Nilofabicin
Based on 1 Customer Validation
Nilofabicin (CG-400549) is an anti-bacterialagent that targets FabI. Nilofabicin shows high selectivity for the genus Staphylococcus and weak activity against most Gram-negative bacteria. Nilofabicin inhibits bacterial fatty acid biosynthesis, blocks phospholipid synthesis, and disrupts the structure of bacterial cell membranes. Nilofabicin exhibits in vivo antibacterial efficacy in a mouse model of systemic Staphylococcus aureus infection. Nilofabicin can be used in studies related to bacterial infections.
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- Purity : 99.58%
- CAS No.: 934628-27-0
- 화학식: C19H20N2O2S
- 분자량:340.44
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
All Antibiotic Isoforms
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Biological Activity
제품 설명
In Vitro
Nilofabicin (CG-400549) exists in a total of 7 crystal forms, all of which exhibit excellent physical stability; they show different dissolution rates in artificial gastric juice at 37°C[1].
Nilofabicin potently inhibits the growth of MSSA and MRSA isolates; experiments inducing drug resistance via fabI overexpression, as well as the identification of the F204L mutation in nilofabicin-resistant S. aureus, confirm that FabI is its primary target[2].
Nilofabicin inhibits the growth of methicillin-resistant Staphylococcus aureus (MRSA) cells, with an MIC of 0.74 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 934628-27-0
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Appearance Solid
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분자량 340.44
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화학식 C19H20N2O2S
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Color White to off-white
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SMILES
O=C1C=C(OCCC2=CC=CS2)C=CN1CC3=CC=CC(N)=C3C
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Synonyms
CG-400549
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
In Vitro:
DMSO : 100 mg/mL (293.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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Gram Staining of Tissue Sections
Gram staining of tissue sections is a histochemical technique used to differentiate Gram-positive and Gram-negative bacteria within histological specimens based on differences in bacterial cell wall structure and dye retention, adapted from classical bacteriological Gram staining into tissue-compatible “histological Gram stain” variants. In tissue applications, modifications of the Brown-Hopps and Brown-Brenn methods are commonly used to improve differentiation of microorganisms embedded within host connective tissue and to reduce overstaining or loss of Gram-negative signal, which are known limitations of earlier approaches. The principle relies on crystal violet-iodine complex retention in Gram-positive organisms and subsequent decolorization and counterstaining steps that allow contrast visualization of Gram-negative organisms against tissue background.
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
순도&문서
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Data Sheet (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Kim BY, et al. Solid state of CG-400549, a novel FabI inhibitor: characterization, dissolution, transformation. Archives of pharmacal research. 2011 May;34(5):775-9. [Content Brief]
[2]. Douglas EJA, et al. Novel antimicrobial strategies to treat multi-drug resistant Staphylococcus aureus infections. Microbial biotechnology. 2023 Jul;16(7):1456-1474. [Content Brief]
[3]. Wang J, et al. Inhibitors of fatty acid synthesis in prokaryotes and eukaryotes as anti-infective, anticancer and anti-obesity drugs. Future medicinal chemistry. 2012 Jun;4(9):1113-51. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.9374 mL | 14.6869 mL | 29.3738 mL | 73.4344 mL |
| 5 mM | 0.5875 mL | 2.9374 mL | 5.8748 mL | 14.6869 mL | |
| 10 mM | 0.2937 mL | 1.4687 mL | 2.9374 mL | 7.3434 mL | |
| 15 mM | 0.1958 mL | 0.9791 mL | 1.9583 mL | 4.8956 mL | |
| 20 mM | 0.1469 mL | 0.7343 mL | 1.4687 mL | 3.6717 mL | |
| 25 mM | 0.1175 mL | 0.5875 mL | 1.1750 mL | 2.9374 mL | |
| 30 mM | 0.0979 mL | 0.4896 mL | 0.9791 mL | 2.4478 mL | |
| 40 mM | 0.0734 mL | 0.3672 mL | 0.7343 mL | 1.8359 mL | |
| 50 mM | 0.0587 mL | 0.2937 mL | 0.5875 mL | 1.4687 mL | |
| 60 mM | 0.0490 mL | 0.2448 mL | 0.4896 mL | 1.2239 mL | |
| 80 mM | 0.0367 mL | 0.1836 mL | 0.3672 mL | 0.9179 mL | |
| 100 mM | 0.0294 mL | 0.1469 mL | 0.2937 mL | 0.7343 mL |
Nilofabicin Related Classifications
HY-111071 Related Classifications
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Keywords
- Nilofabicin
- 934628-27-0
- CG-400549
- CG400549
- CG 400549
- Antibiotic
- Bacterial
- complicated acute bacterial skin and skin structure infections
- enoyl-acyl carrier protein reductase
- bacterial fatty acid biosynthesis
- methicillin-resistant Staphylococcus aureus infection
- methicillin-sensitive Staphylococcus aureus
- FabI
- NADPH
- methicillin-resistant Staphylococcus aureus
- enoyl-ACP reductase
- Staphylococcus aureus
- Inhibitor
- inhibitor
- inhibit