半岛bd体育手机客户端 说明
一般描述
A cell-permeable oxodihydroquinoline that preferentially inhibits the transcription activity of Forkhead box O family member Foxo1 over that of the functionally related Foxo3a and Foxo4 (70%, 20%, and 3% inhibition, respectively, in HepG2-based reporter assays; [AS184256] = 100 nM) in a dose-dependent manner (IC50= 33 nM) via direct binding of the non-Ser256-phosphorylated/active Foxo1, but not the Ser256-phosphorylated/inactive form of Foxo1. Shown to inhibit gluconeogenesis in rat heptoma Fao cultures (IC50= 37 and 130 nM against PEPCK and G6Pase mRNA level; IC50= 43 nM against glucose production)in vitroand in murine liver of both normoglycemic ICR mice (60% and 45% inhibition of hepatic G6Pase and PEPCK mRNA level, respectively; three 100 mg/kg p.o. dosages at 0, 12, 24 h) and diabeticdb/dbmice (86%, 70%, 56%, 48%, 35%, and 31% inhibition of hepatic G6Pase, ABCG8, ABCG5, PEPCK, IL-1β, and apoCIII mRNA level, respectively; three 100 mg/kg p.o. dosages at 0, 12, 24 h) during a 26-hour fasting periodin vivo.
生化/生理作用
Cell permeable: yes
Reversible: yes
Primary Target
Foxo1
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
外形
A 50 mM (5 mg/288 ?L) sterile-filtered solution of Foxo1 Inhibitor, AS1842856 (Cat. No. 344355) in DMSO.
重悬
Following initial thaw, aliquot and freeze (-20°C). Aliquots are stable for up to 6 months at -20°C.
其他说明
Nagashima, T., et al. 2010.Mol. Pharmacol.78,961.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C18H22FN3O3 |
| 分子量 | 347.38 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | liquid |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze avoid repeated freeze/thaw cycles desiccated (hygroscopic) protect from light |
| 储存温度 | ?70℃ |
安全信息
| 储存分类代码 | 10 - Combustible liquids |
| WGK | WGK 1 |
| 闪点(F) | 188.6 °F - (refers to pure substance) |
| 闪点(C) | 87 ℃ - (refers to pure substance) |
Sigma-Aldrich
m.cnreagent.com
