[CAS NO. 147511-69-1] Pitavastatin

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PRODUCTS SPECIFICATIONS [147511-69-1]

Catalog

HY-B0144A

Brand

MCE

CAS

147511-69-1

DESCRIPTION [147511-69-1]

Overview

MDL	-
Molecular Weight	421.46
Molecular Formula	C25H24FNO4
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

For research use only. We do not sell to patients.

4 Publications Citing Use of MCE

Summary

Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC ₅₀ of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin 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 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) ^[4] .
Pitavastatin (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 ^[4] .
Pitavastatin (1 μM, 48 hours) causes PARP cleavage in Ovcar-8 cells ^[4] .
Pitavastatin (0.1 and 1 μM; 1 h, then cells incubate with TNF-α for 6 h) increases the expression of ICAM-1 mRNA through suppressing NF-κB pathway in TNF-α-stimulated human saphenous vein endothelial cells ^[6] .

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis ^[4]

Cell Line:	Ovcar-8 cells
Concentration:	1 μM
Incubation Time:	48 hours
Result:	Induced PARP cleavage.

In Vivo

Pitavastatin (59 mg/kg; p.o.; twice daily for 28 days) causes significant tumour regression ^[4] .
Pitavastatin (0.1 mg/kg; p.o; daily for 12 weeks) retards the progression of atherosclerosis formation and improves NO bioavailability by eNOS up-regulation and decrease of O ^2- in diet induced severe hyperlipidemia rabbit model ^[7] .

MedChemExpress (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) ^[4]
Dosage:	59 mg/kg
Administration:	p.o.; twice daily for 28 days
Result:	Caused significant tumour regression.

Animal Model:	Female New Zealand white rabbits (diet induced severe hyperlipidemia) ^[7]
Dosage:	0.1 mg/kg
Administration:	p.o; daily for 12 weeks
Result:	Retarded the progression of atherosclerosis formation and improved NO bioavailability by eNOS up-regulation and decrease of O ^2- .

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00701285	JW Pharmaceutical	Chronic Heart Failure	July 2008	Phase 4
NCT02888327	Alios Biopharma Inc.	Influenza in Humans	July 31, 2016	Phase 1
NCT02442700	Ramathibodi Hospital	HIV\|Dyslipidemia	May 2014	Phase 4
NCT03730038	Yonsei University	Dyslipidemias	February 18, 2019	Not Applicable
NCT01386853	Tai Tien Pharmaceuticals Co., Ltd.	Hyperlipidemia	July 2011	Phase 3
NCT02940366	Seoul National University Hospital\|JW Pharmaceutical	Metabolic Syndrome	December 1, 2016	Phase 4
NCT04402112	JW Pharmaceutical	Hypercholesterolemia	April 2, 2012
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
NCT00444717	Aichi Gakuin University	Metabolic Syndrome\|Oxidative Stress\|Inflammation	April 2007	Phase 4
NCT00242944	Kyoto University\|Yamaguchi University Hospital\|Juntendo University\|Kyoto University Hospital	Coronary Disease\|Hypercholesterolemia	November 2005	Phase 4
NCT00309777	Kowa Research Europe	Hypercholesterolemia\|Dyslipidemia	September 2005	Phase 3
NCT00711919	Kyoto Prefectural University of Medicine	Hyperlipidemia\|Carotid Artery Diseases	July 2007	Not Applicable
NCT02545231	Korea University Anam Hospital	Atherosclerosis\|Neointima\|Angina	February 2013	Phase 4
NCT00249249	Kowa Research Europe	Primary Hypercholesterolemia\|Dyslipidemia	October 2005	Phase 3
NCT01178853	Kowa Research Institute, Inc.	Healthy	July 2010	Phase 4
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
NCT01256476	Kowa Research Institute, Inc.	Primary Dyslipidemia\|Mixed Dyslipidemia	October 2010	Phase 4
NCT00889226	JW Pharmaceutical	Hypercholesterolemia With Type2DM	April 2008	Phase 4
NCT05977738	C.Dirven\|Erasmus Medical Center	Glioblastoma Multiforme, Adult\|Recurrent Glioblastoma	November 2023	Early Phase 1
NCT00325780	Kowa Research Europe	Hypercholesterolemia\|Dyslipidemia	July 2006	Phase 3
NCT01042730	Juntendo University\|Tokyo University\|Yamaguchi University Hospital\|Tohoku University\|Kyoto University\|Kumamoto University	Coronary Artery Disease	February 2010	Not Applicable
NCT00257686	Kowa Research Europe	Hypercholesterolemia or Combined Dyslipidemia	September 2005	Phase 3
NCT04945122	Chinese Academy of Medical Sciences, Fuwai Hospital	Acute Myocardial Infarction\|Glucose Metabolism Disorders	October 1, 2015	Phase 4
NCT01648829	University of Roma La Sapienza	Coronary Artery Disease	January 2014	Phase 4
NCT01502904	Yonsei University	Stable Angina or Acute Coronary Syndrome Considered for Percutaneous Coronary Intervention With Dyslipidemia or Hypertension	July 2010	Phase 4
NCT00549926	Yokohama City University Medical Center	Coronary Disease\|Hypercholesterolemia	October 2007	Phase 4
NCT01057433	Kowa Research Institute, Inc.	Healthy Volunteers	January 2010	Phase 4
NCT00846118	Chieko Hamada\|Juntendo University	Cardiovascular Disease	February 1, 2009	Not Applicable
NCT02595268	Janssen Research & Development, LLC	Healthy	November 2015	Phase 1
NCT00548145	Osaka University\|Kowa Company, Ltd.	Alzheimer Disease\|Hypercholesterolemia	November 2007	Not Applicable
NCT02956590	Carelon Research\|National Heart, Lung, and Blood Institute (NHLBI)	Dyslipidemia\|Obesity	May 1, 2018	Phase 3
NCT03532620	Jun Tao\|Sun Yat-sen University\|First Affiliated Hospital, Sun Yat-Sen University	Prediabetic State\|Hypertension\|Dyslipidemias	August 9, 2018	Phase 4
NCT03717064	Hoffmann-La Roche	Healthy Volunteers	November 7, 2018	Phase 1
NCT00330876	Kowa Research Europe	Hypercholesterolemia\|Dyslipidemias	June 2006	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
NCT03070223	AIDS Clinical Trials Group\|National Institute of Allergy and Infectious Diseases (NIAID)\|National Institute on Aging (NIA)	HIV-1 Infection	February 28, 2017
NCT00861861	Kumamoto University	Hypercholesterolemia\|Coronary Artery Disease	September 2008	Phase 4
NCT00786734	JW Pharmaceutical	Percutaneous Coronary Intervention	August 2008	Phase 4
NCT02863185	Dong-A University	Chronic Kidney Disease	May 1, 2016	Phase 4
NCT01043094	Kowa Research Institute, Inc.	Severe Renal Impairment	December 2009	Phase 4
NCT04270344	JW Pharmaceutical	Hypercholesterolemia	July 1, 2018
NCT03418974	Fudan University\|Peking University People´s Hospital\|Jiangsu Wanbang Medicine Marketing Co., Ltd.	Dyslipidemias	November 1, 2017	Phase 4
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
NCT00344175	Kowa Research Europe	Hypercholesterolemia\|Dyslipidemia\|Coronary Heart Disease	June 2006	Phase 3
NCT02144922	Asan Medical Center\|JW Pharmaceutical	Hypertension\|Cardiovascular Risk	May 2014	Phase 4
NCT03311841	Merck Sharp & Dohme LLC	Renal Insufficiency	March 1, 2018	Phase 1
NCT01422382	Kowa Research Institute, Inc.	Healthy	May 2011	Phase 4
NCT01695954	NYU Langone Health\|New York City Health and Hospitals Corporation\|Kowa Pharmaceuticals America, Inc.\|University at Buffalo	Hyperlipidemia\|HIV	May 2012	Phase 1
NCT05705804	Yonsei University	Dyslipidemias\|Atherosclerotic Cardiovascular Disease	June 13, 2023	Not Applicable
NCT04705909	Mansoura University	Breast Cancer	January 15, 2021	Phase 2\|Phase 3
NCT00716846	Hamamatsu University	Healthy Volunteers	June 2006	Not Applicable
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
NCT00653913	Organon and Co	Hypercholesterolemia	March 2004	Phase 1
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
NCT00309738	Kowa Research Europe	Hypercholesterolemia\|Dyslipidemia	September 2005	Phase 3
NCT02634034	Kowa Research Institute, Inc.	Hyperlipidemia	December 2015	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
NCT00309751	Kowa Research Europe	Type II Diabetes Mellitus\|Dyslipidemia	December 2005	Phase 3
NCT04643093	Orient Pharma Co., Ltd.	Primary Hypercholesterolemia\|Mixed Dyslipidemias	August 1, 2020	Phase 3
NCT02290106	Massachusetts General Hospital	Obesity\|Fatty Liver, Nonalcoholic	March 2, 2015	Not Applicable
NCT01595828	Kowa Research Europe	Metabolic Syndrome	October 2010	Phase 1
NCT00344370	Kowa Research Europe	Type II Diabetes Mellitus\|Dyslipidemia	August 2006	Phase 3
NCT01166633	JW Pharmaceutical	Hypercholesterolemia	June 2009	Phase 4
NCT01301066	Kowa Research Institute, Inc.\|Kowa Pharmaceuticals America, Inc.\|Eli Lilly and Company	Dyslipidemia	December 2010	Phase 4
NCT00640276	JW Pharmaceutical	Hypercholesterolemia\|Metabolic Syndrome	April 2008	Phase 4
NCT01422369	Kowa Research Institute, Inc.	Healthy	April 2011	Phase 4

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 237.27 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3727 mL	11.8635 mL	23.7270 mL
5 mM	0.4745 mL	2.3727 mL	4.7454 mL
10 mM	0.2373 mL	1.1864 mL	2.3727 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% Saline

Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

* All of the co-solvents are available by MedChemExpress (MCE).