FFAR4 agonist-1
FFAR4 agonist-1 is an orally active, selective agonist of FFAR4. FFAR4 agonist-1 improves glucose tolerance, reduces blood glucose levels and promotes insulin secretion. FFAR4 agonist-1 can be used in the research of type 2 diabetes.
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- No. CAS: 3110207-82-1
- Fòrmula: C22H17F2NO4
- Peso molecular:397.37
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Almacenamiento:
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Actividad biológica
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FFAR4 |
FFAR4 agonist-1 (compound 10f) potently activates human FFAR4-transfected CHO cells with an EC50 of 78.6 nM and shows ~400-fold selectivity for FFAR4 over FFAR1 in human FFAR1-transfected CHO cells[1].
FFAR4 agonist-1 interacts stably with FFAR4 (PDB code 8G59) via multiple hydrogen bonds and hydrophobic interactions, mimicking the binding mode of TUG-891[1].
FFAR4 agonist-1 has improved druggability properties, with a lower cLogP (4.35) and higher TPSA (75.63 Å2) than FFAR4 agonist TUG-891[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Cmax | Tmax | AUC | T1/2 |
|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 3.14 μg/mL | 30 min | 9.83 μg·h/mL | 1.51 h |
FFAR4 agonist-1 (1-100 mg/kg; p.o.; single dose) exhibits dose-dependent anti-hyperglycemic activity in diet-induced obese male C57BL/6 mice, reducing glucose AUC0-t by up to 32.4% at 100 mg/kg and increasing insulin secretion at doses ≥10 mg/kg without causing hypoglycemia[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR (male, 4-week-old, acclimatized for 1 week before testing)[1]
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Dosage:20 mg/kg
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Administration:p.o.; single dose
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Result:Reduced the area under the blood glucose-time curve (AUC) between 0 and 120 min by 30.8% compared to the vehicle-treated group.
Showed no significant change in fasting blood glucose after administration.
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Animal Model:C57BL/6 (male, 4-week-old, fed high-fat diet for 12 weeks to induce diet-induced obesity)[1]
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Dosage:1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg; 100 mg/kg
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Administration:p.o.; single dose
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Result:Reduced blood glucose AUC between -30 and 120 min in a dose-dependent manner: 30 mg/kg reduced AUC by 20.1%, and 100 mg/kg reduced AUC by 32.4% compared to the vehicle-treated group.
Restored blood glucose levels to normal by 120 min in the 30 mg/kg and 100 mg/kg groups.
Increased plasma insulin levels significantly compared to the control group at doses ≥10 mg/kg.
Caused no hypoglycemia at any dose tested.
Chemical Information
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No. CAS 3110207-82-1
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Peso molecular 397.37
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Fòrmula C22H17F2NO4
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SMILES
O=C(COC1=CC=C(C(NC2=CC(F)=CC=C2C3=CC=C(C)C=C3)=O)C=C1F)O
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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)
FFAR4 agonist-1 Related Classifications
HY-185937 Related Classifications
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