"目录号: HY-14601
Cell Cycle/DNA DamageNF-κB-
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。
PPAR
相关产品
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
NCT00494559
Korea University Anam Hospital
Diabetes Mellitus-Coronary Artery Stenosis
July 2007
Phase 4
NCT03080480
Children's Hospital of Fudan University
Chronic Granulomatous Disease
September 1, 2017
Phase 1-Phase 2
NCT01090752
University Hospital, Geneva-University of Lausanne Hospitals
Diabetes-Hypertension
October 2005
Phase 4
NCT02687425
Meng Li-Tongji Hospital
Leukemia, Myelogenous, Chronic, BCR-ABL Positive
February 2016
Phase 2
NCT00671515
Joseph Calabrese, MD-Takeda Pharmaceuticals North America, Inc.-University Hospitals Cleveland Medical Center
Depressive Disorder, Major-Metabolic Syndrome X
April 2008
Phase 2
NCT02697617
Indiana University
Polycystic Kidney Disease
October 2015
Phase 2
NCT00719381
Paul Beringer-University of Southern California
Cystic Fibrosis
January 2008
Phase 1
NCT01151670
Wake Forest University Health Sciences
Brain Neoplasms, Malignant-Brain Neoplasms, Benign-Malignant Meningioma-Glioblastoma Multiforme-Anaplastic Astrocytoma
August 2010
Phase 1
NCT01352182
Children's Hospital Medical Center, Cincinnati
Severe Sepsis-Septic Shock
October 2011
Phase 1-Phase 2
NCT01637935
Takeda-Kaiser Permanente-Department of Epidemiology at University of Pennsylvania
Diabetes-Bladder Cancer
July 2004
NCT00811681
Assistance Publique - Hôpitaux de Paris
Friedreich's Ataxia
December 2008
Phase 3
NCT01931566
Takeda-Zinfandel Pharmaceuticals Inc.
Mild Cognitive Impairment Due to Alzheimer's Disease
August 2013
Phase 3
NCT01068444
Kaohsiung Medical University Chung-Ho Memorial Hospital
Hepatitis
April 2009
Phase 2
NCT02958956
Takeda
Diabetes Mellitus, Type 2, Cancer
January 1997
NCT01935804
King Abdulaziz University
Diabetes Mellitus-Diabetes Mellitus, Type 2-Glucose Metabolism Disorders
January 2009
Phase 2
NCT00835120
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
NCT00845182
The University of Texas Health Science Center at San Antonio
Type 2 Diabetes-Healthy-Impaired Glucose Tolerance
June 2007
Phase 4
NCT01972724
Takeda
Type II Diabetes Mellitus
January 2014
Phase 4
NCT01882907
Pusan National University Hospital
Type 2 Diabetes
December 2009
Phase 4
NCT02133625
Dana-Farber Cancer Institute
Advanced Solid Tumor-Metastatic Solid Tumor
August 2011
Phase 1
NCT01001013
LG Life Sciences
Healthy
February 2009
Phase 1
NCT00855010
University of Texas Southwestern Medical Center-National Institutes of Health (NIH)
Obesity-Type 2 Diabetes
February 2009
NCT01258322
Huashan Hospital-Baxter Healthcare Corporation
Peritoneal Dialysis-Pioglitazone-Hypertriglyceridemia-Insulin Resistance-Inflammation
January 2008
NCT00861341
University of Rochester
Diabetes-Platelet Function-Healthy
December 2008
Phase 2
NCT01223196
The University of Texas Health Science Center at San Antonio
Type 2 Diabetes
August 2009
Phase 4
NCT01186250
Stanford University
Cardiac Allograft Vasculopathy
July 2010
Phase 2
NCT02284906
Takeda
Mild Cognitive Impairment Due to Alzheimer's Disease
November 17, 2014
Phase 3
NCT03060772
Emory University-National Institute on Alcohol Abuse and Alcoholism (NIAAA)
Alcoholism
August 28, 2017
Phase 2
NCT01935466
Postgraduate Institute of Medical Education and Research
Bladder Cancer
July 2013
NCT01819402
Kurume University
To Evaluate the Effect of Pioglitazone on Glucose Metabolism of Fat Tissue by Using FDG-PET/CT Imaging
March 2012
NCT00770367
Dana King-Takeda Pharmaceuticals North America, Inc.-Medical University of South Carolina
Diabetes
October 2008
Phase 4
NCT02730195
Emory University
Chronic Myelogenous Leukemia, BCR-ABL1 Positive-Recurrent Chronic Myelogenous Leukemia, BCR-ABL1 Positive
May 2016
Phase 2
NCT00099021
National Cancer Institute (NCI)
Head and Neck Cancer-Oral Leukoplakia
June 2003
Phase 2
NCT01396564
Coordinación de Investigación en Salud, Mexico
Type 2 Diabetes
October 2005
Phase 1-Phase 2
NCT02181842
Takeda
Type 2 Diabetes Mellitus
January 2009
NCT01156597
University of Miami-Takeda Pharmaceuticals North America, Inc.
Type 2 Diabetes Mellitus
April 2008
Phase 3
NCT01280123
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
NCT00782795
University of Michigan-National Institute on Alcohol Abuse and Alcoholism (NIAAA)
Chronic Pancreatitis-Insulin Resistance-Normal Stool Fat Levels
November 2008
Phase 2
NCT01589445
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
NCT00609856
Skane University Hospital-Medical Research Council-Skane County Council Research & Development Foundation
Type 2 Diabetes-Secondary Drug Failure
April 2004
Phase 4
NCT00545857
Stony Brook University
Type 1 Diabetes Mellitus
June 2002
Phase 1
NCT01082120
AstraZeneca
Type 2 Diabetes Mellitus
February 2010
Phase 1
NCT00676260
Takeda
Diabetes Mellitus
December 2002
Phase 2
NCT00174993
Takeda-Eli Lilly and Company
Diabetes Mellitus
May 2001
Phase 3
NCT01195090
Sung-Chen Liu-Mackay Memorial Hospital
Type 2 Diabetes