Rosiglitazone maleate

"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。

PPARAutophagy

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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

NCT00182052

Massachusetts General Hospital-Dana-Farber Cancer Institute

Adenocarcinoma of the Prostate-Prostate Cancer

September 2000

Phase 3

NCT00785213

Mutual Pharmaceutical Company, Inc.-Cetero Research, San Antonio

Healthy

September 2008

Phase 1

NCT00065065

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

NCT01100619

Exelixis

Papillary Thyroid Cancer-Follicular Thyroid Cancer-Huerthle Cell Thyroid Cancer-Renal Cell Carcinoma

April 2010

Phase 1

NCT00486187

Dr. Milan Gupta-GlaxoSmithKline-Canadian Collaborative Research Network

Type 2 Diabetes Mellitus

April 2006

NCT00405015

Radboud University-GlaxoSmithKline

Ischemia-Reperfusion Injury-The Metabolic Syndrome

April 2007

Phase 2

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Laval University-GlaxoSmithKline

Diabetes-Coronary Artery Bypass Grafting

June 2003

Phase 3

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University of Washington-National Institute on Aging (NIA)-GlaxoSmithKline

Mild Cognitive Impairment

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Centro de Investigacao em Saude de Manhica-University Health Network, Toronto-Barcelona Institute for Global Health

Malaria

February 2016

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University of Texas Southwestern Medical Center-GlaxoSmithKline

Insulin Sensitivity

February 2004

Phase 4

NCT00207402

Brooke Army Medical Center-InterMune

Hepatitis C

October 2005

Phase 4

NCT00231387

GlaxoSmithKline

Non-insulin-dependent Diabetes Mellitus

September 2002

Phase 3

NCT01577095

China Medical University Hospital

Type 2 Diabetes Mellitus With Features of Insulin Resistance

April 2006

Phase 2

NCT00819910

Ahmad Slim-GlaxoSmithKline-Brooke Army Medical Center

Hypertriglyceridemia in Type 4 Hyperlipidemia-Non Diabetic Subjects With Normoglycemia

September 2008

Phase 4

NCT00367744

National Institute of Allergy and Infectious Diseases (NIAID)-GlaxoSmithKline

HIV Infections

July 2006

Phase 2

NCT00004180

Dana-Farber Cancer Institute-National Cancer Institute (NCI)

Sarcoma

October 1999

Phase 2

NCT02526615

Turku University Hospital-SmithKline Beecham

Insulin Sensitivity-Type 2 Diabetes

October 2000

Phase 4

NCT00369174

National Cancer Institute (NCI)

Oral Leukoplakia

June 2006

Phase 2

NCT00616642

Jonsson Comprehensive Cancer Center-National Cancer Institute (NCI)

Brain and Central Nervous System Tumors

October 2006

Phase 2

NCT00381238

GlaxoSmithKline

Alzheimer's Disease

June 20, 2006

Phase 2

NCT00424762

University of Texas Southwestern Medical Center-GlaxoSmithKline-Biosite

Diabetes Mellitus, Type 2

February 2005

Phase 4

NCT01406704

Seoul St. Mary's Hospital-GlaxoSmithKline

NASH (Non-alcoholic Steato-hepatitis)

January 2004

Phase 4

NCT00285805

Radboud University

Insulin Resistance

February 2006

NCT01150981

University of Massachusetts, Worcester-GlaxoSmithKline

Metabolic Syndrome-Insulin Resistance

November 2006

Phase 2

NCT00609362

University of Aarhus

Change in Bone Mineral Density-Change in Bone Marrow Fat Content

January 2008

Phase 2

NCT00337350

Massachusetts General Hospital-National Alliance for Research on Schizophrenia and Depression-Stanley Medical Research Institute

Schizophrenia

September 2003

Phase 4

NCT00614874

Creighton University

Asthma

December 2008

Phase 2

NCT00290394

Baskent University

Diabetes Mellitus, Type 2

March 2004

Phase 4

NCT01195259

GlaxoSmithKline

Diabetes Mellitus, Type 2

October 2009

NCT00733174

Denver Research Institute-GlaxoSmithKline

Impaired Glucose Tolerance

March 2004

Phase 4

NCT00274495

Beth Israel Medical Center

Chronic Hepatitis C Infection-Fatty Liver

January 2006

Phase 4

NCT00306176

Aristotle University Of Thessaloniki-University of Athens

Type II Diabetes Mellitus

January 2005

Phase 4

NCT00413335

Yale University

Obesity-Impaired Glucose Tolerance-Type 2 Diabetes Mellitus

November 2005

NCT00135330

AstraZeneca-Eli Lilly and Company

Diabetes Mellitus, Type 2

October 2005

Phase 3

NCT00500955

GlaxoSmithKline

Diabetes Mellitus, Type 2

April 2000

Phase 3

NCT01415128

VIVUS, Inc.

Erectile Dysfunction

April 2010

Phase 1

NCT00333723

GlaxoSmithKline

Diabetes Mellitus, Type 2

July 2000

Phase 4

NCT00242619

Stanford University

Depression-Bipolar Disorder-Insulin Resistance

July 2007

NCT00523913

GlaxoSmithKline

Diabetes Mellitus, Type 2

November 2005

Phase 3

NCT00349427

GlaxoSmithKline

Type 2 Diabetes Mellitus-Diabetes Mellitus, Type 2

October 2005

Phase 3

NCT00265148

GlaxoSmithKline

Alzheimer's Disease

May 2004

Phase 2

NCT00612066

Jonsson Comprehensive Cancer Center-National Cancer Institute (NCI)

Cushing's Disease

April 2007

Phase 2

NCT00119496

University of Glasgow-GlaxoSmithKline-Chest, Heart and Stroke Association Scotland-Chief Scientist Office of the Scottish Government

Asthma

July 2005

Phase 2-Phase 3

NCT01453049

GlaxoSmithKline

Diabetes Mellitus, Type 2

April 2010

Phase 3

NCT00688207

GlaxoSmithKline

Alzheimer's Disease

April 2008

Phase 1

NCT00279045

GlaxoSmithKline

Diabetes Mellitus, Type 2

January 2000

Phase 3

NCT00550420

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