产品说明书

AS1842856

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Chemical Structure| 836620-48-5 同义名 : FOXO1 Inhibitor
CAS号 : 836620-48-5
货号 : A169136
分子式 : C18H22FN3O3
纯度 : 99%+
分子量 : 347.384
MDL号 : MFCD30718173
存储条件:

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 4 mg/mL(11.51 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.88mL

0.58mL

0.29mL

14.39mL

2.88mL

1.44mL

28.79mL

5.76mL

2.88mL

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