罗格列酮 (BRL 49653) 钾是一种具有口服活性的选择性 PPARγ；激动剂（EC50:60 nM，Kd:40 nM）。
| Cas No. | 316371-84-3 |
| 别名 | 罗格列酮钾盐,BRL 49653 potassium |
| Canonical SMILES | CN(CCOC1=CC=C(CC2SC([N-]C2=O)=O)C=C1)C3=NC=CC=C3.[K+] |
| 分子式 | C18H18N3O3S•K |
| 分子量 | 395.5 |
| 溶解度 | DMF: >25 mg/ml,DMSO: >25 mg/ml,DMSO:PBS (7.2 pH) (1:3): 500 µ g/ml,Ethanol: 2 mg/ml,Water: 1 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Rosiglitazone is a thiazolidinedione agonist of peroxisome proliferator-activated receptor γ (PPARγ) that binds to the ligand binding domain (LBD) of PPARγ with a Kd value of 43 nM. It selectively activates chimeras containing the LBDs of PPARγ over PPARα and PPARδ in a cell-based reporter assay when used at a concentration of 10 mM. Rosiglitazone also activates full-length PPARγ1 and PPARγ2 in a reporter assay (EC50s = 30 and 100 nM, respectively). It induces differentiation of C3H10T1/2 stem cells to adipocytes when used at a concentration of 1 μM. Rosiglitazone (4 mg/kg) decreases hemoglobin A1c (HbA1c) and fasting blood glucose levels in a rat model of type 2 diabetes induced by streptozotocin and a high-carbohydrate/high-fat diet. It also inhibits increases in contusion volume, macrophage infiltration and activation of microglia, and expression of IL-6, MCP1, ICAM1, caspase-3, and Bax in mouse cerebral cortex in a model of traumatic brain injury induced by controlled cortical impact when administered at a dose of 6 mg/kg. Formulations containing rosiglitazone have been used to improve glycemic control in the treatment of type 2 diabetes. |
