DPP-4-IN-17
DPP-4-IN-17 is an orally active and selective dipeptidyl peptidase-4 (DPP-4) inhibitor with an IC50 value of 0.12 nM. DPP-4-IN-17 increases the enzyme's Km value (75.73 μM vs. 27.18 μM of substrate alone) and reduces catalytic efficiency. DPP-4-IN-17 reduces blood glucose levels and reverses weight loss in Streptozotocin (STZ) (HY-13753)/Nicotinamide (NA) (HY-B0150)-induced diabetic rats. DPP-4-IN-17 can be used for the study of type 2 diabetes mellitus (T2DM).
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- Formule: C32H53N5O9
- Masse moléculaire:651.79
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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DPP-4 0.12 nM (IC50) |
DPP-4-IN-17 (Compound 8) acts as a competitive DPP-4 inhibitor, increasing the Km value from 27.18 μM to 75.73 μM and decreasing the catalytic efficiency[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (6-8 weeks, 200-250 g) were fasted overnight (12 h), ip injected with 110 mg/kg nicotinamide (NA); 15 min later, ip injected with 50 mg/kg streptozotocin[1]
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Dosage:10, 20, 40 mg/kg
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Administration:p.o., once daily, 21 days
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Result:Reduced blood glucose to normal.
Reversed weight loss.
Normalized serum lipids, liver enzymes and renal parameters.
Repaired kidney (glomerulosclerosis reversed, tubule integrity restored) and pancreas (islet β-cells increased, acinar cells/ducts intact).
Chemical Information
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Masse moléculaire 651.79
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Formule C32H53N5O9
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SMILES
COC([C@@H]1CCCN1C([C@@H](NC([C@@H]2CCCN2C(OC(C)(C)C)=O)=O)CCCCNC([C@@H]3CCCN3C(OC(C)(C)C)=O)=O)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)