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
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[2]|
DPP-4 2.25 nM (IC50) |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Zucker fatty rats (male, 12-13 weeks old, Type 2 diabetes model)[1]
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Dosage:0.01 mg/kg; 0.1 mg/kg
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Administration:p.o.; single dose 30 min prior to refeeding
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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
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CAS No. 851510-67-3
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Molecular Weight 235.29
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Formula C12H17N3O2
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SMILES
C(=O)([C@@H]1[C@]2(C[C@@](N1)([C@H](O)C2)[H])[H])N3[C@H](C#N)CCC3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)