Pioglitazone hydrochloride 是一种选择性PPARγ激动剂,高亲和力结合到 PPARγ 配体结合域。作用于人和鼠 PPARγ,EC50分别为 0.93 和 0.99 μM。它是一种口服活性噻唑烷二酮的盐酸盐,具有抗糖尿病特性和潜在的抗肿瘤活性。
产品描述
Pioglitazone Hydrochloride is the hydrochloride salt of an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity.
体外活性
在雄性肥胖鼠中,口服 Pioglitazone(0.3-3 mg/kg)7天,能够以剂量依赖性的方式地降低高血糖症,高脂血症,和高胰岛素血症.
体内活性
Pioglitazone 通过抑制iNOS的表达和NO的产生,保护多巴胺能神经元被LPS损伤。Pioglitazone也能够抑制脂多糖诱导的p38蛋白磷酸化。
细胞实验
In order to evaluate cell proliferation, HIT-T15 cells are seeded on 96-well plates (3×104 cells/well) and cultured for 5 days as described. Viable cells are determined using the Cell Titer 96 Aqueous One Solution Cell Proliferation Assay. To evaluate cell apoptosis and cell necrosis, HIT-T15 cells are plated on 6-well dishes (7×105 cells/well) for 5 days in standard conditions (CTR) or in the presence of AGEs (AGEs) with or without Pioglitazone (0.5 or 1 μM) or AG (1 mM). They are then processed to measure both the activity of caspase-3 and the activity of lactate dehydrogenase (LDH) (a stable cytosolic enzyme that is a marker of cell membrane damage and cell death due to necrosis) using Cytotox 96 Non Radioactive Cytotoxicity Assay[2].
Cas No.
112529-15-4
分子式
C19H21ClN2O3S
分子量
392.9
别名
Pioglitazone HCl;匹格列酮盐酸盐;U-72107E;AD 4833;U 72107A
储存和溶解度
DMSO:9.8 mg/mL (25 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years