851884-87-2
中文名称
GKA-50; GKA 50
英文名称
GKA-50
CAS
851884-87-2
分子式
C26H28N2O6
分子量
464.51
MOL 文件
851884-87-2.mol
更新日期
2025/04/28 09:05:23
851884-87-2 结构式
基本信息
中文别名
化合物 T11401 英文别名
GKA50GKA-50
GKA 50
GKA-50
GKA 50
OCBMECSFDVUYQN-ROUUACIJSA-N
6-[[3-[(1S)-2-Methoxy-1-Methylethoxy]-5-[(1S)-1-Methyl-2-phenylethoxy]benzoyl]aMino]-3-pyridinecarboxylic Acid
物理化学性质
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
GKA-50; GKA 50价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/02/08 | HY-15671 | GKA-50; GKA 50 GKA50 | 851884-87-2 | 1mg | 650元 |
| 2025/02/08 | HY-15671 | GKA-50; GKA 50 GKA50 | 851884-87-2 | 5mg | 1600元 |
| 2025/02/08 | HY-15671 | GKA-50; GKA 50 GKA50 | 851884-87-2 | 10mM * 1mLin DMSO | 1635元 |
常见问题列表
生物活性
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。体外研究
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. |
体内研究
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. |