| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| G408680-1ml |
1ml |
现货  |
|
| 英文别名 | 5-((1-(3-isopropyl-1,2,4-oxadiazol-5-yl)piperidin-4-yl)methoxy)-2-(4-(methylsulfonyl)phenyl)pyridine |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | GSK1292263 |
| 生化机理 | GSK1292263 是一种新型 GPR119 激动剂，具有治疗 2 型糖尿病的潜力。第二阶段 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 激动剂 |
| 作用机制 | 葡萄糖依赖性胰岛素受体激动剂 |
| 产品介绍 |
GSK1292263是PR119受体激动剂，可用于2型糖尿病。 Information GSK1292263 GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2. GSK-1292263 is selected from 1538 compounds by using Hypo1, the Fit-Value and Estimate of GSK-1292263 that is aligned in Hypo1 are 8.8 and 7.7 (nM), respectively. In vivo GSK-1292263 administrated at a single dose of 3-30 mg/kg in the absence of nutrients correlates with increased levels of circulating gastrointestinal peptides, including Glukagon-like peptide 1 (GLP-1), gastric inhibitory polypeptide (GIP), peptide YY (PYY) and Glukagon in male Sprague-Dawley rats, the increase is enhanced following administration of glucose in the oral glucose tolerance test (OGTT). GSK-129226 significant increases in the peak insulin response and insulin AUC(0-15 min) of 30-60% compared with values in the vehicle control cohort in the intravenous glucose tolerance test in rats, this insulin upregulation correlated with a significant increase in the glucose disposal rate. GSK-1292263 is associated with a statistically significant increase in insulin immunoreactivity in pancreatic sections in a 6-week study performed in Zucker diabetic fatty rats, compared with insulin immunoreactivity in samples obtained from rats receiving vehicle control. GSK-1292263 administrated at dose of 10 or 30 mg/kg or vehicle control at 2 hours prior to insulin infusion in hyperinsulinemic-euglycemic clamps stimulates Glukagon secretion without increasing blood glucose levels Sprague-Dawley rats. cell lines： Concentrations： Incubation Time： Powder Purity:≥99% |
| ALogP | 3.893 |
|---|---|
| hba_count | 7 |
| Rotatable Bond | 7 |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CC(C)C1=NOC(=N1)N2CCC(CC2)COC3=CN=C(C=C3)C4=CC=C(C=C4)[S](C)(=O)=O |
| 分子量 | 456.56 |
| Reaxy-Rn | 19915189 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=19915189&ln= |
| DMSO(mg / mL) Max Solubility | 34 |
|---|---|
| DMSO(mM) Max Solubility | 74.47 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 19915189 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=19915189&ln= |
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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