product name Alogliptin
Description: Alogliptin (also known as SYR-322) is a potent, orallyavailable, and selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Like other medications for the treatment of Type 2 diabetes, alogliptin does not decrease the risk of heart attack and stroke. Alogliptin and other gliptins are commonly used in combination with metformin in patients whose diabetes cannot adequately be controlled with metformin alone.
References: J Med Chem. 2007 May 17;50(10):2297-300; Life Sci. 2009 Jul 17;85(3-4):122-6.
339.39
Formula
C18H21N5O2
CAS No.
850649-61-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 68 mg/mL (200.4 mM)
Water: 2 mg/mL (5.89 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
0.5% methylcellulose: 30 mg/mL
Synonyms
SYR-322
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19414866
| In Vitro |
In vitro activity: Alogliptin(SYR-322) is a potent inhibitor of DPP-4 and exhibits greater than 10,000 fold selectivity over the closely related serine proteases DPP-8 and DPP-9. Alogliptin is not an inhibitor of CYP-450 enzymes and does not block the hERG channel at concentrations up to 30 μM. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Alogliptin(SYR-322) produces dose-dependent improvements in glucose tolerance and increases plasma insulin levels in female Wistar fatty rats. Acute administration of alogliptin results in a significant decrease in plasma DPP-4 activity, and increases plasma active GLP-1. Alogliptin improves glucose tolerance at a dose of 0.3 mg/kg and higher, with a dose-dependent increase in plasma IRI, suggesting that improved glucose tolerance results from the ability of alogliptin to enhance insulin secretion. |
| Animal model | The N-STZ-1.5 rats |
| Formulation & Dosage | Dissolved in 0.5% methylcellulose; 0.1, 0.3, 1 or 3 mg/kg; p.o. administration |
| References | J Med Chem. 2007 May 17;50(10):2297-300; Life Sci. 2009 Jul 17;85(3-4):122-6 |
