| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| L407945-1ml |
1ml |
现货  |
|
| 别名 | 利格列汀 (BI-1356) |
|---|---|
| 英文别名 | (R)-8-(3-aminopiperidin-1-yl)-7-(but-2-ynyl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-1H-purine-2,6(3H,7H)-dione |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Linagliptin (BI-1356) |
| 生化机理 | 利拉利汀（BI-1356）是一种强效、选择性 DPP-4 抑制剂，其 IC50 值为 1 nM，对 DPP-4 的选择性比对 DPP-2、DPP-8 和 DPP-9 等其他二肽基肽酶的选择性高 10,000 倍。利拉利汀能在2型糖尿病模型中激活肾小球自噬。DPP4在TP53缺陷的CRC细胞中介导铁变态反应。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 二肽基肽酶 IV 抑制剂 |
| 产品介绍 |
Linagliptin是一种高效的，选择性的DPP-4抑制剂，IC50为1 nM。A highly potent, selective CD26 (DPP-4) inhibitor. Information Linagliptin (BI-1356) Linagliptin (BI-1356) is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM and exhibits a 10,000-fold higher selectivity for DPP-4 than for other dipeptidyl peptidases such as DPP-2, DPP-8, and DPP-9. Linagliptin activat Linagliptin shows a potent inhibition effect against DPP-4 in vitro and a low affinity for hERG channel and M1 receptor (IC50 295 nM). Linagliptin acts as a competitive inhibitor with a Ki of 1 nM, and also shows 10,000-fold more selectivity for DPP-4 than DPP-8, DPP-9, amino-peptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin, and 90-fold more selectivity than fibroblast activation protein in vitro. In vivo In male Wistar rats, Beagle dogs, and Rhesus monkeys, Linagliptin shows a highly efficacious, long-lasting, and potent inhibitory activity against DPP-4 by more than 70% inhibition for all three species after oral administration of 1 mg/kg. Oral administration of Linagliptin to db/db mice 45 min before an oral glucose tolerance test reduces plasma glucose excursion in a dose-dependent manner from 0.1 mg/kg (15% inhibition) to 1 mg/kg (66% inhibition). By inhibiting DPP-4 activity, Linagliptin reduces the expression of the proinflammatory markers cyclooxygenase-2 and macrophage inflammatory protein-2, and enhances the formation of myofibroblasts in healing wounds from ob/ob mice. cell lines： Concentrations： Incubation Time： Powder Purity:≥99% |
| ALogP | 2.718 |
|---|---|
| hba_count | 5 |
| HBD Count | 1 |
| Rotatable Bond | 5 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CC#CC[N]1C(=NC2=C1C(=O)N(CC3=NC4=CC=CC=C4C(=N3)C)C(=O)N2C)N5CCCC(N)C5 |
| 分子量 | 472.54 |
| Reaxy-Rn | 23529727 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23529727&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 50 mg/mL (61.55 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|---|
| DMSO(mg / mL) Max Solubility | 17 |
| DMSO(mM) Max Solubility | 35.98 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 23529727 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23529727&ln= |
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