Name: Pitavastatin (NK-104) Calcium
Brand: Selleck Chemicals
SKU: S1759
Availability: InStock
Rating: 5 (28 reviews)

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Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other HMG-CoA Reductase Inhibitors	Mevastatin SR-12813 Clinofibrate Cerivastatin sodium Dihydrolanosterol 7-ketocholesterol

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (113.5 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (5.68mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 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.

Chemical Information, Storage & Stability

Molecular Weight	880.98	Formula	C₅₀H₄₆CaF₂N₂O₈	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	147526-32-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NK-104 calcium			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]

Mechanism of Action

Targets/IC₅₀/Ki	cholesterol esters HMG-CoA reductase
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. 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/20699675/ [2] https://pubmed.ncbi.nlm.nih.gov/11390424/ [3] https://pubmed.ncbi.nlm.nih.gov/11554731/ [4] https://pubmed.ncbi.nlm.nih.gov/12481202/ [5] https://pubmed.ncbi.nlm.nih.gov/27621652/ [6] https://pubmed.ncbi.nlm.nih.gov/24670355/

Applications

Methods	Biomarkers	Images	PMID
Western blot	Nrf2 / NQO1 / HO-1 Flt1 / Flk1 VEGF / p-Akt / AKT / Jagged-1 / c-Notch1 / Notch-1 / Hes-1		28542559
Growth inhibition assay	Cell number		21301413

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05977738	Recruiting	Glioblastoma Multiforme Adult\|Recurrent Glioblastoma	C.Dirven\|Erasmus Medical Center	January 18 2024	Early Phase 1
NCT04643093	Completed	Primary Hypercholesterolemia\|Mixed Dyslipidemias	Orient Pharma Co. Ltd.	August 1 2020	Phase 3

Tech Support

Handling Instructions

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

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

Frequently Asked Questions

Question 1:
How to prepare the solution of it 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 (NK-104) Calcium HMG-CoA Reductase inhibitor

Chemical Structure

Molecular Weight: 880.98