851884-87-2
中文名稱(chēng)
GKA-50; GKA 50
英文名稱(chēng)
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
2024/12/05 21:11:26
851884-87-2 結(jié)構(gòu)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
安全數(shù)據(jù)
警示詞警告
危險(xiǎn)性描述H302-H413
防范說(shuō)明P273-P301+P312+P330
危險(xiǎn)品標(biāo)志Xn
危險(xiǎn)類(lèi)別碼22
WGK Germany3
GKA-50; GKA 50價(jià)格(試劑級(jí))
報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱(chēng) | CAS號(hào) | 包裝 | 價(jià)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(jiàn)問(wèn)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(xì)胞分泌胰島素。GKA50 對(duì)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. |