Pitavastatin Chemical Properties

Melting point:

182 - 185°C

Boiling point:

692.0±55.0 °C(Predicted)

Density 

1.352±0.06 g/cm3(Predicted)

storage temp. 

-20°C, Hygroscopic

solubility 

Chloroform (Slightly), Methanol (Slightly)

pka

4.24±0.10(Predicted)

form 

Solid

color 

White to Off-White

Stability:

Hygroscopic

CAS DataBase Reference

147511-69-1(CAS DataBase Reference)

EPA Substance Registry System

6-Heptenoic acid, 7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl]-3,5-dihydroxy-, (3R,5S,6E)- (147511-69-1)

Safety Information

Hazardous Substances Data

147511-69-1(Hazardous Substances Data)

Pitavastatin Usage And Synthesis

Description

Pitavastatin (Brand Name: LIVALO) is an inhibitor of HMG-CoA reductase which catalyzes the first step of cholesterol synthesis. It appears as odorless and white to pale-yellow powder. It takes effects by reducing the level of certain fatty substances such as cholesterol in the body. Therefore, it is mainly indicated for the treatment of hypercholesterolaemia and for the prevention of cardiovascular diseases. It can not only lower the high cholesterol and triglyceride in certain patients, but also can increase the content of high density lipoprotein (HDL), the “good” cholesterol levels. It should be generally administrated together with a proper diet.

Reference

https://en.wikipedia.org/wiki/Pitavastatin
http://www.rxlist.com/livalo-drug.htm
https://www.drugs.com/cdi/pitavastatin.html

Uses

HMGA reductase inhibitor

Definition

ChEBI: A hydroxy monocarboxylic acid anion that is the conjugate base of pitavastatin, obtained by deprotonation of the carboxy group.

brand name

[Name previously used: Itavastatin].

Biological Activity

pitavastatin (nk-104) is a potent hmg-coa reductase inhibitor, pitavastatin inhibited cholesterol synthesis from acetic acid with an ic50 of 5.8 nm in a human liver cancer cell line (hepg2).

Enzyme inhibitor

This HMG-CoA reductase inhibitor (FW = 421.46 g/mol; CAS 147511-69- 1; IUPAC Name: (3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin- 3-yl]-3,5-dihydroxyhept-6-enoic acid), also known as itavastatin, itabavastin, nisvastatin, NK-104, NKS-104, and the trade name Livalo?, is indicated for ameliorating hypercholesterolemia and preventing cardiovascular disease. NK-104 potency is dose-dependent and is roughly equivalent to that of atorvastatin. It is well-tolerated in the treatment of patients with hypercholesterolemia. Pitavastatin uptake is carrier-mediated. Target(s): Reduces inflammatory cytokine production from human bronchial epithelial cells; Decreases microtubule tau protein levels via the inactivation of Rho/ROCK; Inhibits hepatic steatosis and fibrosis in non-alcoholic steatohepatitis model; Suppresses therosclerosis induced by chronic inhibition of the synthesis of nitric oxide in moderately hypercholesterolemic rabbits; Decreases the expression of endothelial lipase both in vitro and in vivo; Inhibits NFkB pathway in brain; Inactivates NFkB and decreases IL-6 production through Rho kinase pathway in MCF-7 human breast cancer cells; Reduces C-reactive-protein-induced interleukin-8 production in human aortic endothelial cells; Inhibits lysophosphatidic acid-induced proliferation and monocyte chemoattractant protein-1 expression in aortic smooth muscle cells by suppressing Rac-1-mediated reactive oxygen species generation; Inhibits upregulation of intermediate conductance calcium-activated potassium channels and coronary arteriolar remodeling induced by long-term blockade of nitric oxide synthesis; Inhibits migration and proliferation of rat vascular smooth muscle cells.

Pitavastatin(147511-69-1)Related Product Information

• Atorvastatin
• Isoquinoline
• Simvastatin
• Ethoxyquin
• PITAVASTATIN CALCIUM
• Quinclorac
• Quinolinic acid
• Fluvastatin
• Atorvastatin calcium
• Quinhydrone
• Pravastatin
• (E)-3-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl-2-propenal
• Tert-buthyl Pitavastatin
• 2-Cyclopropyl-4-(4-fluorophenyl)quinoline-3-carboxaldehyde
• PITAVASTATIN LACTONE
• 2-Cyclopropyl-4-(4-fluorophenyl)-quinolyl-3-methanol
• Pitavastatin Intermediates
• Pitavastatin