FT113
目录号 : GC64974FT113 is a potent inhibitor of fatty acid synthase (FAS/FASN) with ic50 of 213 nM.
Cas No.:1630808-89-7
Sample solution is provided at 25 µL, 10mM.
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FT113 is a potent inhibitor of fatty acid synthase (FAS/FASN) with ic50 of 213 nM.
[1] Martin MW,et al.Bioorg Med Chem Lett.2019 15;29(8):1001-1006.
Cas No. | 1630808-89-7 | SDF | Download SDF |
分子式 | C22H20FN3O4 | 分子量 | 409.41 |
溶解度 | DMSO : 62.5 mg/mL (152.66 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.4425 mL | 12.2127 mL | 24.4254 mL |
5 mM | 0.4885 mL | 2.4425 mL | 4.8851 mL |
10 mM | 0.2443 mL | 1.2213 mL | 2.4425 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN)
Bioorg Med Chem Lett 2019 Apr 15;29(8):1001-1006.PMID:30803804DOI:10.1016/j.bmcl.2019.02.012
The discovery, structure-activity relationships, and optimization of a novel class of fatty acid synthase (FASN) inhibitors is reported. High throughput screening identified a series of substituted piperazines with structural features that enable interactions with many of the potency-driving regions of the FASN KR domain binding site. Derived from this series was FT113, a compound with potent biochemical and cellular activity, which translated into excellent activity in in vivo models.