Cerivastatin sodium Chemical Properties

Melting point:

197-199°C

alpha 

D20 +24.1° (c = 1 in ethanol)

storage temp. 

Hygroscopic, Store under Inert atmosphere -20°C Freezer

solubility 

H2O: ≥5mg/mL

form 

powder

color 

white to tan

optical activity

[α]/D +18 to +26° in ethanol

Stability:

Hygroscopic

CAS DataBase Reference

143201-11-0(CAS DataBase Reference)

Safety Information

WGK Germany 

3

Cerivastatin sodium Usage And Synthesis

Description

Lipobay was launched in Denmark, Germany and the UK for treatment of primary hypercholesteremia types Ⅱa and Ⅱb. It is available through a nine step synthesis beginning with the Hantsch reaction of ethyl 3-amino-4-methylpent-2-enoate and 4-(ethoxycarbonyl)-5-(4-fluorophenyl)-2-methylpent-4-en-3-one. Lipobay acts as an HMG-CoA reductase inhibitor showing a high liver selectivity (50 fold). In vitro Lipobay had a higher affinity (110x) for the enzyme than does Lovastatin, Simvastatin and pravastatin which resulted in a lower ED₅₀, in vivo compared to Lovastatin. Three metabolites generated by the CYP3A4 enzyme system were equal to the parent in activity. Lipobay was as effective as Gemfibrozil in type lib hypercholesteremia and had no age or gender effects. It decreased plasma levels of VLDL and LDL cholesterol by a mechanism similar to other HMG-CoA reductase inhibitors. The (-)- antipode is completely inactive indicating a high stereospecificity by the enzyme. It is therapeutically useful at ultra-low doses which may minimize any drug-drug interactions.

Chemical Properties

Solid

Originator

Bayer (Germany)

Uses

Cerivastatin is a competitive inhibitor of HMG-CoA reductase.

Uses

Cerivastatin sodium salt hydrate has been used as a supplement in cell culture.

Definition

ChEBI: The sodium salt of cerivastatin. Formerly used to lower cholesterol and prevent cardiovascular disease, it was withdrawn from the market worldwide in 2001 following reports of a severe form of muscle toxicity.

brand name

Baycol (Bayer).

General Description

Cerivastatin sodium salt hydrate belongs to the statin class of lipid lowering agents. It helps in decreasing MAP kinase activation, blocking AP-1 (activator protein-1) and NF-kB (nuclear factor-kB ) binding activity, inhibiting inflammatory responses and ameliorated renal damage. It also lowers cholesterol. It is metabolized by cytochrome P450 (CYP)3A4 and (CYP)2C8. Cerivastatin sodium salt hydrate is linked to rhabdomyolysis.

Hazard

A poison by ingestion.

Biochem/physiol Actions

Cerivastatin sodium is an HMG-CoA reductase inhibitor. HMG-CoA is a key enzyme in the production of cholesterol.

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