Pitavastatin Calcium

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

Pitavastatin Calcium  Chemical Structure

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.

Size Price Stock Quantity  
USD 97 In stock
USD 310 In stock
USD 647 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Cited by 4 Publications

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     


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     


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     


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     


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]

+ Expand
  • 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]

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

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

Molecular Weight 880.98
Formula

C50H46CaF2N2O8

CAS No. 147526-32-7
Storage powder
in solvent
Synonyms NK-104, P-872441, itavastatin, nisvastatin

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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.

HMG-CoA Reductase Signaling Pathway Map

Tags: buy Pitavastatin Calcium | Pitavastatin Calcium supplier | purchase Pitavastatin Calcium | Pitavastatin Calcium cost | Pitavastatin Calcium manufacturer | order Pitavastatin Calcium | Pitavastatin Calcium distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID