Evernic Acid (Synonyms: NSC 81164) |
| Catalog No.GC13238 |
inhibitor of two key plasmodial FAS-II enzymes PfFabZ and PfFabI
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 537-09-7
Sample solution is provided at 25 µL, 10mM.
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Evernic Acid is an inhibitor of two key plasmodial FAS-II enzymes PfFabZ and PfFabI
The Type II fatty acid synthase (FAS) system catalysed fatty acid biosynthesis in most bacteria. Fatty acids are aliphatic acids important for energy production and storage, cellular structure and as intermediates in the biosynthesis of hormones and other biologically important molecules. The FAS-II exists in archaea and bacteria, which has been characterized by the use of discrete, monofunctional enzymes for fatty acid synthesis. Inhibitors of this pathway (FASII) are being investigated as possible antibiotics. The bacterial FASII pathway is a promising target for the development of novel antimicrobial drugs [2]. Disruption of genes encoding mitochondrial FAS enzymes in yeast results in a respiratory-deficient phenotype and small rudimentary mitochondria [3].
Evernic acid was a secondary metabolite produced by some species of lichen. Evernic acid bound to allosteric sites on the protein surface of FAS-II enzymes and produced antibacterial and antiplasmodial effects. Evernic acid inhibited PfFabZ and PfFabI with the IC50 values of 10.7 and 36.1 μM, respectively. Evernic acid showed low efficacy against the malaria parasite P. berghei with an IC50 of 77.3 μM [1].
References:
[1] Lauinger I L, Vivas L, Perozzo R, et al. Potential of lichen secondary metabolites against Plasmodium liver stage parasites with FAS-II as the potential target[J]. Journal of natural products, 2013, 76(6): 1064-1070.
[2] Marrakchi H, Zhang Y M, Rock C O. Mechanistic diversity and regulation of Type II fatty acid synthesis[J]. 2002.
[3] Hiltunen J K, Schonauer M S, Autio K J, et al. Mitochondrial fatty acid synthesis type II: more than just fatty acids[J]. Journal of Biological Chemistry, 2009, 284(14): 9011-9015.
| Cas No. | 537-09-7 | SDF | |
| Synonyms | NSC 81164 | ||
| Chemical Name | 2-hydroxy-4-[(2-hydroxy-4-methoxy-6-methylbenzoyl)oxy]-6-methyl-benzoic acid | ||
| Canonical SMILES | CC1=CC(OC(C2=C(C)C=C(OC)C=C2O)=O)=CC(O)=C1C(O)=O | ||
| Formula | C17H16O7 | M.Wt | 332.3 |
| Solubility | ≤0.5mg/ml in ethanol;10mg/ml in DMSO;10mg/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 | 3.0093 mL | 15.0466 mL | 30.0933 mL |
| 5 mM | 0.6019 mL | 3.0093 mL | 6.0187 mL |
| 10 mM | 0.3009 mL | 1.5047 mL | 3.0093 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
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 33 reference(s) in Google Scholar.)
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