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  3. Imiglitazar

Imiglitazar (Synonyms: TAK-559)

Cat. No.: HY-101649
Handling Instructions

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

For research use only. We do not sell to patients.

Imiglitazar Chemical Structure

Imiglitazar Chemical Structure

CAS No. : 250601-04-8

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Description

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)

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].

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].

Clinical Trial
Molecular Weight

470.52

Formula

C₂₈H₂₆N₂O₅

CAS No.

250601-04-8

SMILES

CC(OC(C1=CC=CC=C1)=N2)=C2COC(C=C3)=CC=C3CO/N=C(CCC(O)=O)/C4=CC=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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.

References
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Keywords:

ImiglitazarTAK-559TAK559TAK 559PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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