产品说明书

AMG3969

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Chemical Structure| 1361224-53-4 同义名 : -
CAS号 : 1361224-53-4
货号 : A491672
分子式 : C21H20F6N4O3S
纯度 : 99%+
分子量 : 522.464
MDL号 : MFCD28386194
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(200.97 mM)，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 AMG-3969 demonstrates strong cellular activity, with an EC50 of 0.202 μM and IC50 of 4 nM [1]. It effectively counteracts GKRP's inhibition of GK activity and facilitates GK translocation in vitro (using isolated hepatocytes) [3].
作用机制 AMG-3969 may bind to a previously unknown binding pocket in GKRP distinct from that of the phosphofructose-binding site.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.57mL

1.91mL

0.96mL

19.14mL

3.83mL

1.91mL
参考文献

[1]Lloyd DJ, et al. Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors. Nature. 2013 Dec 19;504(7480):437-40.

[2]Nishimura N, et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series. J Med Chem. 2014 Apr 10;5

[3]St Jean DJ Jr, et al. Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles. J Med Chem. 2014 Jan 23;57(2):325-38.