吡格列酮 (U 72107) 钾是一种具有口服活性和选择性的 PPARγ; (过氧化物酶体增殖物激活受体)激动剂,与 PPARγ 具有高亲和力;配体结合结构域,EC50 分别为 0.93 μM 和 0.99 μM 对于人和小鼠 PPARγ,分别。
Cas No. | 1266523-09-4 |
别名 | U 72107 potassium |
Canonical SMILES | CCC1=CC=C(CCOC2=CC=C(CC(C3=O)SC([N-]3)=O)C=C2)N=C1.[K+] |
分子式 | C19H19N2O3S•K |
分子量 | 394.5 |
溶解度 | DMF: 30 mg/ml,DMSO: 10 mg/ml,Ethanol: 10 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 | Pioglitazone is an agonist of the peroxisome proliferator-activated receptor γ (PPARγ; EC50 = ~500-600 nM for both human and murine PPARγ). It is selective for PPARγ over PPARα, exhibiting low level activation of PPARα at 1 µM and 5.4-fold activation at a concentration of 10 µM. Pioglitazone inhibits pyruvate oxidation and glucose production in hepatocytes when used at a concentration of 10 μM. In vivo, pioglitazone (0.3-3 mg/kg per day) reduces hyperglycemia, hyperlipidemia, and hyperinsulinemia in a dose-dependent manner in male Wistar fatty rats. It reduces the number of lesions in a transgenic rat adenocarcinoma of prostate (TRAP) model. Pioglitazone (2.5 mg/kg) also decreases production of neuroinflammatory cytokines and reduces immobility in the forced swim and tail suspension tests in a mouse model of chronic mild stress, indicating antidepressant-like activity that can be reversed by the PPARγ antagonist GW9662 . |