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Pioglitazone hydrochloride (AD 4833) 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。
Pioglitazone hydrochloride (AD 4833) 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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
50 mg | ¥ 155 | 现货 | |
100 mg | ¥ 198 | 现货 | |
500 mg | ¥ 570 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 218 | 现货 |
产品描述 | Pioglitazone hydrochloride (AD 4833) is the hydrochloride salt of an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity. |
靶点活性 | PPARγ (human):0.93 μM (EC50), PPARγ (mouse):0.99 μM (EC50) |
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]. |
别名 | 匹格列酮盐酸盐, U-72107E, U 72107A, Pioglitazone HCl, AD 4833 |
分子量 | 392.9 |
分子式 | C19H20N2O3S·HCl |
CAS No. | 112529-15-4 |
Smiles | Cl.CCc1ccc(CCOc2ccc(CC3SC(=O)NC3=O)cc2)nc1 |
密度 | 1.26 g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (127.26 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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