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Imiglitazar

Catalog No. T15567 CAS 250601-04-8

Synonyms: TAK-559

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

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Imiglitazar, CAS 250601-04-8

Pack Size	Availability	Price/USD	Quantity
1 mg	In stock	$ 700.00
5 mg	In stock	$ 1,800.00

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Purity: 97.33%

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Chemical Properties

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Description	Imiglitazar (TAK559) is a potent PPAR-β/δ receptor agonist with hypoglycemic effects.
Targets&IC50	PPARγ1:31 nM (EC50), PPARα:67 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].

Synonyms	TAK-559
Molecular Weight	470.52
Formula	C28H26N2O5
CAS No.	250601-04-8

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

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