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Pitavastatin (NK-104) calcium

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

For research use only.

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 (NK-104) calcium Chemical Structure

CAS No. 147526-32-7

Selleck's Pitavastatin (NK-104) calcium has been cited by 12 Publications

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Biological Activity

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.
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].
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 NXfBUnZiTnWwY4Tpc44h[XO|YYm= MkXFSJJ2\yC3cIThb4UhcW5iSFXLNlk{KGOnbHzzJIV5eHKnc4PpcochV0GWUEHCNUApfW6tbn;3ckBwemmpaX6pJIF{e2W|c3XkJIF{KE:DVGCxRlEudWWmaXH0[YQh\HK3ZzD0doFve3CxcoSsJGtuKD1iND64JO69VS5? NIjFc5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkW4O|k5Pid-MkK1PFc6QDZ:L3G+
hepatocytes NH3yVGZHfW6ldHnvckBie3OjeR?= MXuwMlEhfG9iMUCgeW0> MWj1dEB1dyB7MDDtbY5{ MmnzSJJ2\yCvZYThZo9tcXOvIHnuJHNxemGpdXWtSIF4dGW7IILheEBp\XCjdH;jfZRmeyCjc4Pld5Nm\CCyZYKgNVAoPiClZXzsd{BifCByLkGgeI8hOTBidV2geZAhfG9iOUCgcYlveyCkeTDt[YRq[S2ub4PzJI1mfGixZDygT40hRSBzMzFOwG0v NYjPb2FHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK1PVMxOzhpPkKyOVk{ODN6PD;hQi=>
Neuro2a M1zZcWZ2dmO2aX;uJIF{e2G7 M3nyblEhfU1? MknJTY5pcWKrdHnvckBw\iCmZXz0ZUA5NTdiaYPvcYVz[XOnIHnuJI1wfXOnIF7leZJwOmFiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gO{1FUENibHX2[Yx{KGG2IEGgeW0h[nliTFOtUXMwT0NvTWOgZY5idHm|aYO= M4fTelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4N{i5OlU4Lz5{Nke4PVY2PzxxYU6=
Neuro2a MmSwSpVv[3Srb36gZZN{[Xl? MX:xJJVO NVfoRZI3UW6qaXLpeIlwdiCxZjDEVlI1KGmwIH3veZNmKE6ndYLvNoEh[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5iNz3ETGMhdGW4ZXzzJIF1KDFidV2gZpkhVENvTWOvS2MuVVNiYX7hcJl{cXN? NEG5V4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke4PVY2Pyd-Mk[3PFk3PTd:L3G+
Neuro2a NXjKflZ{TnWwY4Tpc44h[XO|YYm= MVixJJVO NX;nR3R5UW6qaXLpeIlwdiCxZjDIUWdEd0FicnXkeYN1[XOnIHnuJGRp[3J5LXTl[olkcWWwdDDtc5V{\SCQZYXyc|JiKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIEetSGhEKGyndnXsd{BifCBzIIXNJIJ6KEyFLV3TM2dENU2VIHHuZYx6e2m| MmfPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ5OEm2OVcoRjJ4N{i5OlU4RC:jPh?=
MCF-7 NVrVVplWTnWwY4Tpc44h[XO|YYm= MnjJNVAhfU1? M3z6V|I1KGi{cx?= NE\xNoZCdnSjZ3;ubZN1KGGldHn2bZR6KGG2IF35Z{11[WepZXSgVnhT[WyyaHGgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hcHWvYX6gUWNHNTdiY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kA6NWOrcz3SRUBqdmS3Y3XkJJJm[2WydH;yJJRz[W6|YXP0bZZifGmxbjDheEAyOCC3TTDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5 NVizZ|hSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiwPFk{PDdpPkK4NFg6OzR5PD;hQi=>
MCF-7 MYrGeY5kfGmxbjDhd5NigQ>? MYmxJJVO MYmyOEBpenN? MXrBcpRi\2:waYP0JIFkfGm4aYT5JIF1KE27Yz30ZYdo\WRiUmjSZYxxcGFiKIXub45wf25ib4Lp[4lvMSCneIDy[ZN{\WRiaX6gbJVu[W5iTVPGMVch[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjC5MYNqey2UQTDpcoR2[2WmIILlZ4VxfG:{IITyZY5{[WO2aY\heIlwdiCjdDCxJJVOKGGodHXyJFI1KGi{czDifUBtfWOrZnXyZZNmKHKncH;yeIVzKGenbnWgZZN{[Xl? M2nsNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MEi5N|Q4Lz5{OEC4PVM1PzxxYU6=
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot Nrf2 / NQO1 / HO-1 ; Flt1 / Flk1 ; VEGF / p-Akt / AKT / Jagged-1 / c-Notch1 / Notch-1 / Hes-1 28542559 21301413
Growth inhibition assay Cell number 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 (from reference)

Cell Research:

[5]
  • 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.
Animal Research:

[6]
  • Animal Models: C57BL/6 mice
  • Dosages: 1 or 3 mg/kg/d
  • Administration: oral

Solubility (25°C)

In vitro

 DMSO 51 mg/mL
(57.89 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 880.98
Formula

C50H46CaF2N2O8

CAS No. 147526-32-7
Storage 3 years -20°C powder
2 years -80°C in solvent
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]

In vivo Formulation Calculator (Clear solution)

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04643093 Active not 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 Active not recruiting Drug: Pitavastatin|Drug: Placebo Dyslipidemia|Obesity HealthCore-NERI|National Heart Lung and Blood Institute (NHLBI) May 1 2018 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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.

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