"目录号: HY-13956
Pioglitazone (U 72107)是选择性PPARγ刺激剂。
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生物活性
Description
Pioglitazone (U 72107) is a selective peroxisome proliferator-activated receptor gamma(PPARγ) stimulator.IC50 Value:Target: PPARin vitro: HIT-T15 cells were cultured for 5 days in the presence of AGEs alone, or supplemented with 1 μmol/l Pioglitazone. Cell viability, insulin secretion and insulin content, redox balance, expression of the AGE receptor (RAGE), and NF-kB activation were then determined. The results showed that Pioglitazone protected beta cellsagainst AGEs-induced apoptosis and necrosis. Moreover, Pioglitazone restored the redox balance and improved the responsiveness to low glucose concentration. Adding Pioglitazone to the AGEs culture attenuated NF-kB phosphorylation, and prevented AGEs to down-regulate IkBα expression [1]. Pioglitazone attenuated AngII-induced CTGF expression and proliferation in atrial fibroblasts, and pioglitazone also inhibited the expression or phosphorylation of AngII-induced transforming growth factor-β1 (TGF-β1), tumor necrosis factor receptor associated factor 6 (TRAF6), TGF-β-associated kinase 1 (TAK1) and Smad2/3. In HL-1 cells, pioglitazone suppressed AngII-induced ICa-L α1c expression and current density as well as CAMP responsive element binding protein (CREB) phosphorylation. Besides, pioglitazone inhibited AngII-induced production of AngII type I receptor (AT1R) and downregulation of PPAR-γ in both atrial fibroblasts and HL-1 cells. In conclusion, Pioglitazone suppresses AngII-induced CTGF expression and proliferation in atrial fibroblasts, which might be at least in part related with its inhibitory effects on TGF-β1/Smad2/3 and TGF-β1/TRAF6/TAK1 signaling pathways [2]. in vivo: Diabetic nephropathic group treated by oral administration of pioglitazone (10 mg/kg per d) for 4 weeks. DN (Diabetic nephropathic) rats showed excessive deposition of collagen fibers in their cardiac tissue, along with a marked myocyte hypertrophy. This was associated with a dramatic upregulation of cardiac transforming growth factor-β1 (TGF-β1) gene. Furthermore, the gene expression of matrix metalloproteinase 2 (MMP-2) decreased, while the gene expression of tissue inhibitor of metalloproteinase 2 (TIMP-2) increased in the hearts of DN rats [3]. Pioglitazone, given orally at a dose of 2.5mg/kg/d, reduced cardiac triglyceride content and suppressed lipid deposition in the heart of angiotensin II-induced hypertensive rats without affecting angiotensin II-induced upregulation of lipogenic gene expression [4]. Toxicity: On June 9, 2011 the French Agency for the Safety of Health Products decided to withdraw pioglitazone in regards to high risk of bladder cancer.
Clinical Trial
Korea University Anam Hospital
Diabetes Mellitus-Coronary Artery Stenosis
July 2007
Phase 4
Children's Hospital of Fudan University
Chronic Granulomatous Disease
September 1, 2017
Phase 1-Phase 2
University Hospital, Geneva-University of Lausanne Hospitals
Diabetes-Hypertension
October 2005
Phase 4
Meng Li-Tongji Hospital
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
February 2016
Phase 2
Joseph Calabrese, MD-Takeda Pharmaceuticals North America, Inc.-University Hospitals Cleveland Medical Center
Depressive Disorder, Major-Metabolic Syndrome X
April 2008
Phase 2
Indiana University
Polycystic Kidney Disease
October 2015
Phase 2
Paul Beringer-University of Southern California
Cystic Fibrosis
January 2008
Phase 1
Wake Forest University Health Sciences
Brain Neoplasms, Malignant-Brain Neoplasms, Benign-Malignant Meningioma-Glioblastoma Multiforme-Anaplastic Astrocytoma
August 2010
Phase 1
Children's Hospital Medical Center, Cincinnati
Severe Sepsis-Septic Shock
October 2011
Phase 1-Phase 2
Takeda-Kaiser Permanente-Department of Epidemiology at University of Pennsylvania
Diabetes-Bladder Cancer
July 2004
Assistance Publique - Hôpitaux de Paris
Friedreich's Ataxia
December 2008
Phase 3
Takeda-Zinfandel Pharmaceuticals Inc.
Mild Cognitive Impairment Due to Alzheimer's Disease
August 2013
Phase 3
Kaohsiung Medical University Chung-Ho Memorial Hospital
Hepatitis
April 2009
Phase 2
Takeda
Diabetes Mellitus, Type 2, Cancer
January 1997
King Abdulaziz University
Diabetes Mellitus-Diabetes Mellitus, Type 2-Glucose Metabolism Disorders
January 2009
Phase 2
University Hospitals Cleveland Medical Center-National Alliance for Research on Schizophrenia and Depression-Takeda Pharmaceuticals North America, Inc.
Metabolic Syndrome-Bipolar Depression-Insulin Resistance
March 2009
Phase 4
The University of Texas Health Science Center at San Antonio
Type 2 Diabetes-Healthy-Impaired Glucose Tolerance
June 2007
Phase 4
Takeda
Type II Diabetes Mellitus
January 2014
Phase 4
Pusan National University Hospital
Type 2 Diabetes
December 2009
Phase 4
Dana-Farber Cancer Institute
Advanced Solid Tumor-Metastatic Solid Tumor
August 2011
Phase 1
LG Life Sciences
Healthy
February 2009
Phase 1
University of Texas Southwestern Medical Center-National Institutes of Health (NIH)
Obesity-Type 2 Diabetes
February 2009
Huashan Hospital-Baxter Healthcare Corporation
Peritoneal Dialysis-Pioglitazone-Hypertriglyceridemia-Insulin Resistance-Inflammation
January 2008
University of Rochester
Diabetes-Platelet Function-Healthy
December 2008
Phase 2
The University of Texas Health Science Center at San Antonio
Type 2 Diabetes
August 2009
Phase 4
Stanford University
Cardiac Allograft Vasculopathy
July 2010
Phase 2
Takeda
Mild Cognitive Impairment Due to Alzheimer's Disease
November 17, 2014
Phase 3
Emory University-National Institute on Alcohol Abuse and Alcoholism (NIAAA)
Alcoholism
August 28, 2017
Phase 2
Postgraduate Institute of Medical Education and Research
Bladder Cancer
July 2013
Kurume University
To Evaluate the Effect of Pioglitazone on Glucose Metabolism of Fat Tissue by Using FDG-PET/CT Imaging
March 2012
Dana King-Takeda Pharmaceuticals North America, Inc.-Medical University of South Carolina
Diabetes
October 2008
Phase 4
Emory University
Chronic Myelogenous Leukemia, BCR-ABL1 Positive-Recurrent Chronic Myelogenous Leukemia, BCR-ABL1 Positive
May 2016
Phase 2
National Cancer Institute (NCI)
Head and Neck Cancer-Oral Leukoplakia
June 2003
Phase 2
Coordinación de Investigación en Salud, Mexico
Type 2 Diabetes
October 2005
Phase 1-Phase 2
Takeda
Type 2 Diabetes Mellitus
January 2009
University of Miami-Takeda Pharmaceuticals North America, Inc.
Type 2 Diabetes Mellitus
April 2008
Phase 3
University of Rochester-National Institute of Neurological Disorders and Stroke (NINDS)-Michael J. Fox Foundation for Parkinson's Research
Parkinson's Disease
March 2011
Phase 2
University of Michigan-National Institute on Alcohol Abuse and Alcoholism (NIAAA)
Chronic Pancreatitis-Insulin Resistance-Normal Stool Fat Levels
November 2008
Phase 2
University of Dhaka-Bangladesh Institute of Research and Rehabilitation in Diabetes, Endocrine and Metabolic Disorders-University of Dundee
Type 2 Diabetes Mellitus
November 2008
Phase 4
Skane University Hospital-Medical Research Council-Skane County Council Research & Development Foundation
Type 2 Diabetes-Secondary Drug Failure
April 2004
Phase 4
Stony Brook University
Type 1 Diabetes Mellitus
June 2002
Phase 1
AstraZeneca
Type 2 Diabetes Mellitus
February 2010
Phase 1
Takeda
Diabetes Mellitus
December 2002
Phase 2
Takeda-Eli Lilly and Company
Diabetes Mellitus
May 2001
Phase 3
Sung-Chen Liu-Mackay Memorial Hospital
Type 2 Diabetes
October 2009
