Home Metabolism HMG-CoA Reductase inhibitor - COVID-19 inhibitor - Autophagy activator - Mitophagy inhibitor - Apoptosis related activator Pitavastatin calcium For research use only.

Pitavastatin calcium

Synonyms: NK-104 calcium

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. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.

Pitavastatin calcium Chemical Structure

Pitavastatin calcium Chemical Structure

CAS: 147526-32-7

Selleck's Pitavastatin calcium has been cited by 23 Publications

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Purity & Quality Control

Batch: Purity: 99.96%
99.96

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 Function assay Drug uptake in HEK293 cells expressing OATP1B1 (unknown origin) assessed as OATP1B1-mediated drug transport, Km = 4.8 μM. 22587986
hepatocytes Function assay 0.1 to 10 uM up to 90 mins Drug metabolism in Sprague-Dawley rat hepatocytes assessed per 10'6 cells at 0.1 to 10 uM up to 90 mins by media-loss method, Km = 13 μM. 22593038
Neuro2a Function assay 1 uM Inhibition of delta 8-7 isomerase in mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis 26789657
Neuro2a Function assay 1 uM Inhibition of DR24 in mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis 26789657
Neuro2a Function assay 1 uM Inhibition of HMGCoA reductase in Dhcr7-deficient mouse Neuro2a cells assessed as decrease in 7-DHC levels at 1 uM by LC-MS/GC-MS analysis 26789657
MCF-7 Function assay 10 uM 24 hrs Antagonist activity at Myc-tagged RXRalpha (unknown origin) expressed in human MCF-7 cells assessed as inhibition of 9-cis-RA induced receptor transactivation at 10 uM after 24 hrs by luciferase reporter gene assay 28089347
MCF-7 Function assay 1 uM 24 hrs Antagonist activity at Myc-tagged RXRalpha (unknown origin) expressed in human MCF-7 cells assessed as inhibition of 9-cis-RA induced receptor transactivation at 1 uM after 24 hrs by luciferase reporter gene assay 28089347
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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. Pitavastatin Calcium attenuates AGEs-induced mitophagy via inhibition of ROS generation. Pitavastatin Calcium induces autophagy and apoptosis.
Targets
cholesterol esters [1] HMG-CoA reductase [4]
In vitro
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].
Cell Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot VEGF / p-Akt / AKT / Jagged-1 / c-Notch1 / Notch-1 / Hes-1 Flt1 / Flk1 Nrf2 / NQO1 / HO-1 21301413
Growth inhibition assay Cell number 21301413
In Vivo
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].
Animal Research Animal Models C57BL/6 mice
Dosages 1 or 3 mg/kg/d
Administration oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05977738 Not yet recruiting Glioblastoma Multiforme Adult|Recurrent Glioblastoma C.Dirven|Erasmus Medical Center November 2023 Early Phase 1
NCT04643093 Completed Primary Hypercholesterolemia|Mixed Dyslipidemias Orient Pharma Co. Ltd. August 1 2020 Phase 3
NCT03717064 Completed Healthy Volunteers Hoffmann-La Roche November 7 2018 Phase 1

Chemical lnformation & Solubility

Molecular Weight 880.98 Formula

C50H46CaF2N2O8

CAS No. 147526-32-7 SDF Download Pitavastatin calcium SDF
Smiles C1CC1C2=NC3=CC=CC=C3C(=C2C=CC(CC(CC(=O)[O-])O)O)C4=CC=C(C=C4)F.C1CC1C2=NC3=CC=CC=C3C(=C2C=CC(CC(CC(=O)[O-])O)O)C4=CC=C(C=C4)F.[Ca+2]
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (113.5 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

HMG-CoA Reductase Signaling Pathway Map

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