Linagliptin
产品说明书
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同义名 : | 利格列汀 ;BI 1356;GSK2118436;Linagliptin. trade names Tradjenta and Trajenta |
| CAS号 : | 668270-12-0 | |
| 货号 : | A392251 | |
| 分子式 : | C25H28N8O2 | |
| 纯度 : | 99% | |
| 分子量 : | 472.542 | |
| MDL号 : | MFCD14635356 | |
| 存储条件： |
Pure form Keep in dark place,Inert atmosphere,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 25 mg/mL(52.91 mM)，配合低频超声，并水浴加热至45℃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 |
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| 动物实验配方： |
0.5% hydroxyethyl cellulose+water 30 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Dipeptidyl peptidase 4 (DPP4) is an intrinsic membrane glycoprotein and a serine exopeptidase that cleaves X-proline dipeptides from the N-terminus of polypeptides, which is ubiquitously expressed on the surface of a variety of cells. DPP4 selectively cleaves N-terminal dipeptides from a variety of substrates, including cytokines, growth factors, neuropeptides, and the incretin hormones. Linagliptin is a potent and selective DPP4 inhibitor with IC50 value of 0.77 nM[12]. In vitro, Linagliptin markedly reduces LPS induced expression of IL-6 in HUVECs at concentration ranging in 1 - 10 μM[7]. Treatment with 30 nM linagliptin for 3 days significantly inhibits podocyte growth. Treatment with 100 nM Linagliptin casued an increase in cells in the G0/G1 phase at 5 days in podocytes[13]. In vivo, linagliptin significantly inhibits DPP4 activity in kidney and plasma of diabetic mice. Oral administration of linagliptin at 5 mg/kg once daily for 24 weeks restored the normal kidney structure of STZ-induced diabetic kidney fibrosis in CD-1 mice[14]. Administration of linagliptin at 83 mg/kg to female C57BL/6 mice fed a western diet for 4 months ameliorated the develop western diet induced aortic and endothelial cell stiffness[15]. Oral administration of linagliptin at 10 mg/kg for 7 weeks significantly inhibits DPP-4 activity, and increases blood GLP-1 levels in HFD-fed mice. In addition, linagliptin decreases ischemic brain damage[16]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| CHO cells | Function assay | Displacement of [N-methyl-3H]scopolamine from human recombinant muscarinic M1 receptor expressed in CHO cells, IC50=0.295 μM | 18052023 | ||
| HEK293 cells | Function assay | Inhibition of mouse recombinant FAP expressed in HEK293 cells using Ala-Pro-p-nitroanilide as substrate incubated for 15 mins prior to substrate addition, IC50=0.37 μM | 24900696 | ||
| human Caco-2 cells | Function assay | Inhibition of DPP4 in human Caco-2 cells after 1 hr, IC50=1 nM | 18485703 | ||
| 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 |
| NCT02183376 | Hepatic Insufficiency | Phase 1 | Completed | - | - |
| NCT01778049 | Diabetes Mellitus, Type 2 | Phase 3 | Completed | - | - |
| NCT02183532 | Healthy | Phase 1 | Completed | - | - |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.12mL 0.42mL 0.21mL |
10.58mL 2.12mL 1.06mL |
21.16mL 4.23mL 2.12mL |
| 参考文献 |
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