PPAR agonist 4
PPAR agonist 4 (Compound 12) is an orally active agonist for peroxisome proliferator-activated receptor (PPAR), which activates PPARα, PPARδ and PPARγ with EC50s of 0.7, 0.7 and 1.8 μM, respectively. PPAR agonist 4 exhibits anti-liver fibrosis efficacy.
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- Fòrmula: C23H28F3N3O3
- Peso molecular:451.48
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Almacenamiento:
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Actividad biológica
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PPARα 0.7 μM (EC50) |
PPARδ 0.7 μM (EC50) |
PPARγ 1.8 μM (EC50) |
PPAR agonist 4 (3-10 μM) dose-dependently upregulates expressions of PPARα/δ target genes CPT1A, PDK4 and ANGPTL4 in HepG2 cells and PPARγ target genes CD36 and FABP4 in HEK293 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 and HEK293
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Concentration:3-10 μM
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Incubation Time:12 h
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Result:Upregulated levels of CPT1A, PDK4 and ANGPTL4, downregulated levels of CD36 and FABP4.
Pharmacokinetic Analysis of PPAR agonist 4 in Sprague-Dawley rats[1]
| route | Dose (mg/kg) | T1/2 (h) | MRT (h) | Cmax (μM) | AUC0-t (h·μM) | F (%) |
| i.v. | 2 | 9.7 | 6.8 | 12.2 | 59.8 | - |
| p.o. | 10 | 17.0 | 10.1 | 15.9 | 274.5 | 91.8 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CCL4-induced liver fibrosis in C57BL/6 mice[1]
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Dosage:3-30 mg/kg
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Administration:p.o., once a day for 3 weeks
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Result:Reduced levels of collagen and α-SMA, reduced accumulation of collagen and inflammatory cell infiltration in the portal area.
Upregulated the expression of PPARs target genes (Cpt1a, Cpt2, Angptl4 and Cd36).
Chemical Information
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Peso molecular 451.48
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Fòrmula C23H28F3N3O3
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SMILES
CC1=CC(CN2CCN(CC2)C3=NC=C(C=C3)C(F)(F)F)=CC(C)=C1OC(C)(C(O)=O)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PPAR agonist 4 Related Classifications
HY-163443 Related Classifications
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