GSK837149A |
| Catalog No.GC15820 |
selective, reversible inhibitor of fatty acid synthase(FAS)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 13616-29-0
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Chemical Name | 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 | ||
| Formula | C23H22N8O5S2 | M.Wt | 554.6 |
| Solubility | ≤5mg/ml in DMSO;5mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)
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