| Bioactivity | Alogliptin Benzoate (SYR-322) is a potent, selective and orally active inhibitor of DPP-4 with an IC50 of <10 nM, and exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. Alogliptin Benzoate can be used for the research of type 2 diabetes[1][2][3]. |
| Target | IC50: <10 nM (DPP-4) |
| Invitro | Alogliptin (1 nM; 5-60 min) inhibits LPS-induced extracellular signal-regulated kinase (ERK) phosphorylation in U937 cells[2].Alogliptin (0.5-5 nM; 24 h) inhibits LPS-stimulated MMP-1 secretion and mRNA expression that is mediated by ERK pathway in U937 cells[2]. |
| In Vivo | Alogliptin (0.01-1 mg/kg; p.o.) produced dose-dependent improvements in glucose tolerance and increased plasma insulin levels in female Wistar fatty rats[1].Alogliptin (40 mg/kg/day for 2 weeks; p.o.) reduces infarction area and improves brain vascular integrity in middle cerebral artery occlusion (MCAO) mice[3]. |
| Name | Alogliptin Benzoate |
| CAS | 850649-62-6 |
| Formula | C25H27N5O4 |
| Molar Mass | 461.51 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Feng J, et, al. Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. J Med Chem. 2007 May 17;50(10):2297-300. [2]. Ta NN, et, al. DPP-4 (CD26) inhibitor alogliptin inhibits TLR4-mediated ERK activation and ERK-dependent MMP-1 expression by U937 histiocytes. Atherosclerosis. 2010 Dec;213(2):429-35. [3]. Hao FL, et, al. The neurovascular protective effect of alogliptin in murine MCAO model and brain endothelial cells. Biomed Pharmacother. 2019 Jan;109:181-187. [4]. Asakawa T, et, al. A novel dipeptidyl peptidase-4 inhibitor, alogliptin (SYR-322), is effective in diabetic rats with sulfonylurea-induced secondary failure. Life Sci. 2009 Jul 17;85(3-4):122-6. [5]. Moritoh Y, et al. The dipeptidyl peptidase-4 inhibitor alogliptin in combination with pioglitazone improves glycemic control, lipid profiles, and increases pancreatic insulin content in ob/ob mice. Eur J Pharmacol. 2009 Jan 14;602(2-3):448-54. |