Rosiglitazone (BRL 49653)

CatalogusnummerS2556 Batch:S255606

Afdrukken

Technische gegevens

Formule

C18H19N3O3S
Moleculair gewicht 357.43 CAS-nr. 122320-73-4
Oplosbaarheid (25°C)* In vitro DMSO 71 mg/mL (198.64 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Voeg oplosmiddelen afzonderlijk en in volgorde toe aan het product.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
4%DMSO 30%PEG300 5%Tween80 61%ddH2O

Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor maatwerktesten.

 5.000mg/ml (13.99mM) Taking the 1 mL working solution as an example, add 40 μL of 125 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 610 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml betekent licht oplosbaar of onoplosbaar.
* Houd er rekening mee dat Selleck de oplosbaarheid van alle verbindingen intern test en de werkelijke oplosbaarheid enigszins kan afwijken van gepubliceerde waarden. Dit is normaal en is te wijten aan lichte batch-tot-batch variaties.
* Verzending op kamertemperatuur (Stabiliteitstests tonen aan dat dit product zonder koelmaatregelen kan worden verzonden.)

Voorbereiden van stamoplossingen

Biologische activiteit

Beschrijving Rosiglitazone is een potent antihyperglycemisch middel en een potente thiazolidinedion insuline sensitizer met IC50 van 12, 4 en 9 nM voor respectievelijk rat-, 3T3-L1- en humane adipocyten. Rosiglitazone is een pure ligand van PPAR-gamma en heeft geen PPAR-alpha-bindende werking. Rosiglitazone moduleert TRP channels en induceert autophagy. Rosiglitazone voorkomt ferroptosis.
Doelen
PPAR
(Cell-free assay)		 TRPC Ferroptosis
In vitro

Rosiglitazone markedly increase phosphorylation of threonine 172 within the α subunit of AMPK, with increased AMP:ATP ratio. This compound has been reported to decrease cholesterol synthesis in a number of cell lines in a peroxisome proliferator-activated receptor γ-independent manner. It activates both α1- and α2-containing AMPK complexes, and this leads to a marked increase in the phosphorylation of acetyl-CoA carboxylase.

This chemical activates PPAR-gamma2 which acts as a dominant inhibitor of osteoblastogenesis in murine bone marrow in vitro.

It increases adiponectin secretion from omental cells up to 2.3-fold higher, whereas secretion from subcutaneous adipose cells is unaffected.

This compound 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. This compound also leads to a decrease in bone formation rate, with a simultaneous increase in fat content in the bone marrow. It 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.

This chemical 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.

Protocol (uit referentie)

Dierstudie:

[8]
  • Dierlijke modellen

    Male Sprague dawely rats

  • Doseringen

    5 mg/kg

  • Toediening

    p.o.

Referenties

  • https://pubmed.ncbi.nlm.nih.gov/11994296/
  • https://pubmed.ncbi.nlm.nih.gov/14500573/
  • https://pubmed.ncbi.nlm.nih.gov/12466369/
  • https://pubmed.ncbi.nlm.nih.gov/15520860/
  • https://pubmed.ncbi.nlm.nih.gov/21406603/
  • https://pubmed.ncbi.nlm.nih.gov/30737476/
  • https://pubmed.ncbi.nlm.nih.gov/35131600/
  • https://pubmed.ncbi.nlm.nih.gov/28892640/

Klantproductvalidatie

Gegevens van [ J Leukoc Biol , 2014 , 95(4), 587-98 ]

Gegevens van [ J Leukoc Biol , 2014 , 95(4), 587-98 ]

BV2 cells were pretreated with JuA for 30 min, followed by administration of Aβ42 (5 μM) for 12 h. Cells were fixed and immunostained with PPARγ antibody. The representative images demonstrate the amount and localization of PPARγ (green). Nuclei were counterstained with DAPI (blue). Scale bar: 40 μm.

Gegevens van [ , , Theranostics, 2018, 8(15):4262-4278 ]

Rosiglitazone normalizes colon carcinoma vasculature and reduces tumor‐associated macrophage (TAM) infiltration. When CT26 tumor size approximately reached 50 mm3, the mice were given 100 mg/kg rosiglitazone or vehicle by oral gavage per day for 2 weeks. Then, the tumor samples were collected. A, Microvascular density and pericyte coverage were investigated by double immunofluorescence staining for CD31 and NG2. Scale bar, 50 μm. B, Multiphoton laser‐scanning microscopy images of CT26 tumor vasculature (green) stained with FITC‐dextran. Scale bar, 100 mm. C, Tumor vessel perfusion indicated by CD31‐positive endothelial cells stained red; FITC‐lectin perfused vessels are stained green. Scale bar, 50 μm. D, Representative micrographs show pimonidazole (PIMO)‐stained (green) CT26 tumor sections for hypoxia study. Scale bar, 100 μm. Hypoxic tumor regions are highlighted by dashed lines. E, Immunofluorescence staining for F4/80 showing TAM infiltration. Scale bar, 50 μm. Immunofluorescence images from (A to E) were captured within randomly selected fields (4‐6 fields per tumor, n = 6 mice). Data are presented mean ± SEM. **P < .01; ***P < .001

Gegevens van [ , , Cancer Sci, 2018, 109(7):2243-2255 ]

Selleck's Rosiglitazone (BRL 49653) Is geciteerd door 80 Publicaties

EBF2 condensates enable adipose thermogenesis through ZFP423 sequestration and epigenetic remodeling [ Nat Commun, 2026, 17(1):5607] PubMed: 42026085
Adipocytes orchestrate obesity-related chronic inflammation through β2-microglobulin [ Signal Transduct Target Ther, 2025, 10(1):394] PubMed: 41330906
Vesicle-associated membrane protein 5 is an intrinsic defense factor for embryonic stem cells against coronaviruses [ Nat Commun, 2025, 16(1):6241] PubMed: 40624080
Compromised Peroxisome Proliferator-Activated Receptor γ-Mediated Impaired Placental Glucose Transport Via the Phosphatidylinositol 3-Kinase/Protein Kinase B Signaling Pathway Is Associated With Fetal Growth Restriction [ Lab Invest, 2025, 105(4):104103] PubMed: 39909142
The role of lipid metabolism and peroxisome proliferator activation in mediating pro-cancer phenotypes of poly- and perfluoroalkyl substances in testicular cancer [ Environ Toxicol Pharmacol, 2025, 120:104866] PubMed: 41237835
Rosiglitazone-Mediated Activation of PPARγ Induces PlGF Expression in Trophoblast Cells [ Reprod Sci, 2025, 32(6):1864-1875] PubMed: 40295383
Comparative Study of Porcine Mesenchymal Stem Cells Behavior and Lipid Metabolism on Plant-Based Scaffolds and Two-Dimensional Systems for Cultivated Fat [ Eng Life Sci, 2025, 25(10):e70050] PubMed: 41098339
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

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NIET VOOR HUMANE, VETERINAIRE DIAGNOSTISCHE OF THERAPEUTISCHE DOELEINDEN.