Tamanho : 1mLx10mM(inDMSO)
Telefone : +1 850 650 7790
Synonyms: BRL49653
| Description | Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer. |
| Targets & IC50 | PPARγ:60 nM(EC50), PPARγ:40 nM (Kd), PPARγ1:30 nM(EC50), TRPC5:30 μM, PPARγ2:100 nM(EC50) |
| In vitro | Rosiglitazone reduces bone formation rate and increases adipose content within the bone marrow. It decreases the expression of osteoblast-specific genes Runx2/Cbfa1, DLX5, and α1(I) collagen, while expression of the adipocyte-specific fatty acid binding protein AP2 is increased. This drug leads to significant bone loss, evidenced by reductions in bone mass, trabecular width, and number, along with an increase in trabecular separation. Furthermore, in ob/ob mice, rosiglitazone enhances transcription of genes encoding mitochondrial proteins in white adipocytes, which is accompanied by changes in mitochondrial number and structure. |
| In vivo | In certain cell lines, Rosiglitazone reduces cholesterol synthesis independent of peroxisome proliferator-activated receptor γ (PPARγ). The compound significantly enhances the phosphorylation of threonine 172 in the α subunit of AMP-dependent protein kinase, increasing the AMP: ATP ratio. Additionally, Rosiglitazone boosts secretion of adiponectin by up to 2.3-fold from omental cells, while secretion from subcutaneous fat cells remains unaffected. In 3T3-L1 adipocytes, Rosiglitazone alters mitochondrial morphological characteristics and protein profile. It activates complexes containing α1- and α2-AMPK, leading to a marked increase in phosphorylation of acetyl-CoA carboxylase. Rosiglitazone also acts as a dominant inhibitor of osteoblastogenesis from mouse marrow in vitro through the activation of PPAR-gamma2. |
| Synonyms | BRL49653 |
| Cell Research | Rosiglitazone is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2]. Human neuroblastoma SH-SY5Y cells are maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum, 100 μg/mL Streptomycin and 100 U/mL Penicillin G. SH-SY5Y cells are transfected with the longest isoform of human tau (2N4R) tagged with GFP using lipofectamine. 24 hr after transfection, cells are treated with Rosiglitazone (10 μM, 50 μM) for 24 hr[2]. |
| Molecular Weight | 357.43 |
| Formula | C18H19N3O3S |
| Cas No. | 122320-73-4 |
| Smiles | C(C1SC(=O)NC1=O)C2=CC=C(OCCN(C)C3=CC=CC=N3)C=C2 |
| Relative Density. | 1.315 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 262.5 mg/mL (734.41 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.58 mg/mL (10.02 mM), Suspension. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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