Trelagliptin succinate
产品说明书
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同义名 : | 曲格列汀琥珀酸盐 ;SYR-472 succinate; SYR472; Trelagliptin(succinate) |
| CAS号 : | 1029877-94-8 | |
| 货号 : | A147484 | |
| 分子式 : | C22H26FN5O6 | |
| 纯度 : | 99% | |
| 分子量 : | 475.47 | |
| MDL号 : | MFCD22665720 | |
| 存储条件： |
Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 50 mg/mL(105.16 mM)，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: 100 mg/mL(210.32 mM)，配合低频超声助溶 |
| 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)[3]. Trelagliptin succinate, a novel DPP4 inhibitor, shows sustained efficacy by once-weekly dosing in type 2 diabetes patients and it exhibits >10,000-fold selectivity over related proteases including DPP8 and DPP9. Trelagliptin exhibited potent inhibitory activity toward DPP4 prepared from Caco-2 cells with an IC50 value of 5.4 nM. It also inhibited human, dog, and rat plasma DPP4 activity with IC50 values of 4.2, 6.2, and 9.7 nM respectively. In a phase 2 dose-ranging study using a sigmoid Emax model, the plasma trelagliptin concentration estimated to yield 50% and 70% inhibition of plasma DPP4 activity was 1.43 ng/mL and 2.31 ng/mL, respectively[4]. | ||
| 作用机制 | The aminopiperidine forms a salt bridge to Glu205/Glu206, while the cyanobenzyl group effectively fills the S1 pocket and interacts with Arg125. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.10mL 0.42mL 0.21mL |
10.52mL 2.10mL 1.05mL |
21.03mL 4.21mL 2.10mL |
| 参考文献 |
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