GSK837149A
目录号 : GC15820
A selective FASN inhibitor
Cas No.:13616-29-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
GSK837149A is a selective and reversible inhibitor of fatty acid synthase (FAS) [1].
Fatty acids are essential for all the living cells and have a diversity of biological functions. Fatty acids are fundamental aliphatic acids served as energy production and storage, cellular structure and as intermediates in the biosynthesis of hormones and other biologically important molecules. In cells, fatty acids provide structural integrity to cellular membranes and cell walls. Fatty acids have been also involved in the transmission of cellular signals and can be used to modify proteins during post-translational processing. Fatty acid synthase has been involved in catalyzing the formation of long-chain fatty acids from acetyl-CoA and malonyl-CoA in the presence of NADPH [1].
GSK837149A inhibited FAS in a reversible manner, with a Ki value of ~30 nm. GSK837149A possibly bound to the enzyme–ketoacyl-ACP complex [1]. GSK837149A selectively and reversibly inhibited the activity of FAS with the pIC50 of 7.8 [1]. GSK837149A functioned by inhibiting the β-ketoacyl reductase activity of FAS [1].
Reference:
[1] Vázquez M J, Leavens W, Liu R, et al. Discovery of GSK837149A, an inhibitor of human fatty acid synthase targeting the β‐ketoacyl reductase reaction[J]. FEBS journal, 2008, 275(7): 1556-1567.
| Cas No. | 13616-29-0 | SDF | |
| 化学名 | 4,4'-(carbonyldiimino)bis[N-(4-methyl-2-pyrimidinyl)-benzenesulfonamide | ||
| Canonical SMILES | CC1=CC=NC(NS(C2=CC=C(NC(NC3=CC=C(S(NC4=NC=CC(C)=N4)(=O)=O)C=C3)=O)C=C2)(=O)=O)=N1 | ||
| 分子式 | C23H22N8O5S2 | 分子量 | 554.6 |
| 溶解度 | ≤5mg/ml in DMSO;5mg/ml in dimethyl formamide | 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 | 1.8031 mL | 9.0155 mL | 18.031 mL |
| 5 mM | 0.3606 mL | 1.8031 mL | 3.6062 mL |
| 10 mM | 0.1803 mL | 0.9016 mL | 1.8031 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。