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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 851884-87-2 結(jié)構(gòu)式

基本信息

中文別名
化合物 T11401
英文別名
GKA50
GKA-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(xué)性質(zhì)

儲(chǔ)存條件-20°C
溶解度DMSO:可溶15mg/mL,澄清
形態(tài)粉末
顏色白色至米色

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
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
2024/11/08HY-15671GKA-50; GKA 50
GKA50
851884-87-21mg650元
2024/11/08HY-15671GKA-50; GKA 50
GKA50
851884-87-25mg1600元
2024/11/08HY-15671GKA-50; GKA 50
GKA50
851884-87-210mM * 1mLin DMSO1635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.
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