GKA-50; GKA 50
| 中文名称 | GKA-50; GKA 50 |
|---|---|
| 中文同义词 | 化合物 T11401;化合物 GKA50;GKA 50,葡萄糖激酶激活剂 |
| 英文名称 | GKA-50 |
| 英文同义词 | GKA 50;GKA50;GKA-50;6-[[3-[(1S)-2-Methoxy-1-Methylethoxy]-5-[(1S)-1-Methyl-2-phenylethoxy]benzoyl]aMino]-3-pyridinecarboxylic Acid;OCBMECSFDVUYQN-ROUUACIJSA-N;GKA-50; GKA 50;3-Pyridinecarboxylic acid, 6-[[3-[(1S)-2-methoxy-1-methylethoxy]-5-[(1S)-1-methyl-2-phenylethoxy]benzoyl]amino]- |
| CAS号 | 851884-87-2 |
| 分子式 | C26H28N2O6 |
| 分子量 | 464.51 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 851884-87-2.mol |
| 结构式 |  |
GKA-50; GKA 50 性质
| 沸点 | 607.0±55.0 °C(Predicted) |
|---|---|
| 密度 | 1.247±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 溶解度 | DMSO：可溶15mg/mL，澄清 |
| 酸度系数(pKa) | 3.49±0.10(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至米色 |
| InChIKey | OCBMECSFDVUYQN-ROUUACIJSA-N |
| SMILES | N(c3ncc(cc3)C(=O)O)C(=O)c1cc(cc(c1)O[C@H](Cc2ccccc2)C)O[C@H](COC)C |
GKA50 是一种有效的葡萄糖激酶 (glucokinase) 激活剂 (EC50=33 nM)。GKA50 刺激小鼠胰岛和 MIN6 细胞分泌胰岛素。GKA50 对高脂高脂脂肪雌性大鼠有显著的降糖作用。
GKA50 (0.01-100 μM; 24 hours) enhances INS-1 cell proliferation with EC
50
values ranging from 1 to 2 μM.
GKA50 (1.2 μM+40 μM glucose; 2-4 days) treatment reduces apoptosis induced by chronic high glucose in INS-1 cells.
GKA50 activates human glucokinase enzymatic activity with an EC
50
of 0.022 μM. GKA50 stimulates insulin secretion in the pancreatic insulinoma cell line, INS-1, with an EC
50
of 0.065 μM. GKA50 reduces chronic-high-glucose-induced apoptosis via modulation of glucokinase and apoptotic protein BAD.
Cell Proliferation Assay
| Cell Line: | INS-1 cells (starved overnight with 3 μM glucose) |
| Concentration: | 0.01-100 μM |
| Incubation Time: | 24 hours |
| Result: | Stimulated cell proliferation in a dose-dependent manner, with EC 50 values ranging from 1 to 2 μM. |
GKA50 (1-30 mg/kg; p.o.) gives significant glucose lowering in an oral glucose tolerance test.
| Animal Model: | High-fat-fed obese female Zucker (fa/fa) rats |
| Dosage: | 1, 3, 10, 30 mg/kg |
| Administration: | Oral administration |
| Result: | Significant percentage glucose lowering. |
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2025/12/22 | HY-15671 | GKA-50; GKA 50 GKA50 | 851884-87-2 | 1mg | 650元 |
| 2025/12/22 | HY-15671 | GKA-50; GKA 50 GKA50 | 851884-87-2 | 5mg | 1600元 |