Chemical Property of Cerivastatin, sodium salt
Chemical Property:
- Appearance/Colour:Solid
- Vapor Pressure:1.37E-17mmHg at 25°C
- Melting Point:197-199 °C
- Boiling Point:646.3 °C at 760 mmHg
- Flash Point:344.7 °C
- PSA：99.88000
- LogP:4.88070
- Storage Temp.:Hygroscopic, Store under Inert atmosphere -20°C Freezer
- Solubility.:H2O: ≥5mg/mL
- Hydrogen Bond Donor Count:3
- Hydrogen Bond Acceptor Count:7
- Rotatable Bond Count:11
- Exact Mass:482.23187063
- Heavy Atom Count:34
- Complexity:620
- Purity/Quality:
-
97% *data from raw suppliers
CerivastatinSodiumSalt *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CC(C)C1=C(C(=C(C(=N1)C(C)C)COC)C2=CC=C(C=C2)F)C=CC(CC(CC(=O)O)O)O.[Na]
- Isomeric SMILES:CC(C)C1=C(C(=C(C(=N1)C(C)C)COC)C2=CC=C(C=C2)F)/C=C/[C@H](C[C@H](CC(=O)O)O)O.[Na]
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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.
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Uses
Cerivastatin is a competitive inhibitor of HMG-CoA reductase. Cerivastatin sodium salt hydrate has been used as a supplement in cell culture. A competitive inhibitor of HMG-CoA reductase.
