Rosiglitazone (BRL 49653) - Moligand™, 10mM in DMSO , Agonist of FFA1 receptor;Agonist of Peroxisome proliferator-activated receptor-γ;Activator of TRPC5;Channel blocker of TRPM3, CAS No.122320-73-4, Agonist of FFA1 receptor;Agonist of Peroxisome proliferator-activated receptor-γ;Activator of TRPC5;Channel blocker of TRPM3

CAS: 122320-73-4 Cat. No.: R408369 Molecular Weight: 357.43 EC Number: 924-121-1 PubChem CID: 77999

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

5-​[[4-​[2-​(methyl-​2-​pyridinylamino)​ethoxy]​phenyl]​methyl]​-2,​4-​tiazolidinedione

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Rosiglitazone (BRL 49653) Rosiglitazone (BRL 49653) is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of P
In vitro

Rosiglitazone markedly increase phosphorylation of threonine 172 within the α subunit of AMPK, with increased AMP:ATP ratio. Rosiglitazone has been reported to decrease cholesterol synthesis in a number of cell lines in a peroxisome proliferator-activated receptor γ-independent manner. Rosiglitazone activates both α1- and α2-containing AMPK complexes, and this leads to a marked increase in the phosphorylation of acetyl-CoA carboxylase. Rosiglitazone activates PPAR-gamma2 which acts as a dominant inhibitor of osteoblastogenesis in murine bone marrow in vitro. Rosiglitazone increases adiponectin secretion from omental cells up to 2.3-fold higher, whereas secretion from subcutaneous adipose cells is unaffected. Rosiglitazone changes the morphological features and protein profiles of mitochondria in 3T3-L1 adipocytes.

In vivo

Rosiglitazone administration results in significant bone loss, including a decrease in bone volume, trabecular width, and trabecular number and an increase in trabecular spacing. Rosiglitazone also leads to a decrease in bone formation rate, with a simultaneous increase in fat content in the bone marrow. Rosiglitazone decreases the expression of the osteoblast-specific genes Runx2/Cbfa1, Dlx5, and alpha1(I)collagen, whereas the expression of the adipocyte-specific fatty acid binding protein aP2 is increased. Rosiglitazone upregulates gene transcripts encoding mitochondrial proteins in white adipocytes from ob/ob mice accompanied by an increase in mitochondrial mass and changes in mitochondrial structure.
Cell Data

cell lines：RAW 264.7 cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

5-​[[4-​[2-​(methyl-​2-​pyridinylamino)​ethoxy]​phenyl]​methyl]​-2, ​4-​tiazolidinedione

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Rosiglitazone (BRL 49653) is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone is a pure ligand of PPAR-gamma, and has no PPAR-a

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ACTIVATOR, AGONIST, CHANNEL BLOCKER

Mechanism of action

Agonist of FFA1 receptor;Agonist of Peroxisome proliferator-activated receptor-γ;Activator of TRPC5;Channel blocker of TRPM3

Names and Identifiers

• Isomeric SMILES: CN(CCOC1=CC=C(C=C1)CC2C(=O)NC(=O)S2)C3=CC=CC=N3
• WGK Germany: 3
• PubChem CID: 77999
• Molecular Weight: 357.43

Associated Targets(Human)

FFAR1 Tchem Free fatty acid receptor 1 (1 Activities)

Discover Target: FFAR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TRPC5 Tchem Short transient receptor potential channel 5 (1 Activities)

Discover Target: TRPC5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAOB Tclin Amine oxidase [flavin-containing] B (1 Activities)

Discover Target: MAOB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CISD1 Tchem CDGSH iron-sulfur domain-containing protein 1 (2 Activities)

Discover Target: CISD1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PPARA Tclin Peroxisome proliferator-activated receptor alpha (2 Activities)

Discover Target: PPARA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PPARG Tclin Peroxisome proliferator-activated receptor gamma (116 Activities)

Discover Target: PPARG

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Melt Point(°C): 156 °C

References

1. Zhuling Shao, Yanli Wu, Chengxu Gu, Yuyang Ma.  (2025)  Structural characterization and effects on carbohydrate and lipid metabolism of a novel marine exopolysaccharide from P. sclerotiorum isolated in the south china sea.  INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,      [PMID:40730309] [10.1016/j.ijbiomac.2025.146258]

2. Jiawen Ai, Weize Zhao, Quan Yu, Xiang Qian, Jianhua Zhou, Xinming Huo, Fei Tang.  (2023)  SR-Unet: A Super-Resolution Algorithm for Ion Trap Mass Spectrometers Based on the Deep Neural Network.  ANALYTICAL CHEMISTRY,      [PMID:37963290] [10.1021/acs.analchem.3c04172]

3. Zhang Shuai-nan, Liu Qi, Li Xu-zhao, Yang Wu-de, Zhou Ying.  (2023)  Cardioprotection of Eucommiae Folium: the extract and pharmaceutically active compounds attenuate hyperglycemia, mitochondrial dysfunction, calcium dyshomeostasis, insulin resistance, and oxidative stress in diabetic cardiomyopathy db/db mice.  JOURNAL OF PHARMACY AND PHARMACOLOGY,  75  (12): (1509-1520).  [PMID:37889854] [10.1093/jpp/rgad095]

4. Yongju Ye, Weimei Zhou, Yuefang Ren, Jiali Lu, Aixue Chen, Ruiying Jin, Feilan Xuan.  (2023)  The ameliorating effects of Guizhi Fuling Wan combined with rosiglitazone in a rat ovarian model of polycystic ovary syndrome by the PI3K/AKT/NF-κB and Nrf2/HO-1 pathways.  GYNECOLOGICAL ENDOCRINOLOGY,      [PMID:37706434] [10.1080/09513590.2023.2254848]

5. Ke Shenghui, Feng Yiwei, Luo Liying, Qin Wanzhao, Liu Huayu, Nie Jingchong, Liang Beijiang, Ma Hongjie, Xie Mao, Li Jingyu, Niu Zhijie, Li Guojian, Tang Anzhou, Xia Wei, He Guangyao.  (2023)  Isolation, identification, and induced differentiation of satellite cells from skeletal muscle of adult tree shrews.  IN VITRO CELLULAR & DEVELOPMENTAL BIOLOGY-ANIMAL,      [PMID:38127228] [10.1007/s11626-023-00836-5]

6. Shi Sun, Yifang Wang, Jinhu Li, Ailing Wu, Yan Xie, Zhao Wang, Xinjie Zhao, Dandan Wang, Xiaolong Wu, Xinguang Liu.  (2023)  Network Pharmacology-Based Approach to Investigate the Active Ingredients and Therapeutic Mechanisms of Jingu Tongxiao Pill against Osteoarthritis.  ACS Omega,      [PMID:37663478] [10.1021/acsomega.3c04724]

7. Jianv Wang, Jing Jia, Qingqing He, Yang Xu, Hongye Liao, Xia Xiong, Li Liu, Changzhen Sun.  (2023)  A novel multifunctional mitochondrion-targeting NIR fluorophore probe inhibits tumour proliferation and metastasis through the PPARγ/ROS/β-catenin pathway.  EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,      [PMID:37327679] [10.1016/j.ejmech.2023.115435]

8. Zhuling Shao, Yingying Tian, Shan Liu, Xiao Chu, Wenjun Mao.  (2023)  Anti-Diabetic Activity of a Novel Exopolysaccharide Produced by the Mangrove Endophytic Fungus Penicillium janthinellum N29.  Marine Drugs,  21  (5): (270).  [PMID:37233464] [10.3390/md21050270]

9. Yin Zhuang, Xiangying Sun, Siting Deng, Ya Wen, Qiujin Xu, Quanquan Guan.  (2023)  In vivo effects of low dose prenatal bisphenol A exposure on adiposity in male and female ICR offspring.  ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY,      [PMID:37105096] [10.1016/j.ecoenv.2023.114946]

10. Zixian He, Zhiwei Liu, Haihuan Xie, Pengjie Luo, Xiangmei Li.  (2023)  An Ultrasensitive Lateral Flow Immunoassay Based on Metal-Organic Framework-Decorated Polydopamine for Multiple Sulfonylureas Adulteration in Functional Foods.  Foods,  12  (3): (539).  [PMID:36766067] [10.3390/foods12030539]

11. Jingyi Hu, Yiheng Tong, Zhaofeng Shen, Yanan Li, Cheng Cheng, Ryan Au, Feng Xu, Yajun Liu, Lei Zhu, Hong Shen.  (2022)  Gegen Qinlian decoction ameliorates murine colitis by inhibiting the expansion of Enterobacteriaceae through activating PPAR-γ signaling.  BIOMEDICINE & PHARMACOTHERAPY,      [PMID:36007273] [10.1016/j.biopha.2022.113571]

12. Miaomiao Chi, Kunming Qin, Lei Cao, Min Zhang, Yingying Su, Xun Gao.  (2022)  Surface Functionalized Magnetic Nanoparticles as a Selective Sorbent for Affinity Fishing of PPAR-γ Ligands from Choerospondias axillaris.  MOLECULES,  27  (10): (3127).  [PMID:35630609] [10.3390/molecules27103127]

13. Haihuan Xie, Yingying Li, Jin Wang, Yi Lei, Anastasios Koidis, Xiangmei Li, Xing Shen, Zhenlin Xu, Hongtao Lei.  (2021)  Broad-specific immunochromatography for simultaneous detection of various sulfonylureas in adulterated multi-herbal tea.  FOOD CHEMISTRY,      [PMID:34536782] [10.1016/j.foodchem.2021.131055]

14. Lili Tan, Jie Lu, Limin Liu, Lu Li.  (2021)  Fatty acid binding protein 3 deficiency limits atherosclerosis development via macrophage foam cell formation inhibition.  EXPERIMENTAL CELL RESEARCH,      [PMID:34370993] [10.1016/j.yexcr.2021.112768]

15. Mei Wang, Shan-Quan Chang, Yu-Shan Tian, Ge-Qiang Zhang, Jin Qi.  (2020)  Zengye Decoction Ameliorates Insulin Resistance by Promoting Glucose Uptake.  REJUVENATION RESEARCH,  23  (5): (367-376).  [PMID:31941423] [10.1089/rej.2019.2228]

16. Tianlei Sun, Cheryl H. T. Kwong, Cheng Gao, Jianwen Wei, Ludan Yue, Jianxiang Zhang, Richard Dequan Ye, Ruibing Wang.  (2020)  Amelioration of ulcerative colitis via inflammatory regulation by macrophage-biomimetic nanomedicine.  Theranostics,      [PMID:32929337] [10.7150/thno.48448]

17. Zhishen Xie, Jianping Zhao, Hui Wang, Yali Jiang, Qiaoling Yang, Yu Fu, Huahui Zeng, Christian Hölscher, Jiangyan Xu, Zhenqiang Zhang.  (2020)  Magnolol alleviates Alzheimer's disease-like pathology in transgenic C. elegans by promoting microglia phagocytosis and the degradation of beta-amyloid through activation of PPAR-γ.  BIOMEDICINE & PHARMACOTHERAPY,      [PMID:32000045] [10.1016/j.biopha.2020.109886]

18. Tan Jianxin, Wang Yajun, Wang Siliang, Wu Simeng, Yuan Zhe, Zhu Xike.  (2019)  Label-free quantitative proteomics identifies transforming growth factor β1 (TGF-β1) as an inhibitor of adipogenic transformation in OP9-DL1 cells and primary thymic stromal cells.  Cell and Bioscience,  9  (1): (1-15).  [PMID:31249661] [10.1186/s13578-019-0311-1]

19. Jianxin Tan, Yajun Wang, Siliang Wang, Nannan Zhang, Simeng Wu, Zhe Yuan, Xike Zhu.  (2017)  Untargeted metabolomics analysis of adipogenic transformation in OP9-DL1 cells using liquid chromatography-mass spectrometry: Implications for thymic adipogenesis.  CELL BIOLOGY INTERNATIONAL,  41  (4): (447-456).  [PMID:28185342] [10.1002/cbin.10740]

20. Li Wang, Yi-Xiao Chen, Xin-Jing Meng, Hai-Yang Liang, Ya-Dan Zhang, Hui-Hui Zhou, Yu-Hang Liu, Xiao-Yu Chen, Zhen-Hua Liu, Shi-Ming Li, Wen-Yi Kang.  (2024)  Effects of undescribed iridoids in Patrinia punctiflora on insulin resistance in HepG2 cells.  FITOTERAPIA,      [PMID:39098734] [10.1016/j.fitote.2024.106160]

21. Chang Tang, Rui Tong, Guoqing Deng, Jing Yang, Yi Zhang, Zhifeng Cai.  (2024)  Fluorescent carbon dots for highly sensitive diosmetin sensing.  MICROCHEMICAL JOURNAL,      [PMID:] [10.1016/j.microc.2024.110362]

22. Peng Wang, Haifan Wang, Yang Xiao, Jialiang Zou, Hongping Chen, Lin Chen, Fu Wang, Yuan Hu, Youping Liu.  (2024)  Insights into metabolic characteristics and biological activity changes in Zangju (Citrus reticulata cv. Manau Gan) peel at different maturity stages through UPLC–MS/MS-based metabolomics.  Food Chemistry-X,      [PMID:38357370] [10.1016/j.fochx.2024.101197]

23. Chen Zhengfang, He Mudan, Wang Houpeng, Li Xuehui, Qin Ruirui, Ye Ding, Zhai Xue, Zhu Junwen, Zhang Quanqing, Hu Peng, Shui Guanghou, Sun Yonghua.  (2024)  Intestinal DHA-PA-PG axis promotes digestive organ expansion by mediating usage of maternally deposited yolk lipids.  Nature Communications,  15  (1): (1-15).  [PMID:39528516] [10.1038/s41467-024-54258-2]

24. Yujie Xiao, Yinghui Xu, Xianda Liu, Shengjun Cheng, Ran Wei, Weifeng Zhao, Changsheng Zhao.  (2024)  Simultaneous Rosiglitazone Release and Low-Density Lipoprotein Removal by Chondroitin Sodium Sulfate/Cyclodextrin/Poly(acrylic acid) Composite Adsorbents for Atherosclerosis Therapy.  BIOMACROMOLECULES,      [PMID:38687279] [10.1021/acs.biomac.4c00241]

25. Shuang Qi, Tingwei Zhang, Chaofeng Zhang, Bo Jiang, Caoxing Huang, Qiang Yong, Yongcan Jin.  (2024)  Sucrose-derived porous carbon catalyzed lignin depolymerization to obtain a product with application in type 2 diabetes mellitus.  INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES,      [PMID:39214225] [10.1016/j.ijbiomac.2024.135170]

26. Qing-qing Fang, Yang-jun Gu, Yong Wang, Zheng-cai Wang, Xiao-ying Lin, Kai Guo, Ze-ming Zhuang, Xin-cao Zhong, Li-yun Zhang, Jian Chen, Wei-qiang Tan.  (2025)  The therapeutic potential of Rosiglitazone in modulating scar formation through PPAR-γ pathway.  EUROPEAN JOURNAL OF PHARMACOLOGY,      [PMID:40054722] [10.1016/j.ejphar.2025.177445]

27. Wei Guo, Jian Han, Shengmin Wu, Xiongjie Shi, Qiangwei Wang, Bingsheng Zhou.  (2019)  Bis(2-ethylhexyl)-2,3,4,5-tetrabromophthalate Affects Lipid Metabolism in Zebrafish Larvae via DNA Methylation Modification.  ENVIRONMENTAL SCIENCE & TECHNOLOGY,      [PMID:31804803] [10.1021/acs.est.9b05796]

28. Huijun Yu, Xiao Xu, Xian Wang, Xiaonan Qiu, Qinxin Wang, Mengke Lu, Fengyi Du, Qi Guo, Miaomiao Zhang.  (2025)  Prussian-Blue-Functionalized Polypyrrole Nanozyme via PTEN Activation and Hypoxia Reversal for Enhanced Photothermal Therapy of Tumor.  ACS Biomaterials Science & Engineering,      [PMID:40454564] [10.1021/acsbiomaterials.5c00526]

29. Yue Li, Yayue Zhang, Xuran Ding, Taotao Zou, Hu Li, Ke Xu, Cheng Su, Yuting Wang, Ziming Zhao, Yuan He.  (2025)  Tailored platelet biomimetic delivery platform for targeted therapy of inflammatory bowel disease.  CHEMICAL ENGINEERING JOURNAL,      [PMID:] [10.1016/j.cej.2025.166357]

30. Shuang Qi, Hui Yang, Tian Fang, Tingwei Zhang, Bo Jiang, Sehrish Manan, Chaofeng Zhang, Peng Wang, Caoxing Huang, Wenjuan Wu, Yongcan Jin.  (2025)  Antioxidative Lignin Materials Attenuate Type 2 Diabetes Mellitus (T2DM) Progression by Preserving Glutathione via Insulin Receptor Substrate 1/Phosphoinositide 3-Kinase/Protein Kinase B (IRS1/PI3K/AKT) Axis.  Journal of Bioresources and Bioproducts,      [PMID:] [10.1016/j.jobab.2025.10.001]

31. Tian Ran, Zhang Tong, Dong Hao, Seim Inge, Yang Guang.  (2025)  Cetacean loss of the master adipose tissue regulator β3-adrenergic receptor may underlie their thick blubber and an Oligocene radiation and dispersal.  Nature Communications,  16  (1): (1-12).  [PMID:41107224] [10.1038/s41467-025-64288-z]

32. Hongyi Xian, Ruobing Bai, Yu Feng, Shiyue Tang, Zhiming Li, Chudan Gao, Kaiwei Li, Boxuan Liang, Yizhou Zhong, Yuji Huang, Hao Li, Yanhong Deng, Xiaohong Yang, Xiyun Huang, Xiaoqing Chen, Xingfen Yang, Zhenlie Huang.  (2025)  Aged polylactic acid microplastics exacerbate lipid metabolism disorders and cardiac dysfunction via PPARγ activation in zebrafish: A comparative study with polymers and oligomers.  ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY,      [PMID:41187537] [10.1016/j.ecoenv.2025.119337]

33. Xuan Liu, Xijuan Ren, Zhonghua Fan, Penghui Mao, Mingqing Qian, Tingting Qian, Ying Yang, Hui Liu, Li Wang.  (2025)  Metabolomics analysis reveals lipid metabolism disorders caused by triphenyltin via upregulation of PPARγ pathway.  ECOTOXICOLOGY AND ENVIRONMENTAL SAFETY,      [PMID:41207122] [10.1016/j.ecoenv.2025.119359]

34. Ren Yuanyuan, Cui Yue, Wang Zhen, Luo Yizhi, Jin Junchang, Yuan Yiyi, Li Xuan, Zhang Yaning, Cao Nan, Li Xiaofang, Yu Yi, Xiong Yuyan.  (2025)  ALDH3A2 negatively orchestrates gastric cancer progression through a synergistic induction of ferroptosis and ferroptosis-driven macrophage reprogramming.  Cell Death & Disease,      [PMID:41444219] [10.1038/s41419-025-08364-8]

35. Chong Gao, Wei Liu, Sai-Hu Liu, Shuang Zheng, Chen-Yu Wang, Xu Dai, Li-Hua Lian, Zhen-Yu Cui, Ji-Xing Nan, Yan-Ling Wu.  (2026)  Trigonelline regulates glycolysis and energy metabolism during hepatic fibrosis via Glut-1-HIF-1α axis: Focusing the interaction of macrophages and HSCs.  PHYTOMEDICINE,      [PMID:41579590] [10.1016/j.phymed.2026.157854]

36. Zhendong Yang, Tingyu Li, Wenyuan Su, Wangjing Zhai, Zhengzhe Wan, Yong Liang, Ting Ruan, Guibin Jiang.  (2026)  Exposure Profile and Combined Effects of Human PPARγ Agonists in Residential Indoor Dust from China.  ENVIRONMENTAL SCIENCE & TECHNOLOGY,      [PMID:41668385] [10.1021/acs.est.5c16973]

37. Yuchen Zheng, Zijia Liu, Zijie Zhao, Chao Sheng, Wenzhuo Li, Duo Tang, Yunlu Ning, Renhang Zhou, Ao Li, Zhixiang Zhou.  (2026)  Polystyrene nanoplastics promote adipogenesis by stimulating nuclear translocation of PPARγ.  FOOD AND CHEMICAL TOXICOLOGY,      [PMID:41763287] [10.1016/j.fct.2026.116030]

38. Jin Li, Mengyi Yang, Rui Xing, Jingmei Pan, Xing Guo, Shaobing Zhou.  (2026)  Reversing neuroinflammation in ischemic stroke through efferocytotic phenotype reprogramming with polymeric nanoparticles.  BIOMATERIALS,      [PMID:] [10.1016/j.biomaterials.2026.124156]

39. Zhenyu Wu, Xufang Huo, Yubing Huang, Taowu Gong, Pengcheng Zhao, Yuhang Zhu, Qingfan Zeng.  (2026)  AngII promotes hippocampal neuron ferroptosis via inhibiting the PPARγ/ACSL3 axis leading to hypertension-related cognitive impairment.  EXPERIMENTAL NEUROLOGY,      [PMID:] [10.1016/j.expneurol.2026.115755]