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Cat. No.: HY-167075

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ASP4000 free base

ASP4000 free base is an orally effective dipeptidyl peptidase 4 (DPP4) inhibitor, with an IC₅₀ value of 2.25 nM against human recombinant DPP4, and exhibits hypoglycemic activity. By inhibiting DPP4 activity, ASP4000 free base reduces the degradation of active glucagon-like peptide-1 (GLP-1), thereby persistently increasing postprandial active GLP-1 levels and improving glycemic control. ASP4000 free base can be used in studies related to type 2 diabetes.

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

CAS No.: 851510-67-3
Formula: C₁₂H₁₇N₃O₂
Molecular Weight:235.29

Storage:

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

ASP4000 free base Chemical Structure

CAS No.: 851510-67-3

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
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Biological Activity

Description

IC₅₀ & Target

^[2]

DPP-4

2.25 nM (IC₅₀)

All Dipeptidyl Peptidase Isoforms :

In Vivo

ASP4000 free base (0.01-0.1 mg/kg; p.o.; single dose 30 min prior to refeeding) dose-dependently improves postprandial hyperglycemia and constitutively increases active GLP-1 levels in Zucker fatty rats, with the 0.1 mg/kg dose nearly eliminating postprandial hyperglycemia^[1].

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

Animal Model:

Zucker fatty rats (male, 12-13 weeks old, Type 2 diabetes model)^[1]
Dosage:

0.01 mg/kg; 0.1 mg/kg
Administration:

p.o.; single dose 30 min prior to refeeding
Result:

Improved glucose tolerance in a dose-dependent manner.
Almost completely inhibited postprandial hyperglycemia at 0.1 mg/kg, significantly decreasing the Δ plasma glucose AUC (between 30 min and 120 min).
Significantly increased plasma Δ active GLP-1 levels constitutively for 120 min after refeeding at both doses, with the 0.1 mg/kg dose producing a larger increase in Δ active GLP-1 AUC.
Showed no significant difference in plasma Δ insulin levels and AUC compared to vehicle-treated rats.

Chemical Information

CAS No. 851510-67-3
Molecular Weight 235.29
Formula C₁₂H₁₇N₃O₂
SMILES

C(=O)([C@@H]1[C@]2(C[C@@](N1)([C@H](O)C2)[H])[H])N3[C@H](C#N)CCC3
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

Handling Instructions (2659 KB)

References

[1]. Tanaka-Amino K, et al. Constitutive increase in active GLP-1 levels by the DPP4 inhibitor ASP4000 on a new meal tolerance test in Zucker fatty rats. Pharmacological research. 2009 Oct;60(4):264-9.

[2]. Tanaka-Amino K, et al. ASP4,000, a novel, selective, dipeptidyl peptidase 4 inhibitor with antihyperglycemic activity. Eur J Pharmacol. 2008 Aug 20;590(1-3):444-9. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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