1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. 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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DPP-4-IN-17

DPP-4-IN-17 Chemical Structure

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Description

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)[1].

IC50 & Target[1]

DPP-4

0.12 nM (IC50)

In Vitro

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.

In Vivo

DPP-4-IN-17 (Compound 8) (10-40 mg/kg, p.o., once daily, 21 days) significantly reduces blood glucose levels and reverses weight loss in Streptozotocin (STZ) (HY-13753)/Nicotinamide (NA) (HY-B0150)-induced diabetic Wistar rats [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 10, 20, 40 mg/kg
Administration: p.o., once daily, 21 days
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).
Molecular Weight

651.79

Formula

C32H53N5O9

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
DPP-4-IN-17
Cat. No.:
HY-175590
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