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Merck
CN

344355

AS1842856

≥98% (HPLC), solid, Foxo1 inhibitor, Calbiochem®

别名:

Foxo1 抑制剂,AS1842856

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关于此项目

经验公式(希尔记法):
C18H22FN3O3
化学文摘社编号:
分子量:
347.38
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
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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.

Quality Level

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

off-white to tan, tan to yellow

solubility

DMSO: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

SMILES string

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

General description

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。

Packaging

用惰性气体包装

Preparation Note

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。

Other Notes

Nagashima, T., et al. 2010.Mol.Pharmacol.78, 961.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

毒性:监管审查(Z)


存储类别

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable



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货号GTIN
344355-10MG07790788059712