| Identification | Back Directory | [Name]
L-Tyrosine, O-[2-(9H-carbazol-9-yl)ethyl]-N-[2-(4-fluorobenzoyl)phenyl]-, sodium salt (1:1) | [CAS]
2390374-10-2 | [Synonyms]
Carfloglitazar sodium
L-Tyrosine, O-[2-(9H-carbazol-9-yl)ethyl]-N-[2-(4-fluorobenzoyl)phenyl]-, sodium salt (1:1) | [Molecular Formula]
C36H30FN2NaO4 | [MOL File]
2390374-10-2.mol | [Molecular Weight]
596.63 |
| Hazard Information | Back Directory | [Uses]
Chiglitazar (Carfloglitazar) is a PPARα/γ dual agonist, with EC50s of 1.2, 0.08, 1.7 μM for PPARα, PPARγ and PPARδ, respectively. | [in vivo]
After insulin injection, plasma glucose levels in the MSG rats treated with Chiglitazar or rosiglitazone are significantly reduced compared with the control group treated with vehicle at all time points. Fasting PI levels are lower in animals treated with Chiglitazar and rosiglitazone than control. The ISIs of MSG obese rats treated with chiglitazar and rosiglitazone are significantly higher than control. Furthermore, Chiglitazar ameliorates the HOMA indices. For IPGTT, at the 30?min after glucose loading, the glucose values in the 5 and 10?mg?/kg Chiglitazar and rosiglitazone-treatment groups are significantly lower than those in the vehicle treatment group. The integrated for the glucose response during the IPGTT in the treatment groups are significantly less than those in the control groups[2]. | [IC 50]
PPARα: 1.8 μM (EC50); PPAR-γ: 0.08 μM (EC50); PPAR-δ: 1.7 μM (EC50) | [References]
[1] Li PP, et al. The PPARalpha/gamma dual agonist chiglitazar improves insulin resistance and dyslipidemia in MSG obese rats. Br J Pharmacol. 2006 Jul;148(5):610-8. DOI:10.1038/sj.bjp.0706745
[2] He BK, et al. In Vitro and In Vivo Characterizations of Chiglitazar, a Newly Identified PPAR Pan-Agonist. PPAR Res. 2012;2012:546548. DOI:10.1155/2012/546548 |
|
|