"目录号: HY-14601
Pioglitazone hydrochloride 是一种有效的选择性PPARγ激动剂，高亲和力结合到 PPARγ 配体结合域。作用于人和鼠 PPARγ，EC50分别为 0.93 和 0.99 μM。
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GW9662-Rosiglitazone-Retinoic acid-Troglitazone-Elafibranor-GW 501516-CDDO-Im-Fenofibrate-T0070907-Wy-14643-GW0742-Daidzein-FH535-BMS-687453-Inolitazone dihydrochloride-
生物活性
Description
Pioglitazone hydrochloride is a potent and selectivePPARγagonist with high affinity binding to the PPARγ ligand-binding domain withEC50of 0.93 and 0.99 μM for human and mouse PPARγ, respectively.
IC50& Target
EC50: 0.93 μM (human PPARγ), 0.99 μM (mouse PPARγ)[1]
In Vitro
AGEs-induced beta cell necrosis is completely abrogated by adding Pioglitazone to the AGEs culture medium. Furthermore Pioglitazone completely prevented any AGEs-induced increment in caspase-3 activation, thereby restoring caspase-3 activity to the same levels as the control cells. As expected AG is able to counteract AGEs-induced impaired viability[2].
In Vivo
The serum-free fatty acid and triglyceride levels as well as adipocyte sizes in ob/ob andadipo-/-ob/ob mice are unchanged after 10 mg/kg Pioglitazone but are significantly reduced to a similar degree after 30 mg/kg Pioglitazone. Moreover, the expressions of TNFα and resistin in adipose tissues of ob/ob andadipo-/-ob/ob mice are unchanged after 10 mg/kg Pioglitazone but are decreased after 30 mg/kg Pioglitazone. Thus, Pioglitazone-induced amelioration of insulin resistance and diabetes may occur adiponectin dependently in the liver and adiponectin independently in skeletal muscle[3]. Pioglitazone (10 mg/kg per d) treatment significantly attenuates the loss of body weight (BW) and cardiac hypertrophy. Pioglitazone treatment significantly reduces the elevated serum glucose levels and markedly improved the associated dyslipidemia. Furthermore, there is a slight but significant increase in serum creatinine level in D rats over their N controls (P <0.05). However, a marked renal dysfunction is observed in diabetic nephropathic (DN) group (P<0.05). Moreover, DN rats exhibits the highest serum activity of CK-MB, relative to both N and D rats (P<0.05). Pioglitazone is able to decrease the elevated serum levels of both creatinine and creatine kinase-MB (CK-MB)[4].
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
