推荐产品
产品名称
Foxo1 抑制剂，AS1842856, 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.
质量水平
方案
≥98% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
off-white to tan
tan to yellow
溶解性
DMSO: 5 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
O=C1C(C(O)=O)=CN(C2=C1C(N)=C(F)C(NC3CCCCC3)=C2)CC
InChI
1S/C18H22FN3O3/c1-2-22-9-11(18(24)25)17(23)14-13(22)8-12(15(19)16(14)20)21-10-6-4-3-5-7-10/h8-10,21H,2-7,20H2,1H3,(H,24,25)
InChI key
MOMCHYGXXYBDCD-UHFFFAOYSA-N
一般描述
一种细胞可渗透性的氧代二氢喹啉，比功能相关的Foxo3a和Foxo4优先抑制Forkhead box O家族成员Foxo1的转录活性（在基于HepG2的报告基因分析中分别抑制70%，20%和3%；[AS184256]=100 nM），通过直接结合非Ser256磷酸化/活性Foxo1，而不是Ser256磷酸化/非活性形式的Foxo1以剂量依赖性方式（IC50=33 nM）结合。在体内26小时禁食期间，显示可在体外大鼠肝瘤Fao培养物（针对PEPCK和G6Pase mRNA水平，IC50=37和130 nM；针对葡萄糖的产生，IC50 =43 nM）和在正常血糖ICR小鼠（分别抑制肝G6Pase和PEPCK mRNA水平的60%和45%；3个在0、12、24小时的100 mg/kg p.o.剂量）以及糖尿病db/db小鼠的鼠肝中（对肝G6Pase，ABCG8，ABCG5，PEPCK，IL-1β和apoCIII mRNA水平分别为86%，70%，56%，48%，35%和31%；3个在0、12、24小时的100 mg/kg p.o.剂量）抑制糖异生。
一种细胞可渗透性的氧代二氢喹啉，比功能相关的Foxo3a和Foxo4优先抑制Forkhead box O家族成员Foxo1（IC50 = 33 nM）的转录活性（在基于HepG2的报告基因分析中分别抑制70%，20%和3%；[AS184256]=100 nM），通过直接结合活性Foxo1，而不是Ser256磷酸化/非活性形式的Foxo1。显示在体外大鼠肝瘤Fao培养物中抑制糖异生（针对葡萄糖产生的IC50=43 nM），在体内26小时禁食期间（100 mg/kg/8 h p.o.）抑制非糖尿病和糖尿病的小鼠肝脏中的糖异生。也可以50 mM的DMSO溶液（货号506081）提供。
包装
用惰性气体包装
警告
毒性：监管审查（Z）
重悬
复溶后，等分并冷冻保存（-20°C）。储备溶液在-20°C下可稳定保存至多3个月。
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
储存分类代码
11 - Combustible Solids
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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