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  3. Imiglitazar

Imiglitazar  (Synonyms: TAK-559)

目录号: HY-101649
产品使用指南

Imiglitazar (TAK559)是有效地人类PPARαPPARγ1双重激动剂,EC50值分为67 和31 nM。

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Imiglitazar Chemical Structure

Imiglitazar Chemical Structure

CAS No. : 250601-04-8

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  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Imiglitazar (TAK559) is a potent and dual human PPARα and PPARγ1 agonist with EC50 values of 67 and 31 nM.

IC50 & Target[1]

PPARγ1

31 nM (EC50)

PPARα

67 nM (EC50)

体外研究
(In Vitro)

TAK-559 is a partial agonist for hPPARg1 with about 68% of maximal activation obtained with rosiglitazone, a known PPARγ agonist. PPARy is significantly activated at a high concentration (10 μM) of TAK-559. Competition-binding assays using radiolabeled ligand indicates that the transactivation of all hPPAR subtypes by TAK-559 is due to direct binding of TAK-559 to each subtype. TAK-559 also recruit the coactivator SRC-1 to each of hPPARγ1 and hPPARα, and to dissociate the corepressor NCoR from each of hPPARγ1 and hPPARα[1].TNFα- or IL-1β-induced THP-1 cell attachment to cultured endothelial cells is significantly reduced in the presence of 10 μM TAK-559. The secretion of monocyte chemoattractant protein-1 (MCP-1) from endothelial cells is reduced by 36% in the presence of 10 μM TAK-559, accompanied with the decreased mRNA expression in the cells. The proliferation and migration of cultured smooth muscle cells are significantly decreased in the presence of TAK-559[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

TAK-559 treatment results in significant elevation of circulating high-density lipoprotein (HDL) cholesterol levels, consisting of an increase in large HDL particles and a decrease in small dense HDL particles. Plasma triglyceride and apolipoprotein B-100 levels decrease, whereas apolipoprotein A-I increasesduring TAK-559 treatment. Hyperinsulinemia and insulin resistance are significantly corrected with the highest dose of 3.0 mg/kg per day in these prediabetic monkeys. In addition, no adverse effects on representative liver function parameters are observed during the study period[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

470.52

Formula

C28H26N2O5

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
Kinase Assay
[1]

Competition binding assays are performed with cell extract containing hPPARδ and 20 nM [3H]L-783483 in the presence of indicated concentrations of TAK-559 (1, 10, 100 μM) or Iloprost. Data are expressed as the percentage of specific binding in the absence of competitor (vehicle (V) (1% DMSO))[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

COS-1 cells are cotransfected with expression plasmid for full-length hPPARγ1 as a VP16 fusion protein, GAL4-SRC-1 (A) or GAL4-NcoR (B) expression plasmid and (UAS)5-tk-Luciferase reporter plasmid. Cells are cultured in the presence of TAK-559 (0.01, 0.1, 1 μM) or rosiglitazone for 2 days. The cell extracts are assayed for luciferase activity[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Imiglitazar
目录号:
HY-101649
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