| Identification | Back Directory | [Name]
Imiglitazar | [CAS]
250601-04-8 | [Synonyms]
TAK-559
Imiglitazar
Benzenebutanoic acid, γ-[[[4-[(5-methyl-2-phenyl-4-oxazolyl)methoxy]phenyl]methoxy]imino]-, (γE)- | [Molecular Formula]
C28H26N2O5 | [MDL Number]
MFCD16659637 | [MOL File]
250601-04-8.mol | [Molecular Weight]
470.52 |
| Chemical Properties | Back Directory | [Boiling point ]
679.9±65.0 °C(Predicted) | [density ]
1.20±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [pka]
4.17±0.10(Predicted) |
| Hazard Information | Back Directory | [Uses]
Imiglitazar (TAK559) is a potent and dual human PPARα and PPARγ1 agonist with EC50 values of 67 and 31 nM. | [Biological Activity]
Imiglitazar (TAK559) is a potent dual agonist of human PPARα and PPARγ1 with EC50 values of 67 and 31 nM. | [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]. | [target]
| PPARγ1 31 nM (EC 50 ) | PPARα 67 nM (EC 50 ) | | [IC 50]
PPARγ1: 31 nM (EC50); PPARα: 67 nM (EC50) | [storage]
Store at -20°C | [References]
[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. DOI:10.1016/j.ejphar.2004.05.020
[2] 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. DOI:10.1016/j.atherosclerosis.2004.08.015
[3] 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. DOI:10.1016/j.metabol.2007.05.019 |
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