Antimicrobial agent-8
Based on 1 Customer Validation
Antimicrobial agent-8 (Compound 15) is a potent antimicrobial agent, and shows potent antimicrobial activity with an MIC range of 2-8 μg/mL against Gram-negative and Gram-positive bacteria. Antimicrobial agent-8 shows anti-inflammatory activity against lipopolysaccharide-induced inflammation.
For research use only. We do not sell to patients.
- Purity : 95.12%
- CAS No.: 2978694-22-1
- Formula: C39H54N16
- Molecular Weight:746.95
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
Description
In Vitro
Antimicrobial agent-8 (2.8-56.4 μM; 24 h) inhibits Gram-negative bacteria and Gram-positive bacteria growth[1].
Antimicrobial agent-8 (5 and 20 μg/mL; 18 h) inhibits the production of nitric oxide (NO) and tumor necrosis factor-α (TNF-α) by lipopolysaccharide-stimulated in RAW 264.7 cells[1].
Antimicrobial agent-8 (1-32 μg/mL, 16 h; 8-128 μg/mL; 24 h) shows potent biofilm inhibitory (MBIC50=1 μg/mL) and eradicating activities (MBEC50=8 μg/mL) by MDRPA bacteria[1].
Antimicrobial agent-8 exhibits proteolytic resistance and salt/serum stability[1].
Antimicrobial agent-8 displays synergistic or additive effects when combined with selected clinically used antibiotics[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:E. coli [KCTC 1682], P. aeruginosa [KCTC 1637], S. epidermidis [KCTC 1917] and S. aureus [KCTC1621]
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Concentration:2.8-56.4 μM
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Incubation Time:24 hours
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Result:Inhibited Gram-negative bacteria with MIC values of 5.4 μM for E. coli [KCTC 1682] and P. aeruginosa [KCTC 1637].
Inhibited Gram- positive bacteria with MIC values of 2.7 μM and 5.4 μM for S. epidermidis [KCTC 1917] and S. aureus [KCTC1621], respectively.
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Cell Line:RAW 264.7 macrophages
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Concentration:5 and 20 μg/mL
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Incubation Time:18 hours
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Result:Observed LPS-stimulated production of NO with an inhibitory rate of 90.79% at 5 μg/mL.
Exhibited inhibitory effects on the LPS-stimulated production of TNF-α with an inhibitory rate of 95.4% at 20 μg/mL.
Chemical Information
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CAS No. 2978694-22-1
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Appearance Solid
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Molecular Weight 746.95
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Formula C39H54N16
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Color White to off-white
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SMILES
NCCN(C1=NC(NCC2=CC=CC=C2)=NC(N3CCN(C4=NC(NCC5=CC=CC=C5)=NC(N(CCN)CCN)=N4)C(CC6=CC=CC=C6)C3)=N1)CCN
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (133.88 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. 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. 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 (3.35 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (3.35 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
Protocols
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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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Cotton Pellet Granuloma
Cotton pellet granuloma is a classical in vivo chronic inflammation model used to evaluate the anti-inflammatory potential of test substances by measuring their ability to inhibit granuloma tissue formation around an implanted foreign body (cotton pellet) in rodents. The method is based on the biological response to a sterile implanted material, which induces proliferative phase inflammation characterized by fibroblast proliferation and collagen-rich granuloma formation, and the final readout reflects the extent of chronic inflammatory tissue growth surrounding the pellet. In multiple preclinical pharmacological evaluations, inhibition of cotton pellet-induced granuloma formation has been used as an indicator of anti-inflammatory activity in both synthetic and natural product screening contexts.
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Carrageenan-Induced Paw Edema
Carrageenan-induced paw edema is an acute inflammation model in which intraplantar injection of carrageenan induces localized inflammatory swelling characterized by vascular permeability, leukocyte infiltration, and production of inflammatory mediators such as prostaglandins and cytokines, making it widely used to evaluate anti-inflammatory agents in vivo. The resulting paw volume or thickness increase is quantified over time as a direct readout of inflammatory intensity and drug efficacy, typically reflecting cyclooxygenase-mediated prostaglandin-driven edema formation and immune cell recruitment in peripheral tissue[20].
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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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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Purity & Documentation
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Data Sheet (275 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.3388 mL | 6.6939 mL | 13.3878 mL | 33.4694 mL |
| 5 mM | 0.2678 mL | 1.3388 mL | 2.6776 mL | 6.6939 mL | |
| 10 mM | 0.1339 mL | 0.6694 mL | 1.3388 mL | 3.3469 mL | |
| 15 mM | 0.0893 mL | 0.4463 mL | 0.8925 mL | 2.2313 mL | |
| 20 mM | 0.0669 mL | 0.3347 mL | 0.6694 mL | 1.6735 mL | |
| 25 mM | 0.0536 mL | 0.2678 mL | 0.5355 mL | 1.3388 mL | |
| 30 mM | 0.0446 mL | 0.2231 mL | 0.4463 mL | 1.1156 mL | |
| 40 mM | 0.0335 mL | 0.1673 mL | 0.3347 mL | 0.8367 mL | |
| 50 mM | 0.0268 mL | 0.1339 mL | 0.2678 mL | 0.6694 mL | |
| 60 mM | 0.0223 mL | 0.1116 mL | 0.2231 mL | 0.5578 mL | |
| 80 mM | 0.0167 mL | 0.0837 mL | 0.1673 mL | 0.4184 mL | |
| 100 mM | 0.0134 mL | 0.0669 mL | 0.1339 mL | 0.3347 mL |