Pitavastatin

Pitavastatin Basic information
Description Reference
Product Name:Pitavastatin
Synonyms:ITAVASTATIN;monocalciumbis{(3r,5s,6e)-7-[2-cyclopyl-4-(4-fluorophenyl)-3-quinolyl]-3,5-dihydroxy-6-heptenoate};PitavastatinCa;PITVASTATIN;(3R,5S,6E)-7-(2-Cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-3,5-dihydroxyhept-6-enoic acid;PITAVASTATIN;( )-(3R,5S,6E)-7-(2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolyl)-3,5-dihydroxy-6-heptenoic acid;6-Heptenoic acid, 7-(2-cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl)-3,5-dihydroxy-, (3R,5S,6E)-
CAS:147511-69-1
MF:C25H24FNO4
MW:421.46
EINECS:
Product Categories:LIVALO;API
Mol File:147511-69-1.mol
Pitavastatin Structure
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)
pka4.24±0.10(Predicted)
form Solid
color White to Off-White
Stability:Hygroscopic
CAS DataBase Reference147511-69-1(CAS DataBase Reference)
EPA Substance Registry System6-Heptenoic acid, 7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl]-3,5-dihydroxy-, (3R,5S,6E)- (147511-69-1)
Safety Information
Hazardous Substances Data147511-69-1(Hazardous Substances Data)
MSDS Information
Pitavastatin Usage And Synthesis
DescriptionPitavastatin (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.
Referencehttps://en.wikipedia.org/wiki/Pitavastatin
http://www.rxlist.com/livalo-drug.htm
https://www.drugs.com/cdi/pitavastatin.html

UsesHMGA reductase inhibitor
DefinitionChEBI: 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 Activitypitavastatin (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 inhibitorThis 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 Preparation Products And Raw materials
PITAVASTATIN CALCIUM Simvastatin Isoquinoline Ethyl(E)-(5S)-7-[2-cyclopropyl-4-(4-fluorophenyl)-5-hydroxy-3oxoxo-3-quinolinyl] -hept-6-enoate Quinclorac Atorvastatin Atorvastatin calcium (E)-3-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl-2-propenal INTERMEDIATES OF PITAVASTATIN CALCIUM Ethoxyquin Pitavastatin Tert-buthyl Pitavastatin Fluvastatin Quinolinic acid (E)-3-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl-2-propenenitrite 2-Cyclopropyl-4-(4-fluorophenyl)quinoline-3-carboxaldehyde Quinhydrone PITAVASTATIN LACTONE

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