an elimination half-life of 2-4 hours. Cerivastatin is well absorbed, reaching maximal plasma levels in 1-3 hours following oral dosing. Cerivastatin is metabolized predominantly in the liver to three polar metabolites. 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].

Molecular Weight	459.55
Formula	C26H34FNO5
CAS No.	145599-86-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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):1139-48. 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. 3. Furberg CD, et al. Withdrawal of cerivastatin from the world market. Curr Control Trials Cardiovasc Med. 2001;2(5):205-207.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Cerivastatin 145599-86-6 Others inhibitor inhibit

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