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Imiglitazar

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Catalog No. T15567Cas No. 250601-04-8
Alias TAK-559

Imiglitazar (TAK559) is a potent PPAR-β/δ receptor agonist with hypoglycemic effects.

Imiglitazar

Imiglitazar

😃Good
Purity: 97.33%
Catalog No. T15567Alias TAK-559Cas No. 250601-04-8
Imiglitazar (TAK559) is a potent PPAR-β/δ receptor agonist with hypoglycemic effects.
Pack SizePriceAvailabilityQuantity
1 mg665 €8-10 weeks
5 mg1.710 €8-10 weeks
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Purity:97.33%
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Product Introduction

Bioactivity
Description
Imiglitazar (TAK559) is a potent PPAR-β/δ receptor agonist with hypoglycemic effects.
Targets&IC50
PPARα:67 nM (EC50), PPARγ1:31 nM (EC50)
In vitro
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].
In vivo
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].
AliasTAK-559
Chemical Properties
Molecular Weight470.52
FormulaC28H26N2O5
Cas No.250601-04-8
SmilesC(OC1=CC=C(CO/N=C(\CCC(O)=O)/C2=CC=CC=C2)C=C1)C=3N=C(OC3C)C4=CC=CC=C4
Relative Density.1.20 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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