For research use only.
Catalog No.S1759 Synonyms: NK-104, P-872441, itavastatin, nisvastatin
CAS No. 147526-32-7
Pitavastatin Calcium (NK-104, P-872441, itavastatin, nisvastatin), 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. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.
Selleck's Pitavastatin Calcium has been cited by 8 publications
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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.
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.
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Choose Selective HMG-CoA Reductase Inhibitors
|Description||Pitavastatin Calcium (NK-104, P-872441, itavastatin, nisvastatin), 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. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.|
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.  Pitavastatin is able to activate PPARα and induce HDL apoA-I through inducing inhibition of the Rho-signaling pathway.  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. 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.
|In vivo||Pitavastatin decreases the tumor growth and improved the survival of tumor-bearing mice. 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.|
-  Ahmad H, et al. Cardiol Rev, 2010, 18(5):264-267.
-  Martin G, et al. J Clin Invest, 2001, 107(11), 1423-1432.
-  Ohnaka K, et al. Biochem Biophys Res Commun, 2001, 287(2), 337-342.
|In vitro||DMSO||51 mg/mL (57.89 mM)|
* 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.
|Synonyms||NK-104, P-872441, itavastatin, nisvastatin|
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Molecular Weight Calculator
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04643093||Recruiting||Drug: Pitavastatin|Drug: Ezetimibe|Drug: 1PC111||Primary Hypercholesterolemia|Mixed Dyslipidemias||Orient Pharma Co. Ltd.||August 1 2020||Phase 3|
|NCT03717064||Completed||Drug: RO7049389|Drug: Pitavastatin||Healthy Volunteers||Hoffmann-La Roche||November 7 2018||Phase 1|
|NCT02956590||Recruiting||Drug: Pitavastatin|Drug: Placebo||Dyslipidemia|Obesity||HealthCore-NERI|National Heart Lung and Blood Institute (NHLBI)||May 1 2018||Phase 3|
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.
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Frequently Asked Questions
How to prepare the solution of the compound (S1759) for in vivo use?
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.