产品说明书

Alogliptin

Print
Chemical Structure| 850649-61-5 同义名 : 阿洛利停 ;SYR-322 free base;SYR 322
CAS号 : 850649-61-5
货号 : A295732
分子式 : C18H21N5O2
纯度 : 98%
分子量 : 339.392
MDL号 : MFCD09833196
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(309.38 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 10 mg/mL(29.46 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
描述 Dipeptidylpeptidase 4 (DPP4) belongs to the S9b gene family of postproline serine peptidases. It acts mostly as a secreted membrane protein, mediating the degradation and inactivation of glucagon-like peptide (GLP)-1 and gastric inhibitory protein (GIP). Alogliptin is a potent, selective inhibitor of the DPP-4 with IC50 value of 2.63 nM in enzymatic assay. And it has nearly 1000-fold higher IC50 for DPP8/9 inhibition than for DPP4 inhibition[3]. In rats, dogs, and monkeys, the absolute oral bioavailability of alogliptin was 45%, 86%, and 72% to 88%, respectively. After a single oral dose of alogliptin, plasma DPP-4 inhibition was observed within 15 min and maximum inhibition was > 90% in rats, dogs, and monkeys; inhibition was sustained for 12 h in rats (43%) and dogs (65%) and 24 h in monkeys (> 80%). In Zucker fa/fa rats, a single dose of alogliptin (0.3, 1, 3, and 10 mg/kg) inhibited plasma DPP-4 (91% to 100% at 2 h and 20% to 66% at 24 h), increased plasma concentration of GLP-1 and early-phase insulin secretion and reduced blood glucose excursion after oral glucose challenge[4].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03492580 - Completed - United States, New Jersey ... 展开 >> Janssen Investigative Site Titusville, New Jersey, United States, 08560 收起 <<
NCT02312427 Heart Failure ... 展开 >> Diabetes Mellitus 收起 << Phase 4 Completed - Japan ... 展开 >> Mitsui Memorial Hospital Taito-ku, Tokyo, Japan 收起 <<
NCT02528019 Effects of the DPP-4 Inhibitor... 展开 >>s or SGLT2 Inhibitors on the Protective Actions for Diabetic Complications 收起 << Phase 4 Unknown August 2018 Japan ... 展开 >> Kurume University Hospital Recruiting Kurume city, Japan, 830-0011 Contact: Nobuhiro Tahara, MD, PhD    +81-942-31-7580    ntahara@med.kurume-u.ac.jp    Contact: Sho-ichi Yamagishi, MD, PhD    +81-942-31-7562       Principal Investigator: Nobuhiro Tahara, MD, PhD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.95mL

0.59mL

0.29mL

14.73mL

2.95mL

1.47mL

29.46mL

5.89mL

2.95mL
参考文献

[1]Moritoh Y, Takeuchi K, 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.

[2]Feng J, Zhang Z, 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.

[3]Huan Y, Jiang Q, Liu JL, Shen ZF. Establishment of a dipeptidyl peptidases (DPP) 8/9 expressing cell model for evaluating the selectivity of DPP4 inhibitors. J Pharmacol Toxicol Methods. 2015 Jan-Feb;71:8-12. doi: 10.1016/j.vascn.2014.11.002. Epub 2014 Nov 15. PMID: 25464020.

[4]Lee B, Shi L, Kassel DB, Asakawa T, Takeuchi K, Christopher RJ. Pharmacokinetic, pharmacodynamic, and efficacy profiles of alogliptin, a novel inhibitor of dipeptidyl peptidase-4, in rats, dogs, and monkeys. Eur J Pharmacol. 2008 Jul 28;589(1-3):306-14. doi: 10.1016/j.ejphar.2008.04.047. Epub 2008 Apr 26. PMID: 18538760.