"目录号: HY-14600
NF-κBCell Cycle/DNA DamageAutophagy-
Rosiglitazone(BRL-49653C)马来酸盐是PPARγ高亲和性激动剂。
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生物活性
Description
Rosiglitazone maleate(BRL-49653C) is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ(PPARγ).IC50 Value: Target: PPARγin vitro: In competition experiments, rosiglitazone (BRL-49653), a potent antihyperglycemic agent, binds with high affinity to sites in intact adipocytes (IC50 = 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively) [1]. Rosiglitazone could induce AMP-activated protein kinase (AMPK) phosphorylation and reduce p70S6 kinase phosphorylation. Inhibition of AMPK impaired autophagy activation and enhanced palmitate-induced apoptosis during rosiglitazone treatment. Rosiglitazone-treated beta-cells were more resistant to palmitate-induced apoptosis. The conversion of LC3-I to LC3-II and accumulated autophagosomes were found to be upregulated in rosiglitazone-treated cells [2]. in vivo: In LFD mice with AP, Rosiglitazone(RGZ) significantly worsened the degree of intrapancreatic acinar and fat necrosis as well as visceral fat saponification, without affecting other parameters of disease severity or inflammation. Induction of AP lead to major suppression of adiponectin levels at Day 7 in both HFD and HFD + RGZ mice [3]. Rosiglitazone treatment of db/db mice normalized hyperglycemia, attenuated renal injury and decreased urinary ACE2 and renal ADAM17 protein expression [4]. Chronic administration of RSG (10 mg/kg/day, i.p) significantly improved motor function and attenuated hyperglycemia in N171-82Q HD mice. RSG administration rescued brain derived neurotrophic factor(BDNF) deficiency in the cerebral cortex, and prevented loss of orexin-A-immunopositive neurons in the hypothalamus of N171-82Q HD mice [5].Toxicity:
Clinical Trial
Massachusetts General Hospital-Dana-Farber Cancer Institute
Adenocarcinoma of the Prostate-Prostate Cancer
September 2000
Phase 3
Mutual Pharmaceutical Company, Inc.-Cetero Research, San Antonio
Healthy
September 2008
Phase 1
James Lewis-National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)-GlaxoSmithKline-University of Pennsylvania
Ulcerative Colitis-Inflammatory Bowel Disease
September 2002
Phase 2
Exelixis
Papillary Thyroid Cancer-Follicular Thyroid Cancer-Huerthle Cell Thyroid Cancer-Renal Cell Carcinoma
April 2010
Phase 1
Dr. Milan Gupta-GlaxoSmithKline-Canadian Collaborative Research Network
Type 2 Diabetes Mellitus
April 2006
Radboud University-GlaxoSmithKline
Ischemia-Reperfusion Injury-The Metabolic Syndrome
April 2007
Phase 2
Laval University-GlaxoSmithKline
Diabetes-Coronary Artery Bypass Grafting
June 2003
Phase 3
University of Washington-National Institute on Aging (NIA)-GlaxoSmithKline
Mild Cognitive Impairment
June 2006
Phase 2
Centro de Investigacao em Saude de Manhica-University Health Network, Toronto-Barcelona Institute for Global Health
Malaria
February 2016
University of Texas Southwestern Medical Center-GlaxoSmithKline
Insulin Sensitivity
February 2004
Phase 4
Brooke Army Medical Center-InterMune
Hepatitis C
October 2005
Phase 4
GlaxoSmithKline
Non-insulin-dependent Diabetes Mellitus
September 2002
Phase 3
China Medical University Hospital
Type 2 Diabetes Mellitus With Features of Insulin Resistance
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Ahmad Slim-GlaxoSmithKline-Brooke Army Medical Center
Hypertriglyceridemia in Type 4 Hyperlipidemia-Non Diabetic Subjects With Normoglycemia
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Phase 4
National Institute of Allergy and Infectious Diseases (NIAID)-GlaxoSmithKline
HIV Infections
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Dana-Farber Cancer Institute-National Cancer Institute (NCI)
Sarcoma
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Turku University Hospital-SmithKline Beecham
Insulin Sensitivity-Type 2 Diabetes
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National Cancer Institute (NCI)
Oral Leukoplakia
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Phase 2
Jonsson Comprehensive Cancer Center-National Cancer Institute (NCI)
Brain and Central Nervous System Tumors
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GlaxoSmithKline
Alzheimer's Disease
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University of Texas Southwestern Medical Center-GlaxoSmithKline-Biosite
Diabetes Mellitus, Type 2
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Seoul St. Mary's Hospital-GlaxoSmithKline
NASH (Non-alcoholic Steato-hepatitis)
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Radboud University
Insulin Resistance
February 2006
University of Massachusetts, Worcester-GlaxoSmithKline
Metabolic Syndrome-Insulin Resistance
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Phase 2
University of Aarhus
Change in Bone Mineral Density-Change in Bone Marrow Fat Content
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Phase 2
Massachusetts General Hospital-National Alliance for Research on Schizophrenia and Depression-Stanley Medical Research Institute
Schizophrenia
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Creighton University
Asthma
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Baskent University
Diabetes Mellitus, Type 2
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GlaxoSmithKline
Diabetes Mellitus, Type 2
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Denver Research Institute-GlaxoSmithKline
Impaired Glucose Tolerance
March 2004
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Beth Israel Medical Center
Chronic Hepatitis C Infection-Fatty Liver
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Aristotle University Of Thessaloniki-University of Athens
Type II Diabetes Mellitus
January 2005
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Yale University
Obesity-Impaired Glucose Tolerance-Type 2 Diabetes Mellitus
November 2005
AstraZeneca-Eli Lilly and Company
Diabetes Mellitus, Type 2
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GlaxoSmithKline
Diabetes Mellitus, Type 2
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VIVUS, Inc.
Erectile Dysfunction
April 2010
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Stanford University
Depression-Bipolar Disorder-Insulin Resistance
July 2007
GlaxoSmithKline
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Phase 3
GlaxoSmithKline
Type 2 Diabetes Mellitus-Diabetes Mellitus, Type 2
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GlaxoSmithKline
Alzheimer's Disease
May 2004
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Jonsson Comprehensive Cancer Center-National Cancer Institute (NCI)
Cushing's Disease
April 2007
Phase 2
University of Glasgow-GlaxoSmithKline-Chest, Heart and Stroke Association Scotland-Chief Scientist Office of the Scottish Government
Asthma
July 2005
Phase 2-Phase 3
GlaxoSmithKline
Diabetes Mellitus, Type 2
April 2010
Phase 3
GlaxoSmithKline
Alzheimer's Disease
April 2008
Phase 1
GlaxoSmithKline
Diabetes Mellitus, Type 2
January 2000
Phase 3
