规格 | 5mg 10mg 50mg 100mg |
CAS | 850649-62-6 |
别名 | SYR322, SYR-322,Nesina; |
化学名 | 2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile;benzoic acid |
分子式 | C25H27N5O4 |
分子量 | 461.51 |
溶解度 | ≥ 46.2 mg/mL in DMSO, ≥ 3.02 mg/mL in EtOH with ultrasonic and warming, ≥ 46.2 mg/mL in H2O with gentle warming |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
Alogliptin is a novel, highly selective and potent inhibitor of serine protease dipeptidylpeptidase-4 (DPP-4) with IC50 value of less than 10 nM [1].
Alogliptin has been reported to significantly reduce plasma DPP-4 activity and increase active GLP-1 levels in a dose-dependent manner in ob/ob mice. Besides, alogliptin after 4 weeks administration remarkably reduced non-fasting glycosylated hemoglobin, non-fasting plasma glucose and triglyceride levels, as well as siginificantly increased non-fasting plasma insulin and fasting pancreatic insulin content in ob/ob mice. Moreover, alogliptin treated ob/ob mice have shown the increase of early-phase insulin secretion and the decrease of plasma glucose AUC [2]
References:
[1] Feng J, Zhang Z, Wallace MB, Stafford JA, Kaldor SW, Kassel DB, Navre M, Shi L, Skene RJ, Asakawa T, Takeuchi K, Xu R, Webb DR, Gwaltney SL 2nd. 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] Moritoh Y1, Takeuchi K, Asakawa T, Kataoka O, Odaka H. Chronic administration of alogliptin, a novel, potent, and highly selective dipeptidyl peptidase-4 inhibitor, improves glycemic control and beta-cell function in obese diabetic ob/ob mice. Eur J Pharmacol. 2008 Jul 7;588(2-3):325-32.
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