Delving into the Latest Updates on Rosiglitazone Sodium with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

太罗

Target

PPARγ

Action

agonists

Mechanism

PPARγ agonists(Peroxisome proliferator-activated receptor γ agonists), Insulin sensitizers

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Diabetes Mellitus, Type 2

Inactive Indication-

Originator Organization

Taiji Group Co. Ltd.

Active Organization

Taiji Group Co. Ltd.

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date

China (14 Sep 2004),

Diabetes Mellitus, Type 2

Regulation-

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Structure/Sequence

Molecular FormulaC18H19N3NaO3S

InChIKeyMIXMIJXAFUYUNO-UHFFFAOYSA-N

CAS Registry316371-83-2

View All Structures (2)

Di-(2-ethylhexyl) phthalate (DEHP) is one of the most extensively used phthalate and poses a public health concern. Perinatal exposure to DEHP has been shown to cause neurodevelopmental abnormalities and neurobehavioral disorders in offspring. However, the precise molecular mechanism has not yet been fully elucidated. In this study, pregnant C57BL/6 mice were exposed to DEHP from gestation to weaning. By RNA sequencing and animal experiments, ferroptosis has been identified as the key pathologic process contributing to DEHP-induced hippocampal injury in adult male offspring. In vitro results also showed that Ferrostatin-1 (Fer-1) effectively ameliorated Mono-(2-ethylhexyl) phthalate (MEHP) -induced cell survival via the inhibiting ferroptosis in HT22 cells. Consistently, we found that the expression of ACSL4 and TFR was significantly up-regulated in offspring hippocampi and MEHP-exposed HT22 neurons. However, silencing ACSL4 or knockdown TFR relieved MEHP-induced generation of lipid ROS and cellular iron accumulation, thereby blocking ferroptosis. Mechanistically, ACSL4/TFR-mediated ferroptosis seemed to be a Yes-associated protein (YAP) dependent via TEA domain transcription factor 4 in HT22 neurons. Importantly, treatment with Fer-1, rosiglitazone, and Deferoxamine effectively rescued DEHP-evoked cognitive decline in adult male offspring. Our findings certified that gestational and lactational exposure to DEHP provoked ACSL4/TFR-mediated hippocampal neuronal ferroptosis via YAP activation.

01 Jun 2025·European Journal of Pharmacology

The therapeutic potential of Rosiglitazone in modulating scar formation through PPAR-γ pathway

Article

Author: Lin, Xiao-Ying ; Gu, Yang-Jun ; Tan, Wei-Qiang ; Zhong, Xin-Cao ; Wang, Zheng-Cai ; Zhuang, Ze-Ming ; Fang, Qing-Qing ; Wang, Yong ; Zhang, Li-Yun ; Guo, Kai ; Chen, Jian

The prevention and treatment of scars has always posed a challenge in the medical field. Researchers have reached the consensus that safe, effective and affordable treatments are needed. Here, by conducting non-targeted metabolomics and RNA sequencing experiments, we revealed that a significant number of metabolites and genes related to glucose and lipid metabolism underwent changes during scar formation, with peroxisome proliferator-activated receptor-γ (PPAR-γ) exerting a profound influence. Considering that rosiglitazone is a selective orally active PPAR-γ receptor agonist, scar models were induced in rats, and rosiglitazone was administered at different dosages. We characterized rosiglitazone as a crucial mediator in a rat scar model in vivo and in vitro in two models of transforming growth factor β1(TGF-β1) stimulated fibroblasts (NIH 3T3 and 3T3 L1). Functionally, activation of PPAR-γ with rosiglitazone effectively impedes fibrosis and mitigates scar formation. Rosiglitazone also inhibits some inflammatory factors, and downregulates triglyceride, lactic acid, glycogen and lactic dehydrogenase levels in rat scars. Conversely, rosiglitazone increases adenosine triphosphate (ATP) production and increases free fatty acid levels and the activity of acetyl-CoA carboxylase, fatty acid synthetase, succinate dehydrogenase. Collectively, these findings shed light on the underlying mechanisms and suggest that the use of rosiglitazone could be a promising therapeutic approach to alleviate fibrosis and reduce scar formation.

01 Jun 2025·Journal of Equine Veterinary Science

Metformin and rosiglitazone affect motility, lipid peroxidation and mitochondrial activity of thawed equine spermatozoa

Article

Author: Vargas, Santiago ; Restrepo, Giovanni ; Tobón, María Camila ; Vergara, Ana Karina ; Rojano, Benjamín ; Usuga, Alexandra

Maintaining sperm energy homeostasis in vitro is very important to improve the efficacy of stallion sperm preservation. Equine spermatozoa preferentially utilize oxidative phosphorylation over glycolysis to generate ATP. Metformin and rosiglitazone are antidiabetic compounds that enhances metabolic flexibility and glucose utilization. The aim of this study was to evaluate metformin and rosiglitazone supplementation of the freezing medium on quality and oxidative status of thawed stallion semen. A total of 15 ejaculates from five horses were collected and supplemented before freezing with metformin at 20 (M20), 50 (M50) and 100 mM (M100) and with rosiglitazone at 10 (R10), 50 (R50) and 100 µM (R100). A control group without supplementation was added. Semen cryopreservation was performed using a programable freezing protocol. Post-thaw, motility and kinetics, vitality (SV), morphology, plasma membrane integrity (PMI), mitochondria membrane potential (ΔΨM), reactive oxygen species (ROS) and lipid peroxidation (LP) of sperm were evaluated. Mixed models were adjusted and means were compared using Tukey tests. Total motility of post-thawed semen increased with M20; M100 reduced motility and most of the sperm kinetic parameters, as well as SV and PMI (p < 0.05). A reduction in LP was observed with M20 and R100; also, M100 produced a higher population of spermatozoa with low and high ΔΨM (p < 0.05). No treatment, except R50, generated an overproduction of ROS. In conclusion, a dose of 20 mM metformin in the freezing extender for stallion semen could improve total motility and reduce lipid peroxidation of thawed spermatozoa.

100 Deals associated with Rosiglitazone Sodium

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External Link

KEGG	Wiki	ATC	Drug Bank
-	-	A10BG02	-

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	China	Taiji Group Co. Ltd.	14 Sep 2004

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00577590 (T2DM, CTgov)	Not Applicable	Diabetes Mellitus, Type 2	78	Lovaza+Metformin (Metformin and Lovaza)	iufrsenzea(sokgwqsvyn) = wpepdirisa cwbbmcewuc (fgfufkdseg, ltbrksajzf - eyokedlbxy) View more	-	31 Aug 2018
				Rosiglitazone+Metformin (Metformin and Rosiglitazone)	iufrsenzea(sokgwqsvyn) = chqrgkrrko cwbbmcewuc (fgfufkdseg, jxgmqrzewd - bgxjphhzsz) View more