Rosiglitazone

Catalog No.S2556 Batch:S255603

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Technical Data

Formula

C18H19N3O3S

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
* <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.)

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Biological Activity

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.
Targets
PPAR [1]
(Cell-free assay)
TRPC [5] Ferroptosis [6]
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]

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]

Protocol (from reference)

Animal Study:

[8]

  • Animal Models

    Male Sprague dawely rats

  • Dosages

    5 mg/kg

  • Administration

    p.o.

Customer Product Validation

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]

Selleck's Rosiglitazone has been cited by 76 publications

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
Establishment of goat mammary organoid cultures modeling the mammary gland development and lactation [ J Anim Sci Biotechnol, 2024, 15(1):124] PubMed: 39350237
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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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