Imiglitazar

SKU: orb1707184

Description

Imiglitazar

Research Area

Metabolism Research, Molecular Biology

Key Properties

• CAS Number: 250601-04-8
• MW: 470.52
• Purity: 97.33% (May vary between batches)
• Formula: C₂₈H₂₆N₂O₅
• SMILES: C(OC1=CC=C(CO/N=C(\CCC(O)=O)/C2=CC=CC=C2)C=C1)C=3N=C(OC3C)C4=CC=CC=C4
• Target: PPAR

Bioactivity

• Target IC50:
  PPARγ1:31 nM (EC50)|PPARα:67 nM (EC50)
• 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.
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• 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. 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PPARδ, PPARγ1, PPARα, PPARβ, TAK 559, TAK559, TAK-559, Imiglitazar

Compound Identifiers

PubChem CID

9890879