Pitavastatin

Modify Date: 2024-01-02 18:40:02

Pitavastatin Structure
Pitavastatin structure
Common Name Pitavastatin
CAS Number 147511-69-1 Molecular Weight 421.461
Density 1.4±0.1 g/cm3 Boiling Point 692.0±55.0 °C at 760 mmHg
Molecular Formula C25H24FNO4 Melting Point N/A
MSDS N/A Flash Point 372.3±31.5 °C

 Use of Pitavastatin


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).IC50 value: 5.8 nM(cholesterol synthesis from aceticacid in HepG2) [1]Target: HMG-CoA reductasein vitro: Pitavastatin inhibited cholesterol synthesis from aceticacid with an IC50 of 5.8 nM in a human liver cancer cell line (HepG2), which indicates that is 2.9 and 5.7 times as potent as simvastatin and atorvastatin, respectively. When the inhibitory activity interms of the ED50 was compared with that of simvastatin,pitavastatin showed a 3-fold stronger activity in the rat and 15-fold stronger activity in a guinea pig model.22 The inhibitory effect of pitavastatin on sterol synthesis is thought to be liver-selective [1]. pitavastatin reduces total and phosphorylated tau levels in a cellular model of tauopathy, and in primary neuronal cultures. The decrease caused by pitavastatin is reversed by the addition of mevalonate, or geranylgeranyl pyrophosphate. The maturation of small G proteins, including RhoA was disrupted by pitavastatin, as was the activity of glycogen synthase kinase 3β (GSK3β), a major tau kinase [4].in vivo: Intravenous treatment with pitavastatin-incorporated nanoparticles, but not with control nanoparticles or pitavastatin alone, inhibited plaque destabilization and rupture associated with decreased monocyte infiltration and gelatinase activity in the plaque[2].The EAM model was established in BALB/c mice by immunization with murine α-myosin heavy chain. Mice were fed pitavastatin (5 mg/kg) or vehicle once daily for 3 weeks from day 0 to day 21 after immunization [3].

 Names

Name pitavastatin
Synonym More Synonyms

 Pitavastatin Biological Activity

Description 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).IC50 value: 5.8 nM(cholesterol synthesis from aceticacid in HepG2) [1]Target: HMG-CoA reductasein vitro: Pitavastatin inhibited cholesterol synthesis from aceticacid with an IC50 of 5.8 nM in a human liver cancer cell line (HepG2), which indicates that is 2.9 and 5.7 times as potent as simvastatin and atorvastatin, respectively. When the inhibitory activity interms of the ED50 was compared with that of simvastatin,pitavastatin showed a 3-fold stronger activity in the rat and 15-fold stronger activity in a guinea pig model.22 The inhibitory effect of pitavastatin on sterol synthesis is thought to be liver-selective [1]. pitavastatin reduces total and phosphorylated tau levels in a cellular model of tauopathy, and in primary neuronal cultures. The decrease caused by pitavastatin is reversed by the addition of mevalonate, or geranylgeranyl pyrophosphate. The maturation of small G proteins, including RhoA was disrupted by pitavastatin, as was the activity of glycogen synthase kinase 3β (GSK3β), a major tau kinase [4].in vivo: Intravenous treatment with pitavastatin-incorporated nanoparticles, but not with control nanoparticles or pitavastatin alone, inhibited plaque destabilization and rupture associated with decreased monocyte infiltration and gelatinase activity in the plaque[2].The EAM model was established in BALB/c mice by immunization with murine α-myosin heavy chain. Mice were fed pitavastatin (5 mg/kg) or vehicle once daily for 3 weeks from day 0 to day 21 after immunization [3].
Related Catalog
References

[1]. Morikawa S, et al. Relative induction of mRNA for HMG CoA reductase and LDL receptor by five different HMG-CoA reductase inhibitors in cultured human cells. J Atheroscler Thromb. 2000;7(3):138-44.

[2]. Katsuki S, et al. Nanoparticle-mediated delivery of pitavastatin inhibits atherosclerotic plaque destabilization/rupture in mice by regulating the recruitment of inflammatory monocytes. Circulation. 2014 Feb 25;129(8):896-906.

[3]. Tajiri K, et al. Pitavastatin regulates helper T-cell differentiation and ameliorates autoimmune myocarditis in mice. Cardiovasc Drugs Ther. 2013 Oct;27(5):413-24.

[4]. Hamano T, et al. Pitavastatin decreases tau levels via the inactivation of Rho/ROCK. Neurobiol Aging. 2012 Oct;33(10):2306-20.

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Boiling Point 692.0±55.0 °C at 760 mmHg
Molecular Formula C25H24FNO4
Molecular Weight 421.461
Flash Point 372.3±31.5 °C
Exact Mass 421.168945
PSA 90.65000
LogP 3.45
Vapour Pressure 0.0±2.3 mmHg at 25°C
Index of Refraction 1.680
Storage condition 2-8℃

 Safety Information

Hazard Codes Xi
HS Code 3004909090

 Customs

HS Code 3004909090

 Synonyms

ITAVASTATIN
Pitavastatin
(6E)-7-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl]-3,5-dihydroxy-6-heptenoic acid
PITVASTATIN
MFCD04113054
6-Heptenoic acid, 7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl]-3,5-dihydroxy-, (6E)-
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