222306-15-2

Basic information

• Product Name: 5-Oxo Pitavastatin
• Synonyms: 5-Oxo Pitavastatin
• CAS NO: 222306-15-2
• Molecular Formula: C25H22FNO4
• Molecular Weight: 419.4448832
• Product Categories: Aromatics, Heterocycles, Inhibitors, Metabolites & Impurities, Pharmaceuticals, Intermediates & Fine Chemicals
• Mol File: 222306-15-2.mol
• Article Data: 3

Chemical Properties

• Boiling Point: 655.1±55.0 °C(Predicted)
• Appearance: /
• Density: 1.349±0.06 g/cm3(Predicted)
• Storage Temp.: Hygroscopic, -20°C Freezer, Under inert atmosphere
• Solubility: Chloroform (Slightly), Methanol (Slightly)
• PKA: 4.18±0.10(Predicted)
• Stability: Hygroscopic
• CAS DataBase Reference: 5-Oxo Pitavastatin(CAS DataBase Reference)
• NIST Chemistry Reference: 5-Oxo Pitavastatin(222306-15-2)
• EPA Substance Registry System: 5-Oxo Pitavastatin(222306-15-2)

Safety Data

• Hazardous Substances Data: 222306-15-2(Hazardous Substances Data)

Usage

Description

5-Oxo Pitavastatin is a metabolite of Pitavastatin, which is a competitive inhibitor of HMG-CoA reductase. It is recognized as an antilipemic agent, playing a significant role in managing lipid levels in the body.

Uses

Used in Pharmaceutical Industry:
5-Oxo Pitavastatin is used as an antilipemic agent for the purpose of controlling and reducing high levels of lipids in the blood. Its role in inhibiting HMG-CoA reductase makes it a valuable component in the development of medications aimed at treating hyperlipidemia and related conditions.

Upstream product

• 147526-32-7 pitavastatin calcium salt 

Relevant articles and documents

Preparation method for pitavastatin calcium 5-oxo-impurity

The invention belongs to the technical field of pharmaceutical synthesis, and particularly relates to a preparation method for a pitavastatin calcium 5-oxo-impurity. According to the preparation method for a pitavastatin calcium 5-oxo-impurity, pitavastat

Metabolic fate of pitavastatin, a new inhibitor of HMG-CoA reductase: Human UDP-glucuronosyltransferase enzymes involved in lactonization

1. Pitavastatin is a potent competitive inhibitor of HMG-CoA reductase little metabolized in hepatic microsomes. Pitavastatin lactone, which can be converted back to the unchanged form, is the major metabolite of pitavastatin in humans. To clarify the mechanism of the lactonization of pitavastatin and the metabolic properties of the lactone, we performed experiments in vitro. 2. On addition of UDP-glucuronic acid, human hepatic microsomes produced pitavastatin lactone and an unknown metabolite (UM-2). UM-2 was converted to its unchanged form by enzymatic hydrolysis and to a lactone form non-enzymatically. Using several human UGT-expressing microsomes, UGT1A3 and UGT2B7 were principally responsible for glucuronidation of pitavastatin leading to lactonization. 3. No marked difference in intrinsic clearance between pitavastatin and its lactone form was detected in human hepatic microsomes. 4. Pitavastatin lactone showed no inhibitory effects on CYP2C9- and CYP3A4-mediated metabolism of model substrates in contrast to other HMG-CoA reductase inhibitors. 5. The mechanism of pitavastatin lactone formation has been clarified, in that glucuronidation by UGT occurs first followed by lactonization via an elimination reaction. It was also found that pitavastatin lactone demonstrates no drug - drug interactions.