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M0865135

Cerivastatinsodium , 98% , 143201-11-0

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: C26H34FNO5

Molecular Weight: 459.55

MDL number: MFCD00865716

Pack Size Price Stock Quantity
1mg RMB390.40 In Stock
5mg RMB1350.40 In Stock
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Update time: 2022-07-08

PRODUCT 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

Description and Uses

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.

Cerivastatin is a competitive inhibitor of HMG-CoA reductase.

Safety

Symbol(GHS) 
GHS07
Signal word  Warning
WGK Germany  3

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