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Imiglitazar

Imiglitazar

产品编号 T15567   CAS 250601-04-8
别名: TAK-559

Imiglitazar (TAK559)是有效的 PPAR-β/δ受体激动剂,具有降血糖作用。

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Imiglitazar Chemical Structure
Imiglitazar, CAS 250601-04-8
规格 价格/CNY 货期 数量
1 mg ¥ 4,900 现货
5 mg ¥ 12,600 现货
产品目录号及名称: Imiglitazar (T15567)
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生物活性
化学信息
存储 & 溶解度
参考文献
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

存储

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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参考文献

1. Sakamoto J, et al. A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes. Eur J Pharmacol. 2004 Jul 8;495(1):17-26. 2. Ding SY, et al. A novel peroxisome proliferator--activated receptor alpha/gamma dual agonist ameliorates dyslipidemia and insulin resistance in prediabetic rhesus monkeys. Metabolism. 2007 Oct;56(10):1334-9. 3. Seki N, et al. A potent activator of PPARalpha and gamma reduces the vascular cell recruitment and inhibits the intimal thickning in hypercholesterolemic rabbits. Atherosclerosis. 2005 Jan;178(1):1-7.
PPARα-MO-1 13-Oxo-9E,11E-octadecadienoic acid Pioglitazone DSO-5a PPARγ agonist 8 Ailanthoidol Anti-NASH agent 1 Oroxin A

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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% ddH2O
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技术支持

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。

Keywords

Imiglitazar 250601-04-8 DNA Damage/DNA Repair Metabolism PPAR TAK 559 TAK-559 TAK559 Inhibitor inhibitor inhibit

 

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