| 产品描述: | DPP-4 抑制剂;DPP-4 Inhibitors;;InformationTrelagliptin succinate Trelagliptin succinate (SYR472) is a dipeptidyl peptidase IV (DPP-4) inhibitor which is used as a new long-acting drug for once-weekly treatment of type 2 diabetes mellitus (DM).TargetsDPP-4 (Cell-free assay) 4 nMIn vitroTrelagliptin is selective over other related DPP enzymes, P450 enzymes and hERG channel. It exhibits approximately 4- and 12-fold more potent inhibition against human dipeptidyl peptidase-4 than alogliptin and sitagliptin, respectively, and >10,000-fold selectivity over related proteases including dipeptidyl peptidase-8 and dipeptidyl peptidase-9. Kinetic analysis reveals reversible, competitive and slow-binding inhibition of dipeptidyl peptidase-4 by trelagliptin (t1/2 for dissociation ≈ 30 minutes). X-ray diffraction data indicates a non-covalent interaction between dipeptidyl peptidase and trelagliptin. |
| 体内研究: |
Trelagliptin (oral gavage; 7 mg/kg; single dose) shows sustained PD effect in dogs and gives >80% inhibition of DPP-4 activity even after 24h. Trelagliptin (oral gavage; 3 mg/kg; single dose; 60 min prior to oral glucose) significantly improves the glucose tolerance capacity by decreasing the AUC0 120min of 19.3% compared with the vehicle group in ob/ob mice. Trelagliptin (oral gavage; 10 mg/kg; once a week; 8 weeks) caused significant reductions in fasting blood glucose (FBG) levels, and the average reduction during the entire treatment period is 16.8% compared to the control.It also increases insulin level and raised it by 1.7-fold in AUC0 120min in ob/ob mice. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.103 ml |
10.516 ml |
21.032 ml |
| 5 mM |
0.421 ml |
2.103 ml |
4.206 ml |
| 10 mM |
0.21 ml |
1.052 ml |
2.103 ml |
| 50 mM |
0.042 ml |
0.21 ml |
0.421 ml |
|
| 注意: |
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