product name Rosiglitazone
Description: Rosiglitazone is a potent antidiabetic drug in the thiazolidinedione class and a potent insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. Rosiglitazone works as an insulin sensitizer, by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin. Rosiglitazone is a member of the thiazolidinedione class of drugs. Thiazolidinediones act as insulin sensitizers. They reduce glucose, fatty acid, and insulin blood concentrations.
References: J Biol Chem. 2002 Jul 12;277(28):25226-32; Endocrinology. 2004 Jan;145(1):401-6.
357.43
Formula
C18H19N3O3S
CAS No.
122320-73-4
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 71 mg/mL (198.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
4% DMSO+30% PEG 300+5% Tween 80+ddH2O: 5mg/mL
Synonyms
BRL 49653
other peoduct :
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
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| Formulation & Dosage | |
| References | J Biol Chem. 2002 Jul 12;277(28):25226-32; Endocrinology. 2004 Jan;145(1):401-6. |
