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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C32H53N5O9
- 分子量:651.79
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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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).
化学情報
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分子量 651.79
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)