Cerivastatin sodium
Synonym(s):(3R,5S,6E)-7-[4-(4-Fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl]-3,5-dihydroxy-6-heptenoic acid sodium salt hydrate;Rivastatin hydrate
- CAS NO.:143201-11-0
- Empirical Formula: C26H35FNNaO5
- Molecular Weight: 483.56
- MDL number: MFCD00865716
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-08 20:21:46
What is Cerivastatin sodium?
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)
The Uses of Cerivastatin sodium
Cerivastatin sodium salt hydrate has been used as a supplement in cell culture.
The Uses of Cerivastatin sodium
Cerivastatin is a competitive inhibitor of HMG-CoA reductase.
What are the applications of Application
Cerivastatin, Sodium Salt is A competitive inhibitor of HMG-CoA reductase
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 Formerly used to lower cholesterol and prevent cardiovascular disease, it was withdrawn from the market worldwide in 2001 following reports of a severe form of muscle toxicity.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.
Properties of Cerivastatin sodium
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 for Cerivastatin sodium
Computed Descriptors for Cerivastatin sodium
New Products
4-Aminotetrahydropyran-4-carbonitrile Hydrochloride (R)-3-Aminobutanenitrile Hydrochloride 4-AMINO-TETRAHYDRO-PYRAN-4-CARBOXYLIC ACID HCL 4-(Dimethylamino)tetrahydro-2H-pyran-4-carbonitrile 3-((Dimethylamino)methyl)-5-methylhexan-2-one oxalate 1,4-Dioxa-8-azaspiro[4.5]decane 5-Bromo-2-nitropyridine Nimesulide BP Aceclofenac IP/BP/EP Mefenamic Acid IP/BP/EP/USP Diclofenac Sodium IP/BP/EP/USP Ornidazole IP Diclofenac Potassium SODIUM AAS SOLUTION ZINC AAS SOLUTION BUFFER SOLUTION PH 10.0(BORATE) GOOCH CRUCIBLE SINTERED AQUANIL 5 BERYLLIUM AAS SOLUTION 2-Bromo-1-(bromomethyl)-3-chloro-5-nitrobenzene 2-Bromo-3-nitroaniline N-(3-Hydroxypropyl)-N-methylacetamide 3-Bromo-6-chloropyridazine 4-ethyl-3-nitrobenzoic acidRelated products of tetrahydrofuran
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