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2041073-22-5

中文名稱 GNF4877
英文名稱 GNF4877
CAS 2041073-22-5
分子式 C25H27FN6O4
分子量 494.52
MOL 文件 2041073-22-5.mol
更新日期 2024/12/23 10:32:13
2041073-22-5 結(jié)構(gòu)式 2041073-22-5 結(jié)構(gòu)式

基本信息

中文別名
化合物GNF4877
英文別名
GNF4877
CID 139600315
CID 139600315(GNF-4877)
3-Piperidinecarboxylic acid, 1-[3-[[[3-amino-6-[2-fluoro-5-(1-methylethoxy)phenyl]-2-pyrazinyl]carbonyl]amino]-4-pyridinyl]-, (3R)-

物理化學(xué)性質(zhì)

沸點669.7±55.0 °C(Predicted)
密度1.367±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度DMSO: 4.17 mg/mL (8.43 mM and warming)
酸度系數(shù)(pKa)2.82±0.70(Predicted)
形態(tài)Solid
顏色Light yellow to yellow

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
GNF4877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
2024/11/08HY-129492GNF4877
GNF4877
2041073-22-51 mg1700元
2024/11/08HY-129492GNF4877
GNF4877
2041073-22-55mg5300元
2024/08/19HY-129492GNF4877
GNF4877
2041073-22-510mg8400元

常見問題列表

生物活性
GNF4877是 DYRK1A 和 GSK3β 的有效抑制劑,IC50 值分別為 6 nM 和 16 nM,可導(dǎo)致 NFATc 核輸出受阻并增加 β 細(xì)胞增殖 (對小鼠 β (R7T1) 細(xì)胞的 EC50 值為 0.66 μM)。
靶點

GSK3β

16 nM (IC 50 )

DYRK1A

6 nM (IC 50 )

體外研究

High glucose concentrations and glucokinase activators (GKAs) increase Ca 2+ signalling in β-cells, and increase intracellular Ca 2+ leads to activation of calcineurin and nuclear translocation of NFATc proteins. Indeed, concentrations of GNF4877 ((0.1?μM, 0.3?μM) well below the EC 50 for β-cell proliferation are able to induce proliferation in the presence of high glucose or pharmacological activators of glucokinase. Finally, increasing intracellular Ca 2+ with glibenclamide (a sulfonylurea receptor 1 inhibitor) or Bay K8644 (an L-type Ca 2+ channel activator) show additive activity with GNF4877.

體內(nèi)研究

GNF4877 (50 mg/kg; oral gavage; twice a day; for 15 days; double transgenic RIP-DTA male mice) treatment induces β-cell proliferation, increases β-cell mass and insulin content, and improves glycaemic control.

Animal Model: Double transgenic RIP-DTA male mice (Tg (Ins 2-rtTA) 2 Efr Tg (teto-DTA) 1 Gfi/J) with Doxycycline (28.8±2.4?g; 82±2 days)
Dosage: 50 mg/kg
Administration: Oral gavage; twice a day; for 15 days
Result: Induced β-cell proliferation, increased β-cell mass and insulin content, and improved glycaemic control.
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