Pitavastatin Calcium

Name: Pitavastatin Calcium
Brand: Selleck Chemicals
SKU: S1759
Rating: 5 (4 reviews)

For research use only. Not for use in humans.

Catalog No.S1759 Synonyms: NK-104, P-872441, itavastatin, nisvastatin

4 publications

Molecular Weight(MW): 880.98

Pitavastatin calcium, a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor.

Selleck's Pitavastatin Calcium has been cited by 4 publications

Drug Metab Dispos, 2017, 45(6):612-623

PubMed: 28283500 ( click the link to review the publication )

PLoS One, 2017, 12(5):e0178278

PubMed: 28542559 ( click the link to review the publication )

Sci Rep, 2015, 5:16407

PubMed: 26553420 ( click the link to review the publication )

Br J Cancer, 2014, 111(8):1562-71

PubMed: 25093497 ( click the link to review the publication )

3 Customer Reviews

Western blotting showed that in U87 cells treated with pitavastatin, the LC3-II isoform dramatically increased after statin treatment and showed at day 2, 3 and 4.

Br J Cancer, 2014, 111(8): 1562-71 . Pitavastatin Calcium purchased from Selleck.

Fewer proliferative cells were detected in the tumour after pitavastatin treatment according to the Ki67 staining results but not in fluvastatin group.

Br J Cancer, 2014, 111(8): 1562-71 . Pitavastatin Calcium purchased from Selleck.
Western blot analysis of Nrf2, NQO1, and HO-1 in statin-treated VSMCs. Cells were exposed to fluvastatin and pitavastatin for 24 h at the indicated dosages. In addition, protein samples were refined from cultured VSMCs treated with fluvastatin (5 μM) or pitavastatin (5 μM) for the indicated times.

PLoS One, 2017, 12(5):e0178278. Pitavastatin Calcium purchased from Selleck.

Purity & Quality Control

Choose Selective HMG-CoA Reductase Inhibitors

Biological Activity

Description

Pitavastatin calcium, a novel member of the medication class of statins, is a calcium salt formulation of pitavastatin which is a highly effective HMG-CoA reductase inhibitor.

Targets

cholesterol esters ^[1]

HMG-CoA reductase ^[4]

In vitro

Pitavastatin significantly reduces both intracellular levels and synthesis of cholesterol esters. Pitavastatin is found to enhance LDL-receptor expression in vitro, as well as the amount of LDL binding to the LDL-receptor. Pitavastatin also exhibits more potent induction of LDL receptor mRNA expression compared with simvastatin and atorvastatin. Pitavastatin has many pleiotropic effects in vitro and in vivo, including deterring progression of atherosclerosis via inhibition of thromboxane synthesis, inhibition of migration/proliferation of vascular smooth muscle cells induced by angiotensin II, and stabilization of atherosclerotic plaque. ^[1] Pitavastatin is able to activate PPARα and induce HDL apoA-I through inducing inhibition of the Rho-signaling pathway. ^[2] Pitavastatin (1 μM) treatment for 48 h is able to enhances bone morphogenetic protein-2 BMP-2 (2.5-fold) and osteocalcin (10-fold) expression by inhibition of Rho-associated kinase in human osteoblasts^[3]. Pitavastatin inhibits growth and colony formation of liver cancer Huh-7 cells and SMMC7721 cells. It induces arrest of liver cancer cells at the G1 phase. Increased proportion of sub-G1 cells is observed after pitavastatin treatment. Pitavastatin promotes caspase-9 cleavage and caspase-3 cleavage in liver cancer cells. Pitavastatin could regulate NF-κB and anti-inflammation in hepatocellular carcinoma cells. Pitavastatin could induce autophagic cell death in glioma cells and promote sensitivity of cells to radiotherapy. It could inhibit cell proliferation and induce cell apoptosis in cholangiocarcinoma cells as well^[5].

Assay

Methods	Test Index	PMID
Western blot	Nrf2 / NQO1 / HO-1 ; PubMed: 28542559 PLoS One Western blot analysis of Nrf2, NQO1, and HO-1 in statin-treated VSMCs. Cells were exposed to fluvastatin and pitavastatin for 24 h at the indicated dosages. Flt1 / Flk1 ; PubMed: 21301413 Lab Invest Immunoblots showing Flt-1 and Flk-1 expression in HUVECs in the absence or presence of pitavastatin. Representative data of three independent experiments with similar results. VEGF / p-Akt / AKT / Jagged-1 / c-Notch1 / Notch-1 / Hes-1 ; PubMed: 21301413 Lab Invest Immunoblots showing the time course of pitavastatin (100 nmol/l)-induced Akt and Notch1 activation, VEGF, Notch1 ligand (Jagged-1) and Hes-1 expression in human umbilical vein endothelial cells (HUVECs). Activation of Akt was assessed by Ser473 phosphorylation of Akt (p-Akt) relative to the total Akt (t-Akt). Activation of Notch1 was determined by the amount of cleaved Notch1 (c-Notch1) relative to total Notch1 (t-Notch1). Representative blots of three independent experiments with similar results.	28542559 21301413
Growth inhibition assay	Cell number; PubMed: 21301413 Lab Invest Cell counts (human umbilical vein endothelial cells) in the absence or presence of pitavastatin (10 nmol/l–1.0 μmol/l). Effects of mevalonate (200 μmol/l), LY294002 (Ly)(10 μmol/l), Akt inhibitor SH-5 (10 μmol/l), NOS inhibitor NG-nitro-L-arginine methyl ester (L-NAME) (1 mmol/l) and γ-secretase inhibitor DAPT (20 μmol/l) on cell numbers were also determined. P<0.007 compared with control and *P<0.001 compared with control and #P<0.001 compared with pitavastatin (100 nmol/l). n = 8 in each group.	21301413

In vivo

Pitavastatin decreases the tumor growth and improved the survival of tumor-bearing mice^[5]. Pitavastatin exerts a protective effect on dilated cardiomyopathy possibly through down-regulating the circulating and local RAS, followed by inhibition of PKCb2 phosphorylation, and consequently promoting the phosphorylation of PLB as well as the activity and the expressions of SERCA2a and RyR2, whereby heart function is preserved in the development of DCM^[6].

Protocol

Cell Research:

^[5]

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Cell lines: Huh-7 and SMMC7721
Concentrations: 5 μM
Incubation Time: 1, 2, 4, 6 days
Method:
The Huh-7 cells and SMMC7721 cells are split into 96-well dishes at 5,000 cells/well and treated with the indicated dosage of pitavastatin for 48 hours or 5 µM pitavastatin for 1, 2, 4, 6 days respectively. The cells are incubated with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and formed formazan in the liver cells. Formazan is dissolved in DMSO, and the absorbance is measured at the wavelength of 570 nm. The cells treated with DMSO are used as a control group. The relative cell number of each group is calculated as pitavastatin-treated group/cell number in the DMSO-treated group.

(Only for Reference)

Animal Research:

^[6]

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Animal Models: C57BL/6 mice
Formulation: saline
Dosages: 1 or 3 mg/kg/d
Administration: oral
(Only for Reference)

References

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Solubility (25°C)

In vitro	DMSO	51 mg/mL (57.89 mM)
	Water	Insoluble
	Ethanol	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Pitavastatin Calcium SDF

Molecular Weight	880.98
Formula	C₅₀H₄₆CaF₂N₂O₈
CAS No.	147526-32-7
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	NK-104, P-872441, itavastatin, nisvastatin
Smiles	[Ca++].OC(CC(O)C=CC1=C(C2=CC=C(F)C=C2)C3=CC=CC=C3N=C1C4CC4)CC([O-])=O.OC(CC(O)C=CC5=C(C6=CC=C(F)C=C6)C7=CC=CC=C7N=C5C8CC8)CC([O-])=O

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2019-10-14)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03717064	Completed	Drug: RO7049389\|Drug: Pitavastatin	Healthy Volunteers	Hoffmann-La Roche	November 7 2018	Phase 1
NCT02956590	Recruiting	Drug: Pitavastatin\|Drug: Placebo	Dyslipidemia\|Obesity	New England Research Institutes\|National Heart Lung and Blood Institute (NHLBI)	May 1 2018	Phase 3
NCT02595268	Completed	Drug: Pitavastatin\|Drug: JNJ-63623872	Healthy	Janssen Research & Development LLC	November 2015	Phase 1

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Frequently Asked Questions

Question 1:
How to prepare the solution of the compound (S1759) for in vivo use?
Answer:
You could use the formulation: 5% DMSO +40%PEG 300+5%Tween80+ddH2O for i.p., at a working concentration of 12.5mg/ml, stable for no longer than 40min.

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Pitavastatin Calcium