1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase

DPP-4 inhibitor 1 

Cat. No.: HY-114408
Handling Instructions

DPP-4 inhibitor 1 (compound 5) is a potent and long acting Dipeptidyl peptidase-4 (DPP-4) inhibitor for t treatment of T2DM, with a KD of 0.177 nM.

For research use only. We do not sell to patients.

DPP-4 inhibitor 1 Chemical Structure

DPP-4 inhibitor 1 Chemical Structure

CAS No. : 1915007-89-4

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Description

DPP-4 inhibitor 1 (compound 5) is a potent and long acting Dipeptidyl peptidase-4 (DPP-4) inhibitor for t treatment of T2DM, with a KD of 0.177 nM[1].

IC50 & Target

KD: 0.177 nM (DPP-4)[1].

In Vivo

A single-dose oral administration of DPP-4 inhibitor 1 (compound 5) (3 mg/kg) inhibits >80% of DPP-4 activity for more than 7 days in diabetic mice[1].
Administration of DPP-4 inhibitor 1 (compound 5) (3 and 10 mg/kg, p.o., qw for 8 weeks) causes significant reductions in fasting blood glucose (FBG) levels, and the average reduction during the entire treatment period is 24.7 and 33.1%, respectively. Chronic administration of DPP-4 inhibitor 1 (compound 5) (10 mg/kg/week) also significantly improves the glucose tolerance of the diabetic mice[1].

Animal Model: ICR mice[1].
Dosage: 0.3, 3, 10 mg/kg.
Administration: Oral, once.
Result: Resulted in a time- and dose-dependent inhibition of plasma DPP-4 activity.
The active GLP-1 and insulin level were significantly increased compared with the vehicle control.
Animal Model: Genetic-type 2 diabetes animal models in db/db Mice[1].
Dosage: 3 and 10 mg/kg.
Administration: Oral administration once a week, for 8 weeks.
Result: Caused significant reductions in fasting blood glucose (FBG) levels.
Improved the glucose tolerance of the diabetic mice significantly.
References
Molecular Weight

384.35

Formula

C₂₁H₁₅F₃N₂O₂

CAS No.

1915007-89-4

SMILES

FC1=CC(F)=C([[email protected]]2OC3=CC=C(C=C(C#N)C(OC)=C4)C4=C3C[[email protected]@H]2N)C=C1F

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
DPP-4 inhibitor 1
Cat. No.:
HY-114408
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DPP-4 inhibitor 1

Cat. No.: HY-114408