1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. Saxagliptin hydrate

Saxagliptin hydrate (Synonyms: BMS-477118 hydrate)

Cat. No.: HY-10285A
Handling Instructions

Saxagliptin hydrate (BMS-477118 hydrate) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrate has the peotential for type 2 diabetes mellitus research.

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

Saxagliptin hydrate Chemical Structure

Saxagliptin hydrate Chemical Structure

CAS No. : 945667-22-1

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Description

Saxagliptin hydrate (BMS-477118 hydrate) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrate has the peotential for type 2 diabetes mellitus research[1][2][3].

IC50 & Target

Ki: 0.6-1.3 nM (Dipeptidyl peptidase-4 (DPP-4))[2]

In Vitro

Saxagliptin (100 nM; 48 hours; INS-1 832/13 cells) treatment significantly induceS β-cell proliferation[1].
Saxagliptin (100 nM; 48 hours; INS-1 832/13 cells) treatment increases the p-AKT and active β-catenin protein levels, paralleled with the increase of c-myc and cyclin D1 protein expression[1].
Saxagliptin acts by preventing the degradation of glucagon-like peptide-1 and hence increases secretion of insulin and decreases secretion of glucagon[3].

Cell Proliferation Assay[1]

Cell Line: INS-1 832/13 cells
Concentration: 100 nM
Incubation Time: 48 hours
Result: Significantly induced β-cell proliferation.

Western Blot Analysis[1]

Cell Line: INS-1 832/13 cells
Concentration: 100 nM
Incubation Time: 48 hours
Result: Increased the p-AKT and active β-catenin protein levels, paralleled with the increase of c-myc and cyclin D1 protein expression.
In Vivo

Saxagliptin (1 mg/kg; for 12 weeks) treatment in high-fat diet/streptozotocin-induced diabetic rats, significant improvement in pancreas insulin secretion capacity evaluated by hyperglycemia clamp and increased β-cell to α-cell areas ratio are observed[1].
Saxagliptin dose-dependently inhibits plasma DPP-4 activity in Han-Wistar rats, by ~70% at 7 hours postdose with 1 mg/kg and by ~90% at 7 hours postdose with 10 mg/kg. At 24 hours postdose, ~20% and 70% inhibition, respectively, remained[2].

Clinical Trial
Molecular Weight

333.43

Formula

C₁₈H₂₇N₃O₃

CAS No.

945667-22-1

SMILES
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Storage

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

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Keywords:

SaxagliptinBMS-477118BMS477118BMS 477118Dipeptidyl PeptidaseDPPDPP-4diabetesglucagon-likepeptide-1insulinglucagonp-AKTβ-cateninc-mycproliferationInhibitorinhibitorinhibit

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