851884-87-2
中文名稱
GKA-50; GKA 50
英文名稱
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 結構式
基本信息
中文別名
化合物 T11401 英文別名
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
物理化學性質
沸點607.0±55.0 °C(Predicted)
密度1.247±0.06 g/cm3(Predicted)
儲存條件-20°C
溶解度DMSO：可溶15mg/mL，澄清
酸度系數(shù)(pKa)3.49±0.10(Predicted)
形態(tài)粉末
顏色白色至米色
GKA-50; GKA 50價格(試劑級)
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 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 |
| 2025/12/22 | HY-15671 | GKA-50; GKA 50 GKA50 | 851884-87-2 | 10mM * 1mLin DMSO | 1635元 |
常見問題列表
生物活性
GKA50 是一種有效的葡萄糖激酶 (glucokinase) 激活劑 (EC50=33 nM)。GKA50 刺激小鼠胰島和 MIN6 細胞分泌胰島素。GKA50 對高脂高脂脂肪雌性大鼠有顯著的降糖作用。體外研究
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. |
體內(nèi)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. |