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Chemical Structure| 147526-32-7 Chemical Structure| 147526-32-7

Structure of Pitavastatin Calcium
CAS No.: 147526-32-7

Chemical Structure| 147526-32-7

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Pitavastatin Calcium is a potent and competitive inhibitor of HMG-CoA reductase with Ki value of 1.7nM, which can block cholesterol synthesis.

Synonyms: NK-104 hemicalcium; Pitavastatin hemicalcium; NKS 104

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Product Details of Pitavastatin Calcium

CAS No. :147526-32-7
Formula : C50H46CaF2N2O8
M.W : 880.98
SMILES Code : O=C([O-])C[C@H](O)C[C@H](O)/C=C/C1=C(C2=CC=C(F)C=C2)C3=CC=CC=C3N=C1C4CC4.O=C([O-])C[C@H](O)C[C@H](O)/C=C/C5=C(C6=CC=C(F)C=C6)C7=CC=CC=C7N=C5C8CC8.[Ca+2]
Synonyms :
NK-104 hemicalcium; Pitavastatin hemicalcium; NKS 104
MDL No. :MFCD01937979

Safety of Pitavastatin Calcium

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335-H351
Precautionary Statements:P201-P202-P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P308+P313-P332+P313-P362+P364-P403+P233-P501

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human primary T cells 1, 5, 10 µM 2 hours pretreatment followed by 22 hours stimulation To evaluate the inhibitory effects of Pitavastatin on cytokine production in PMA plus ionomycin-activated T cells, results showed that Pitavastatin significantly inhibited the production of IL-2, IL-6, IFN-γ, and TNF-α. PMC6678418
Endothelial Progenitor Cells (EPCs) 0.1, 0.5, 1.0 μM 24 hours Pitavastatin Calcium dose-dependently increased the proliferative ability of endothelial progenitor cells and reversed high-fat diet-induced autophagy and mitochondrial dysfunction. PMC8831604
Endothelial progenitor cells (EPC) 0.001 µM, 0.01 µM, 0.1 µM 24 hours To evaluate the effect of Pitavastatin-NPs on EPC proliferation, results showed that Pitavastatin-NPs significantly promoted EPC proliferation. PMC5741712
SCC15 cells 0.5 μM 48 hours Pitavastatin Calcium significantly suppressed cell viability and induced apoptosis in SCC15 cells. PMC7299721
SCC4 cells 0.5 μM 48 hours Pitavastatin Calcium had no significant effect on the cell viability of SCC4 cells. PMC7299721

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/KsJ-db/db obese mice Obesity-related colon cancer model Oral 1 ppm or 10 ppm 8 weeks Pitavastatin significantly reduced the number of colonic premalignant lesions, β-catenin accumulated crypts, by inhibiting proliferation and the surrounding inflammation. Pitavastatin increased the serum levels of adiponectin while conversely decreasing the serum levels of total cholesterol, tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), interleukin-18 (IL-18), and leptin. Pitavastatin also caused a significant increase in the expression of phosphorylated form of the AMP-activated kinase (AMPK) protein on the colonic mucosa of AOM-treated mice. In addition, the expression levels of TNF-α, IL-6, IL-18, and COX-2 mRNAs on the colonic mucosa of AOM-treated mice were decreased by treatment with this agent. PMC11158884
ApoE−/−mice Atherosclerosis model 0.5 μM 24 hours Pitavastatin Calcium improved the proliferative ability of endothelial progenitor cells in atherosclerotic mice by activating mitophagy and reversing mitochondrial dysfunction. PMC8831604
LDLR−/− mice Hypercholesterolemia model induced by high-fat diet Subcutaneous administration 3 mg/kg Once daily for 8 weeks To investigate the effects of Pitavastatin on inflammation and serotonin transporter (SERT) availability induced by hypercholesterolemia. Results showed that Pitavastatin significantly reduced total cholesterol and LDL cholesterol levels, decreased inflammatory markers, and improved SERT availability in brain regions associated with mood regulation, suggesting its potential to alleviate depressive symptoms associated with hypercholesterolemia. PMC11330603
rats carotid artery injury model tail vein injection 0.01 µM, 0.1 µM single injection, experiment lasted for 14 days To evaluate the effect of Pitavastatin-NPs on carotid artery injury repair, results showed that Pitavastatin-NPs promoted re-endothelialization and inhibited intimal hyperplasia. PMC5741712
C57BL/KsJ-db/db mice Obese mouse model Oral 1 ppm and 10 ppm Once daily for 14 weeks Pitavastatin significantly inhibited the development of hepatic premalignant lesions by inducing apoptosis and inhibiting cell proliferation, improved liver steatosis, activated the AMPK-α protein in the liver, decreased serum levels of free fatty acids and aminotransferases, and increased serum adiponectin levels. PMC3146939

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT03418974 Dyslipidemias Phase 4 Active, not recruiting December 31, 2021 China, Beijing ... More >> Heart Center of Peking University People's Hospital Beijing, Beijing, China, 100044 China, Shanghai School of Public Health, Fudan University Shanghai, Shanghai, China, 200032 Less <<
NCT01178853 - Completed - -
NCT00242944 Coronary Disease ... More >> Hypercholesterolemia Less << Phase 4 Completed - Japan ... More >> Juntendo University School of Medicine Bunkyo-ku, Tokyo, Japan, 113-8421 Yamaguchi University Graduate School of Medicine Ube, Yamaguchi, Japan, 755-8505 Kyoto University Graduate School of Medicine Kyoto, Japan, 606-8507 Less <<
NCT01178853 Healthy Phase 4 Completed - United States, Texas ... More >> Austin, Texas, United States Less <<
NCT01166633 Hypercholesterolemia Phase 4 Completed - -
NCT01660191 Hypercholesterolemia Phase 4 Completed - United States, Kansas ... More >> University of Kansas Medical Center Kansas City, Kansas, United States, 66160 Less <<
NCT01660191 - Completed - -
NCT01223586 - Completed - Japan ... More >> Division of Cardiology, Department of Medicine and Clinical Science, Yamaguchi University Graduate School of Medicine Ube, Yamaguchi, Japan, 755-8505 Division of Cardiology, Kyoto University Hospital Kyoto, Japan, 606-8507 Less <<
NCT00861861 Hypercholesterolemia ... More >> Coronary Artery Disease Less << Phase 4 Completed - Japan ... More >> Kumamoto University Graduate School of Medical Sciences Department of Cardiocascular Medicine Kumamoto, Japan, 860-8556 Less <<
NCT02940366 Metabolic Syndrome Phase 4 Recruiting November 30, 2019 Korea, Republic of ... More >> Seoul National University Hospital Recruiting Seoul, Korea, Republic of Contact: Hyung-Kwan Kim, MD    82-2-2072-0243    cardiman73@gmail.com    Principal Investigator: Hyung-Kwan Kim, MD Less <<
NCT00249249 Primary Hypercholesterolemia ... More >> Dyslipidemia Less << Phase 3 Completed - -
NCT00309751 Type II Diabetes Mellitus ... More >> Dyslipidemia Less << Phase 3 Completed - Denmark ... More >> CCBR Aalborg Aalborg, Denmark CCBR A/S Ballerup, Denmark CCBR Vejle Vejle, Denmark Germany Gemeinschaftspraxis am Bahnhof Berlin-Spandau, Germany Pharmakologisches Studienzentum Chemnitz Chemnitz, Germany Internistische Diabetische Schwerpunktpraxis Dr. Frankfurt Am Main, Germany Internistische Gemeinschaftspraxis Mainz, Germany Gemeinschaftspraxis Dr. Senftleber, Dr. Kohler Messkirch, Germany India Bhagwan Mahaveer Jain Heart Centre Bangalore, India Sri Ramachandra Medical College Hospital Chennai, India Apollo Hospitals Hyderabaad, India CARE Group of Hospitals Hyderabaad, India PD Hinduja Hospital Mumbai, India Netherlands Andromed Breda Breda, Netherlands Andromed Eindhoven Eindhoven, Netherlands Andromed Noord Groningen, Netherlands Andromed Leiden Leiden, Netherlands Andromed Nijmegen Nijmegen, Netherlands Andromed Rotterdam Rotterdam, Netherlands Andromed Oost Velp, Netherlands Andromed Zoetermeer Zoetermeer, Netherlands Poland Podlaski Osrodek Kardiologii Bialystok, Poland NZOZ GCP Dobra Praktyka Lekaska Gruziadz, Poland NZOZ Terapia Optima Katowice, Poland NZOZ Esculap, Przychodnia Lekary Rodzinnych Losice, Poland NZOZ Centrum, Poradnia Kardiologiczna Siedlce, Poland Spec. Gab. Lek. Internistyczno-Kardiologicznly Tarnow, Poland Woj.Szp.Spec.Nr 1 im. Prof. J. Gasinskiego Tychy, Poland Instytut Zywnosci i Zywienia Warszawa, Poland Lecznica PROSEN SMO Warszawa, Poland Szpital Wolski,im. Dr A. Gostynskiej Warszawa, Poland United Kingdom Synexus Reading Clinical Research Centre Berkshire, United Kingdom Synexus Lancashire Clinical Research Centre Lancashire, United Kingdom Synexus Merseyside Clinical Research Centre Liverpool, United Kingdom Synexus Manchester Clinical Research Centre Manchester, United Kingdom Less <<
NCT00309751 - Completed - -
NCT01648829 Coronary Artery Disease Phase 4 Unknown December 2017 Italy ... More >> Sapienza University Not yet recruiting Rome, Italy, 00166 Contact: Francesco Pelliccia, MD    +39064997 ext 123    f.pelliccia@mclink.it    Principal Investigator: Francesco Pelliccia, MD Less <<
NCT01386853 Hyperlipidemia Phase 3 Unknown July 2012 Taiwan ... More >> Changhua Christian Hospital Not yet recruiting Chang-hua, Taiwan Principal Investigator: Chien-Hsun Hsia, M.D.          Sub-Investigator: Lee-Shin Lin, M.D.          National Cheng Kung University Hospital Not yet recruiting Tainan, Taiwan Principal Investigator: Ping-Yen Liu, M.D. Ph.D.          Sub-Investigator: Po-Sheng Chen, M.D.          Sub-Investigator: Ju-Yi Chen, M.D.          Sub-Investigator: Wei-Ting Li, M.D.          Sub-Investigator: Yen-Wen Liu, M.D.          Sub-Investigator: Cheng-Han Lee, M.D.          Sub-Investigator: Wei-Chuan Tsai, M.D.          Sub-Investigator: Yi-Heng Li, M.D.          Sub-Investigator: Chih-Chan Lin, M.D.          Sub-Investigator: Shih-Hung Chan, M.D.          Sub-Investigator: Ting-Hsing Chao, M.D.          Chang Gung Memorial Hospital-LinKou Not yet recruiting Taipei, Taiwan Principal Investigator: Ming-Shien Wen, M.D. Ph.D.          Sub-Investigator: Kuo-Chun Hung, M.D.          Sub-Investigator: I-Chang Hsieh, M.D.          Sub-Investigator: Chao-Yung Wang, M.D.          Sub-Investigator: Chun-Chi Chen, M.D.          National Taiwan University Hospital Not yet recruiting Taipei, Taiwan Principal Investigator: Kuo-Liong Chien, M.D. Ph.D.          Sub-Investigator: Chia-Lun Chao, M.D.          Sub-Investigator: Ta-Chen Su, M.D. Ph.D.          Sub-Investigator: Hung-Ju Lin, M.D.          Taipei Veterans General Hospital Not yet recruiting Taipei, Taiwan Principal Investigator: Tao-Cheng Wu, M.D. Ph.D.          Sub-Investigator: Chin-Chou Huang, M.D.          Sub-Investigator: Liang-Yu Lin, M.D.          Sub-Investigator: Wen-Chung Yu, M.D.          Tri-Service General Hospital Taipei, Taiwan Less <<
NCT00249249 - Completed - -
NCT02863185 Chronic Kidney Disease Phase 4 Recruiting December 2019 Korea, Republic of ... More >> Won Suk An Recruiting Busan, Korea, Republic of, 602-715 Contact: Won Suk An, M.D., Ph.D.    +82-51-240-2811    anws@dau.ac.kr    Dong-A University Not yet recruiting Busan, Korea, Republic of, 602715 Contact: Su Mi Lee, MD    +822405549    promise131@hanmail.net Less <<
NCT00889226 Hypercholesterolemia With Type... More >>2DM Less << Phase 4 Completed - -
NCT02056847 HbA1c Level Associated With Li... More >>pid Compositions Less << Phase 4 Completed - Korea, Republic of ... More >> JW pharmaceutical Seoul, Korea, Republic of, 137-864 Less <<
NCT00344370 - Completed - -
NCT01710007 Hypercholesterolemia Phase 3 Completed - Taiwan ... More >> Buddhist Taipei TzuChi General Hospital New Taipei City, Taiwan, 23142 Cardinal Tien Hospital New Taipei City, Taiwan, 231 Taipei Medical University - Shuang Ho Hospital New Taipei City, Taiwan, 23561 Taichung Veterans General Hospital Taichung City, Taiwan, 40705 Taipei Veterans General Hospital Taipei City, Taiwan, 11217 Cheng Hsin General Hospital Taipei City, Taiwan, 112 Tri-Service General Hospital Taipei City, Taiwan, 114 Chang Gung Medical Foundation- LinKuo Branch Taoyuan City, Taiwan, 333 Less <<
NCT00344370 Type II Diabetes Mellitus ... More >> Dyslipidemia Less << Phase 3 Completed - Denmark ... More >> CCBR Aalborg Aalborg, Denmark CCBR A/S Vejle, Denmark CCBR Vejle Vejle, Denmark Germany Gemeinschaftspraxis am Bahnhof Berlin-Spandau, Germany Pharmakologisches Studienzentum Chemnitz Chemnitz, Germany Internistische Diabetische Schwerpunktpraxis Dr. Frankfurt Am Main, Germany Internistische Gemeinschaftspraxis Mainz, Germany Gemeinschaftspraxis Dr. Senftleber, Dr. Kohler Messkirch, Germany India Bhagwan Mahaveer Jain Heart Centre Bangalore, India Sri Ramachandra Medical College Hospital Chennai, India Apollo Hospitals Hyderabaad, India CARE Group of Hospitals Hyderabaad, India PD Hinduja Hospital Mumbai, India Netherlands Andromed Breda Breda, Netherlands Andromed Eindhoven Eindhoven, Netherlands Andromed Noord Groningen, Netherlands Andromed Leiden Leiden, Netherlands Andromed Nijmegen Nijmegen, Netherlands Andromed Rotterdam Rotterdam, Netherlands Andromed Oost Velp, Netherlands Andromed Zoetermeer Zoetermeer, Netherlands Poland Podlaski Osrodek Kardiologii Bialystok, Poland NZOZ GCP Dobra Praktyka Lekaska Gruziadz, Poland NZOZ Terapia Optima Katowice, Poland NZOZ Esculap, Przychodnia Lekary Rodzinnych Losice, Poland NZOZ Centrum, Poradnia Kardiologiczna Siedlce, Poland Spec. Gab. Lek. Internistyczno-Kardiologicznly Tarnow, Poland Woj.Szp.Spec.Nr 1 im. Prof. J. Gasinskiego Tychy, Poland Instytut Zywnosci i Zywienia Warszawa, Poland Lecznica PROSEN SMO Warszawa, Poland Szpital Wolski,im. Dr A. Gostynskiej Warszawa, Poland United Kingdom Synexus Reading Clinical Research Centre Berkshire, United Kingdom Synexus Lancashire Clinical Research Centre Lancashire, United Kingdom Synexus Merseyside Clinical Research Centre Liverpool, United Kingdom Synexus Manchester Clinical Research Centre Manchester, United Kingdom Less <<
NCT03532620 Prediabetic State ... More >> Hypertension Dyslipidemias Less << Phase 4 Recruiting September 2020 China, Chongqing ... More >> Fourth People's Hospital of Chongqing Recruiting Chongqing, Chongqing, China, 400014 Contact: Ruihua Yue, MD          Principal Investigator: Ruihua Yue, MD          China, Guangdong First Affiliated Hospital,Sun Yat-sen University Recruiting Guangzhou, Guangdong, China, 510000 Contact: Jun Tao, MD,PhD    +8613922191609    taojungz123@163.com    Contact: Jianning Zhang    +8615521264372    ningjenny@yeah.net    Principal Investigator: Jun Tao, MD,PhD          Second Affiliated Hospital of Guangzhou Medical University Recruiting Guangzhou, Guangdong, China, 510260 Contact: Wenchao Qu, MD          Principal Investigator: Wenchao Qu, MD          First Affiliated Hospital of Jinan University Recruiting Guangzhou, Guangdong, China, 510630 Contact: Jun Guo, MD          Principal Investigator: Jun Guo, MD          Shenzhen People's Hospital Not yet recruiting Shenzhen, Guangdong, China, 518020 Contact: Xin Jiang, MD          Principal Investigator: Xin Jiang, MD          People's Hospital of Zhongshan City Recruiting Zhongshan, Guangdong, China, 528403 Contact: Li Feng, MD          Principal Investigator: Li Feng, MD          China, Henan First Affiliated Hospital of Zhengzhou University Recruiting Zhengzhou, Henan, China, 450052 Contact: Heping Gu, MD          Principal Investigator: Heping Gu, MD          China, Hubei Yichang Central Hospital Recruiting Yichang, Hubei, China, 443003 Contact: Jiawang Ding, MD          Principal Investigator: Jiawang Ding, MD          China, Jiangsu Taizhou Hospital of TCM Recruiting Taizhou, Jiangsu, China, 214504 Contact: Yongguang Zhang, MD          Principal Investigator: Yongguang Zhang, MD          Wuxi People's Hospital Recruiting Wuxi, Jiangsu, China, 214023 Contact: Ruxing Wang, MD          Principal Investigator: Ruxing Wang, MD          Subei People's Hospital of Jiangsu province Not yet recruiting Yangzhou, Jiangsu, China, 225001 Contact: Shenghu He, MD          Principal Investigator: Shenghu He, MD          China, Qinghai Lanzhou University Second Hospital Recruiting Lanzhou, Qinghai, China, 730030 Contact: Feng Bai, MD          Principal Investigator: Feng Bai, MD          China, Shandong Yantaishan Hospital, Yantai Not yet recruiting Yantai, Shandong, China, 264001 Contact: Lan Zhao, MD          Principal Investigator: Lan Zhao, MD Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.14mL

0.23mL

0.11mL

5.68mL

1.14mL

0.57mL

11.35mL

2.27mL

1.14mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

Historical Records

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