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[CAS NO. 147526-32-7] PitavastatinCalcium
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-B0144 |
| Brand: | MCE |
| CAS: | 147526-32-7 |
Overview
| MDL | MFCD01937979 |
|---|---|
| Molecular Weight | 440.49 |
| Molecular Formula | C25H23Ca0.5FNO4 |
| SMILES | 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.[0.5Ca2+] |
3 Publications Citing Use of MCE
Summary
Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC 50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin Calcium also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects [1] [2] [3] [8] .
IC50 & Target
HMG-CoA Reductase [1]
In Vitro
Pitavastatin Calcium inhibits the growth of a panel of ovarian cancer cells, including those considered most likely to represent HGSOC, grown as a monolayers (IC
50
= 0.4-5 μM) or as spheroids (IC
50
=0.6-4 μM)
[3]
.
Pitavastatin Calcium (1 μM; 48 hours ) induces apoptosis, evidenced by the increased activity of executioner caspases-3,7 as well as caspase-8 and caspase-9 in Ovcar-8 cells and Ovcar-3 cells
[3]
.
Pitavastatin (1 μM, 48 hours) causes PARP cleavage in Ovcar-8 cells
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [3]
| Cell Line: | Ovcar-8 cells |
| Concentration: | 1 μM |
| Incubation Time: | 48 hours |
| Result: | Induced PARP cleavage. |
In Vivo
Pitavastatin Calcium (59 mg/kg; p.o.; twice daily for 28 days) causes significant tumour regression [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | 4 week old female NCR Nu/Nu female mice (bearing Ovcar-4 tumours) [3] |
| Dosage: | 59 mg/kg |
| Administration: | p.o.; twice daily for 28 days |
| Result: | Caused significant tumour regression. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00309738 | Kowa Research Europe |
Hypercholesterolemia|Dyslipidemia
|
September 2005 | Phase 3 |
| NCT02344290 | National Institute of Allergy and Infectious Diseases (NIAID)|National Heart, Lung, and Blood Institute (NHLBI)|Kowa Pharmaceuticals America, Inc.|Gilead Sciences|Massachusetts General Hospital|NEAT ID Foundation |
HIV Infections|Cardiovascular Diseases
|
March 26, 2015 | Phase 3 |
| NCT04402112 | JW Pharmaceutical |
Hypercholesterolemia
|
April 2, 2012 | |
| NCT01695954 | NYU Langone Health|New York City Health and Hospitals Corporation|Kowa Pharmaceuticals America, Inc.|University at Buffalo |
Hyperlipidemia|HIV
|
May 2012 | Phase 1 |
| NCT02940366 | Seoul National University Hospital|JW Pharmaceutical |
Metabolic Syndrome
|
December 1, 2016 | Phase 4 |
| NCT01422382 | Kowa Research Institute, Inc. |
Healthy
|
May 2011 | Phase 4 |
| NCT01042730 | Juntendo University|Tokyo University|Yamaguchi University Hospital|Tohoku University|Kyoto University|Kumamoto University |
Coronary Artery Disease
|
February 2010 | Not Applicable |
| NCT01595828 | Kowa Research Europe |
Metabolic Syndrome
|
October 2010 | Phase 1 |
| NCT01422369 | Kowa Research Institute, Inc. |
Healthy
|
April 2011 | Phase 4 |
| NCT02290106 | Massachusetts General Hospital |
Obesity|Fatty Liver, Nonalcoholic
|
March 2, 2015 | Not Applicable |
| NCT03418974 | Fudan University|Peking University People´s Hospital|Jiangsu Wanbang Medicine Marketing Co., Ltd. |
Dyslipidemias
|
November 1, 2017 | Phase 4 |
| NCT03532620 | Jun Tao|Sun Yat-sen University|First Affiliated Hospital, Sun Yat-Sen University |
Prediabetic State|Hypertension|Dyslipidemias
|
August 9, 2018 | Phase 4 |
| NCT00846118 | Chieko Hamada|Juntendo University |
Cardiovascular Disease
|
February 1, 2009 | Not Applicable |
| NCT02634034 | Kowa Research Institute, Inc. |
Hyperlipidemia
|
December 2015 | Phase 1 |
| NCT00711919 | Kyoto Prefectural University of Medicine |
Hyperlipidemia|Carotid Artery Diseases
|
July 2007 | Not Applicable |
| NCT03070223 | AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID)|National Institute on Aging (NIA) |
HIV-1 Infection
|
February 28, 2017 | |
| NCT01166633 | JW Pharmaceutical |
Hypercholesterolemia
|
June 2009 | Phase 4 |
| NCT00242944 | Kyoto University|Yamaguchi University Hospital|Juntendo University |
Coronary Disease|Hypercholesterolemia
|
November 2005 | Phase 4 |
| NCT02144922 | Asan Medical Center|JW Pharmaceutical |
Hypertension|Cardiovascular Risk
|
May 2014 | Phase 4 |
| NCT04270344 | JW Pharmaceutical |
Hypercholesterolemia
|
July 1, 2018 | |
| NCT01871792 | Gachon University Gil Medical Center|Gangnam Severance Hospital|Severance Hospital|National Health Insurance Service Ilsan Hospital|Myongji Hospital|Bundang CHA Hospital|Inje University|Dankook University|Eulji General Hospital |
Contrast-induced Nephropathy
|
June 2013 | Phase 4 |
| NCT00889226 | JW Pharmaceutical |
Hypercholesterolemia With Type2DM
|
April 2008 | Phase 4 |
| NCT00701285 | JW Pharmaceutical |
Chronic Heart Failure
|
July 2008 | Phase 4 |
| NCT01043094 | Kowa Research Institute, Inc. |
Severe Renal Impairment
|
December 2009 | Phase 4 |
| NCT01648829 | University of Roma La Sapienza |
Coronary Artery Disease
|
January 2014 | Phase 4 |
| NCT00325780 | Kowa Research Europe |
Hypercholesterolemia|Dyslipidemia
|
July 2006 | Phase 3 |
| NCT03606824 | Shaochun.Li|Chinese Academy of Medical Sciences, Fuwai Hospital|Peking University Third Hospital|Beijing Chao Yang Hospital|Xuanwu Hospital, Beijing|Beijing Friendship Hospital|China National Center for Cardiovascular Diseases |
Dyslipidemia|Subclinical hypothyroïdism|Statin|ASCVD
|
March 25, 2019 | Not Applicable |
| NCT01767610 | Hanlim Pharm. Co., Ltd. |
Healthy Male Volunteers
|
January 2013 | Phase 1 |
| NCT04643093 | Orient Pharma Co., Ltd. |
Primary Hypercholesterolemia|Mixed Dyslipidemias
|
August 1, 2020 | Phase 3 |
| NCT02743260 | University of Cologne|Umm Al-Qura University|Institute for Biomedical and Pharmaceutical Research (IBMP), Nürnberg-Heroldsberg, Germany |
Healthy
|
April 2016 | Phase 4 |
| NCT02545231 | Korea University Anam Hospital |
Atherosclerosis|Neointima|Angina
|
February 2013 | Phase 4 |
| NCT00786734 | JW Pharmaceutical |
Percutaneous Coronary Intervention
|
August 2008 | Phase 4 |
| NCT03730038 | Yonsei University |
Dyslipidemias
|
February 18, 2019 | Not Applicable |
| NCT03717064 | Hoffmann-La Roche |
Healthy Volunteers
|
November 7, 2018 | Phase 1 |
| NCT00549926 | Yokohama City University Medical Center |
Coronary Disease|Hypercholesterolemia
|
October 2007 | Phase 4 |
| NCT05537948 | National Medical Research Center for Therapy and Preventive Medicine |
Dyslipidemias|Hyperlipidemias|Liver Transplant Disorder|Immunosuppression|Hydroxymethylglutaryl-CoA Reductase Inhibitors|Statins
|
October 1, 2021 | Phase 4 |
| NCT04512105 | University of California, Irvine|United States Department of Defense |
Acute Myeloid Leukemia|Chronic Lymphocytic Leukemia|AML, Adult|CLL|CLL, Relapsed|CLL, Refractory
|
December 2, 2020 | Phase 1 |
| NCT01301066 | Kowa Research Institute, Inc.|Kowa Pharmaceuticals America, Inc.|Eli Lilly and Company |
Dyslipidemia
|
December 2010 | Phase 4 |
| NCT04705909 | Mansoura University |
Breast Cancer
|
January 15, 2021 | Phase 2|Phase 3 |
| NCT02863185 | Dong-A University |
Chronic Kidney Disease
|
May 1, 2016 | Phase 4 |
| NCT01502904 | Yonsei University |
Stable Angina or Acute Coronary Syndrome Considered for Percutaneous Coronary Intervention With Dyslipidemia or Hypertension
|
July 2010 | Phase 4 |
| NCT00309777 | Kowa Research Europe |
Hypercholesterolemia|Dyslipidemia
|
September 2005 | Phase 3 |
| NCT00257686 | Kowa Research Europe |
Hypercholesterolemia or Combined Dyslipidemia
|
September 2005 | Phase 3 |
| NCT00249249 | Kowa Research Europe |
Primary Hypercholesterolemia|Dyslipidemia
|
October 2005 | Phase 3 |
| NCT00716846 | Hamamatsu University |
Healthy Volunteers
|
June 2006 | Not Applicable |
| NCT01256476 | Kowa Research Institute, Inc. |
Primary Dyslipidemia|Mixed Dyslipidemia
|
October 2010 | Phase 4 |
| NCT00330876 | Kowa Research Europe |
Hypercholesterolemia|Dyslipidemias
|
June 2006 | Phase 3 |
| NCT00344370 | Kowa Research Europe |
Type II Diabetes Mellitus|Dyslipidemia
|
August 2006 | Phase 3 |
| NCT00861861 | Kumamoto University |
Hypercholesterolemia|Coronary Artery Disease
|
September 2008 | Phase 4 |
| NCT02442700 | Ramathibodi Hospital |
HIV|Dyslipidemia
|
May 2014 | Phase 4 |
| NCT02888327 | Alios Biopharma Inc. |
Influenza in Humans
|
July 31, 2016 | Phase 1 |
| NCT04945122 | Chinese Academy of Medical Sciences, Fuwai Hospital |
Acute Myocardial Infarction|Glucose Metabolism Disorders
|
October 1, 2015 | Phase 4 |
| NCT01178853 | Kowa Research Institute, Inc. |
Healthy
|
July 2010 | Phase 4 |
| NCT00344175 | Kowa Research Europe |
Hypercholesterolemia|Dyslipidemia|Coronary Heart Disease
|
June 2006 | Phase 3 |
| NCT02595268 | Janssen Research & Development, LLC |
Healthy
|
November 2015 | Phase 1 |
| NCT02956590 | HealthCore-NERI|National Heart, Lung, and Blood Institute (NHLBI) |
Dyslipidemia|Obesity
|
May 1, 2018 | Phase 3 |
| NCT00548145 | Osaka University|Kowa Company, Ltd. |
Alzheimer Disease|Hypercholesterolemia
|
November 2007 | Not Applicable |
| NCT00640276 | JW Pharmaceutical |
Hypercholesterolemia|Metabolic Syndrome
|
April 2008 | Phase 4 |
| NCT01057433 | Kowa Research Institute, Inc. |
Healthy Volunteers
|
January 2010 | Phase 4 |
| NCT00653913 | Organon and Co |
Hypercholesterolemia
|
March 2004 | Phase 1 |
| NCT02056847 | JW Pharmaceutical|The Catholic University of Korea|Kyunghee University Medical Center|Korea University Guro Hospital|Dong-A University Hospital|Seoul National University Bundang Hospital|Samsung Medical Center|Seoul National University Hospital|Ajou University School of Medicine|Gangnam Severance Hospital|Severance Hospital|Yeungnam University Hospital|Ulsan University Hospital|Eulji University Hospital|Asan Medical Center|Chonnam National University Hospital|Chonbuk National University Hospital|Chungnam National University Hospital|Hallym University Medical Center |
HbA1c Level Associated With Lipid Compositions
|
September 2013 | Phase 4 |
| NCT03311841 | Merck Sharp & Dohme LLC |
Renal Insufficiency
|
March 1, 2018 | Phase 1 |
| NCT00309751 | Kowa Research Europe |
Type II Diabetes Mellitus|Dyslipidemia
|
December 2005 | Phase 3 |
| NCT00444717 | Aichi Gakuin University |
Metabolic Syndrome|Oxidative Stress|Inflammation
|
April 2007 | Phase 4 |
| NCT01386853 | Tai Tien Pharmaceuticals Co., Ltd. |
Hyperlipidemia
|
July 2011 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : ≥ 50 mg/mL ( 113.51 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2702 mL | 11.3510 mL | 22.7020 mL |
| 5 mM | 0.4540 mL | 2.2702 mL | 4.5404 mL |
| 10 mM | 0.2270 mL | 1.1351 mL | 2.2702 mL |
References
- [1] Mukhtar RY, et al. Pitavastatin. Int J Clin Pract. 2005 Feb;59(2):239-52.
- [2] Kajinami K, et al. Pitavastatin: efficacy and safety profiles of a novel synthetic HMG-CoA reductase inhibitor. Cardiovasc Drug Rev. 2003 Fall;21(3):199-215.
- [3] Tajiri K, et al. Pitavastatin regulates helper T-cell differentiation and ameliorates autoimmune myocarditis in mice. Cardiovasc Drugs Ther. 2013 Oct;27(5):413-24.
- [4] Hamano T, et al. Pitavastatin decreases tau levels via the inactivation of Rho/ROCK. Neurobiol Aging. 2012 Oct;33(10):2306-20.
- [5] de Wolf E, et al.Dietary geranylgeraniol can limit the activity of pitavastatin as a potential treatment for drug-resistant ovarian cancer.Sci Rep. 2017 Jul 14;7(1):5410.
- [6] Demir B, et al. The Effects of Pitavastatin on Nuclear Factor-Kappa B and ICAM-1 in Human Saphenous Vein Graft Endothelial Culture. Cardiovasc Ther. 2019 May 2;2019:2549432.
- [7] Hayashi T, et al. A new HMG-CoA reductase inhibitor, pitavastatin remarkably retards the progression of high cholesterol induced atherosclerosis in rabbits. Atherosclerosis. 2004 Oct;176(2):255-63.
- [8] Sahebkar A, et al. A comprehensive review on the lipid and pleiotropic effects of pitavastatin. Prog Lipid Res. 2021 Nov;84:101127.
Synonyms
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