您的位置：首页 > 产品中心 > Foxo1 Inhibitor, AS1842856-Calbiochem
Foxo1 Inhibitor, AS1842856-Calbiochem
| 产品编号： | 4156948 |
| 规格： | Foxo1 Inhibitor, AS1842856, is a cell-permeable inhibitor that blocks the transcription activity of Foxo1 (IC50 = 33 nM). Directly binds to the active Foxo1, but not the Ser256-phosphorylated form. |
| 包装规格： | 10 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
Foxo1 Inhibitor, AS1842856-Calbiochem
5-Amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C18H22FN3O3 |
| Molecular weight | 347.38 |
| MDL number | MFCD30718173 |
| General description【一般描述】 | A cell-permeable oxodihydroquinoline that preferentially inhibits the transcription activity of Forkhead box O family member Foxo1 (IC50 = 33 nM) over that of the functionally related Foxo3a and Foxo4 (70%, 20%, and 3% inhibition, respectively, in HepG2-based reporter assays; [AS184256] = 100 nM) via direct binding of the active Foxo1, but not the Ser256-phosphorylated/inactive form of Foxo1. Shown to inhibit gluconeogenesis in rat heptoma Fao cultures (IC50 = 43 nM against glucose production) in vitro and in liver of both non-diabetic and diabetic mice during a 26-hour fasting period (100 mg/kg/8 h p.o.) in vivo. Also available as a 50 mM solution in DMSO (Cat. No. 506081). 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 vitro and 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 diabetic db/db mice (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 period in vivo. |
| Warning【警告】 | Toxicity: Regulatory Review (Z) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. |
| Other Notes【其他说明】 | Nagashima, T., et al. 2010. Mol. Pharmacol.78, 961. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | off-white to tan tan to yellow |
| solubility【溶解性】 | DMSO: 5 mg/mL |
| shipped in【运输】 | ambient |
| storage temp.【储存温度】 | 2-8℃ |
| SMILES string | O=C1C(C(O)=O)=CN(C2=C1C(N)=C(F)C(NC3CCCCC3)=C2)CC |
| packaging【包装】 | 10 mg in Glass bottle Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 1 |
