store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Imiglitazar (TAK559)是有效的 PPAR-β/δ受体激动剂,具有降血糖作用。
产品描述 | Imiglitazar (TAK559) is a potent PPAR-β/δ receptor agonist with hypoglycemic effects. |
靶点活性 | PPARγ1:31 nM (EC50), PPARα:67 nM (EC50) |
体外活性 |
TAK-559, a partial agonist for hPPARg1, achieves approximately 68% of the maximal activation obtained with rosiglitazone, a known PPARγ agonist. Significant activation of PPARγ is observed at a high concentration (10 μM) of TAK-559. Competition-binding assays using radiolabeled ligand indicate that the transactivation of all hPPAR subtypes by TAK-559 is a result of direct binding of TAK-559 to each subtype. TAK-559 also recruits the coactivator SRC-1 to both hPPARγ1 and hPPARα, and dissociates the corepressor NCoR from both hPPARγ1 and hPPARα[1]. In the presence of 10 μM TAK-559, TNFα- or IL-1β-induced THP-1 cell attachment to cultured endothelial cells is significantly reduced. The secretion of monocyte chemoattractant protein-1 (MCP-1) from endothelial cells is reduced by 36%, accompanied by decreased mRNA expression in the cells. Furthermore, the proliferation and migration of cultured smooth muscle cells are significantly decreased in the presence of TAK-559[3]. |
体内活性 | During TAK-559 treatment, significant elevation of circulating high-density lipoprotein (HDL) cholesterol levels is observed, characterized by an increase in large HDL particles and a decrease in small dense HDL particles. Concurrently, plasma triglyceride and apolipoprotein B-100 levels decrease, while apolipoprotein A-I increases. Hyperinsulinemia and insulin resistance are significantly corrected with the highest dose of 3.0 mg/kg per day in these prediabetic monkeys. Additionally, no adverse effects on representative liver function parameters are observed during the study period[2]. |
别名 | TAK-559 |
分子量 | 470.52 |
分子式 | C28H26N2O5 |
CAS No. | 250601-04-8 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Imiglitazar 250601-04-8 DNA Damage/DNA Repair Metabolism PPAR TAK 559 TAK-559 TAK559 Inhibitor inhibitor inhibit