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Pitavastatin (NK-104) Calcium HMG-CoA Reductase Inhibiteur

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

Réf. Catalogue: S1759

Pitavastatin calcium, un nouveau membre de la classe de médicaments des statines, est une formulation de sel de calcium de la pitavastatine qui est un inhibiteur très efficace de la HMG-CoA réductase. Le Pitavastatin Calcium atténue la mitophagie induite par les AGEs via l'inhibition de la génération de ROS. Le Pitavastatin Calcium induit l'autophagie et l'apoptose.

Pitavastatin (NK-104) Calcium HMG-CoA Reductase Inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 880.98

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Contrôle Qualité (Quality Control)

Lot : Pureté : 99.96%

99.96

Cibles apparentées	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Autre HMG-CoA Reductase Inhibiteurs	Mevastatin SR-12813 Clinofibrate Dihydrolanosterol 7-ketocholesterol Cerivastatin sodium

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)

Lignées cellulaires	Type d'essai	Concentration	Temps d'incubation	Description de l'activité	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
Cliquez pour voir plus de données expérimentales sur la lignée cellulaire

Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire	880.98	Formule	C₅₀H₄₆CaF₂N₂O₈	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	147526-32-7	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	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]

Solubilité (Solubility)

In vitro
Lot:

DMSO : 100 mg/mL (113.5 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
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 Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	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.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre d'animaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme d'action (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.
Références	[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 (Applications)

Méthodes	Biomarqueurs	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

Informations sur l'essai clinique (Clinical Trial Information)

(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	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

Foire aux questions (Frequently Asked Questions)

Question 1:
How to prepare the solution of it for in vivo use?

Réponse :
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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C6=C5/X	C6:	LOG(C6):
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C8=C7/X	C8:	LOG(C8):