|5-氨基-7-(环己基氨基)-1-乙基-6-氟-4-氧代-1,4-二氢喹啉-3-羧酸|CsnPharm

CAS No.: 836620-48-5

AS1842856 Catalog No. CSN19073

Synonyms: FOXO1 Inhibitor

AS-1842856 is a potent inhibitor of forkhead box class O transcription factor 1 (Foxo1) with IC50 of 33 nM in HepG2 cells which directly bind to the active Foxo1.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述The forkhead box protein O1 (Foxo1) is a transcription factor that plays a critical role in hepatic gluconeogenesis. AS-1842856 is a Foxo1 inhibitor with an IC50 value of 0.03μM. In HepG2 cells transiently transfected with vectors carrying human Foxo1, AS-1842856 inhibited Foxo1 activity in a dose-dependent manner. AS-1842856 at a concentration of 0.1μM decreased Foxo1-mediated transactivation by 70%. Treatment of Fao cells with AS-1842856 for 18 hours inhibited the mRNA expression of G6Pase and PEPCK with IC50 values of 0.13μM and 0.037μM, respectively. Treatment of Fao cells with AS-1842856 (0.1 – 10μM) alone or in combination with insulin (0.1 – 10nM) did not affect the phosphorylation state of Akt, ERK, or S6K. In ICR mice, oral administration of AS-1842856 (100mg/kg) at three time points (8AM, 6PM, and 8AM on the second day) during 26-h fasting significantly reduced the mRNA expression of G6Pase and PEPCK in the liver, but did not alter the plasma glucose level.^[3]
作用机制AS-1842856 inhibits Foxo1-mediated transactivation by directly binding to Foxo1.^[3]
参考文献

[1] Tan P, Guan H, et al. FOXO1 inhibits osteoclastogenesis partially by antagnozing MYC. Sci Rep. 2015 Nov 16;5:16835.
[2] Nagashima T, Shigematsu N, et al. Discovery of novel forkhead box O1 inhibitors for treating type 2 diabetes: improvement of fasting glycemia in diabetic db/db mice. Mol Pharmacol. 2010 Nov;78(5):961-70.
[3] Nagashima T, Shigematsu N, Maruki R, Urano Y, Tanaka H, Shimaya A, Shimokawa T, Shibasaki M. Discovery of novel forkhead box O1 inhibitors for treating type 2 diabetes: improvement of fasting glycemia in diabetic db/db mice. Mol Pharmacol. 2010 Nov;78(5):961-70

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8787 mL
- 14.3935 mL
- 28.7869 mL
- 5 mM
- 0.5757 mL
- 2.8787 mL
- 5.7574 mL
- 10 mM
- 0.2879 mL
- 1.4393 mL
- 2.8787 mL

技术信息

CAS号

836620-48-5

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H22FN3O3

运输

蓝冰

分子量

347.38

别名

FOXO1 Inhibitor

溶解度

DMSO	23.0 mg/mL (66.2 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

AS1842856 Catalog No. CSN19073

靶点选择性

请登录您的专属账户

确认信息