851884-87-2
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
GKA-50; GKA 50價格(試劑級)
報價日期 | 產品編號 | 產品名稱 | CAS號 | 包裝 | 價格 |
2024/11/08 | HY-15671 | GKA-50; GKA 50 GKA50 | 851884-87-2 | 1mg | 650元 |
2024/11/08 | HY-15671 | GKA-50; GKA 50 GKA50 | 851884-87-2 | 5mg | 1600元 |
2024/11/08 | 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. |