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Formula | C18H19N3O3S |
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Molecular Weight | 357.43 | CAS No. | 122320-73-4 | ||||
Solubility (25°C)* | In vitro | DMSO | 71 mg/mL (198.64 mM) | ||||
Water | Insoluble | ||||||
Ethanol | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Rosiglitazone 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-alpha-binding action. Rosiglitazone modulates TRP channels and induces autophagy. Rosiglitazone prevents ferroptosis. | |||
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Targets |
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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. [1] Rosiglitazone activates PPAR-gamma2 which acts as a dominant inhibitor of osteoblastogenesis in murine bone marrow in vitro.[2] Rosiglitazone increases adiponectin secretion from omental cells up to 2.3-fold higher, whereas secretion from subcutaneous adipose cells is unaffected. [3] Rosiglitazone changes the morphological features and protein profiles of mitochondria in 3T3-L1 adipocytes. [4] |
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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. [2] 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. [4] |
Animal Study: |
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Data from [J Leukoc Biol, 2014, 95(4), 587-98]
Data from [J Leukoc Biol, 2014, 95(4), 587-98]
Data from [Data independently produced by , , Theranostics, 2018, 8(15):4262-4278]
Data from [Data independently produced by , , Cancer Sci, 2018, 109(7):2243-2255]
Pro-ferroptotic signaling promotes arterial aging via vascular smooth muscle cell senescence [ Nat Commun, 2024, 15(1):1429] | PubMed: 38365899 |
Adipocyte inflammation is the primary driver of hepatic insulin resistance in a human iPSC-based microphysiological system [ Nat Commun, 2024, 15(1):7991] | PubMed: 39266553 |
Brain Short-Chain Fatty Acids Induce ACSS2 to Ameliorate Depressive-Like Behavior via PPARγ-TPH2 Axis [ Research (Wash D C), 2024, 7:0400] | PubMed: 38939042 |
TCP1 expression alters the ferroptosis sensitivity of diffuse large B-cell lymphoma subtypes by stabilising ACSL4 and influences patient prognosis [ Cell Death Dis, 2024, 15(8):611] | PubMed: 39174525 |
Calpain-1 Up-Regulation Promotes Bleomycin-Induced Pulmonary Fibrosis by Activating Ferroptosis [ Am J Pathol, 2024, S0002-9440(24)00356-0] | PubMed: 39326733 |
Celastrol Stabilizes Glycolipid Metabolism in Hepatic Steatosis by Binding and Regulating the Peroxisome Proliferator-Activated Receptor γ Signaling Pathway [ Metabolites, 2024, 14(1)64] | PubMed: 38276299 |
LCN2 secreted by tissue-infiltrating neutrophils induces the ferroptosis and wasting of adipose and muscle tissues in lung cancer cachexia [ J Hematol Oncol, 2023, 16(1):30] | PubMed: 36973755 |
LCN2 secreted by tissue-infiltrating neutrophils induces the ferroptosis and wasting of adipose and muscle tissues in lung cancer cachexia [ J Hematol Oncol, 2023, 16(1):30] | PubMed: 36973755 |
Blockade of IL-6R prevents preterm birth and adverse neonatal outcomes [ EBioMedicine, 2023, 10.1016/j.ebiom.2023.104865] | PubMed: 37944273 |
KLF2/PPARγ axis contributes to trauma-induced heterotopic ossification by regulating mitochondrial dysfunction [ Cell Prolif, 2023, e13521.] | PubMed: 37340819 |
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