| Size | Price | |
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| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Antibiofilm agent-22 (compound 5j) effectively inhibits the formation of biofilms of Pseudomonas aeruginosa PAO1 without having direct bactericidal activity, with an IC50 value of 2.66 μM [1]. Antibiofilm agent-22 (1.25-20 μM; overnight) inhibits the formation of biofilms of Pseudomonas aeruginosa PAO1 in a concentration-dependent manner [1]. Antibiofilm agent-22 (1.25-20 μM) significantly and in a concentration-dependent manner reduces the production of elastase, pyocyanin and rhamnolipid in Pseudomonas aeruginosa PAO1, with the best inhibitory effect at 20 μM [1]. Antibiofilm agent-22 (1.25-20 μM; 24 h) inhibits the quorum sensing systems of las, pqs and rhl in Pseudomonas aeruginosa PAO1, but does not affect GFP protein expression or bacterial growth [1]. Antibiofilm agent-22 (1.25–20 μM) is a potent iron chelator (pFe(III) = 22.99) that enhances the production of pyocyanin and pyrrolizin in Pseudomonas aeruginosa PAO1 in a concentration-dependent manner by inducing iron starvation [1]. Antibiofilm agent-22 (24 h) disrupts iron homeostasis in Pseudomonas aeruginosa PAO1 through transcriptome dysregulation and impairs key processes of biofilm formation, including fimbriae assembly [1]. Antibiofilm agent-22 and its Fe3+ dimer have a strong and stable binding affinity to the FpvA receptor of Pseudomonas aeruginosa and can compete with natural pyocyanin, thereby interfering with iron acquisition [1]. Antibiofilm agent-22 (1.25-20 μM) inhibited the quorum movement of Pseudomonas aeruginosa PAO1 in a concentration-dependent manner (78% inhibition rate at 20 μM) and induced cytoplasmic vacuolization and cell membrane thinning, but had no direct bactericidal activity [1]. Antibiofilm agent-22 and tobramycin had a synergistic effect on Pseudomonas aeruginosa PAO1, and the MIC of tobramycin was reduced by 32-fold (FICI = 0.078) [1]. Antibiofilm agent-22 (3.125-50 μM) had no significant hemolytic activity against rabbit erythrocytes at concentrations up to 50 μM [1]. Antibiofilm agent-22 (6.25-100 μM; 24 hours) had no significant cytotoxicity against RAW 264.7, HSC or 293T cells after incubation for 24 hours at concentrations up to 100 μM [1].
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| ln Vivo |
Antibiofilm agent-22 (compound 5j) (25 μM; topical application; once daily for 3 or 9 days) plus tobramycin sulfate can almost completely clear wound bacteria in a mouse model of Pseudomonas aeruginosa infection [1].
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| Cell Assay |
Cytotoxicity assay [1] Cell Types: RAW 264.7 macrophages, human hepatic stellate cells (HSCs), human embryonic kidney 293T cells Test concentrations: 6.25 μM; 12.5 μM; 25 μM; 50 μM; 100 μM
Incubation Duration: 24 hours Experimental Results: No significant cytotoxicity was observed in any of the three cell types at concentrations up to 100 μM. |
| Animal Protocol |
Animal/Disease Models:ICR (male, 3-4 weeks old, Pseudomonas aeruginosa monoculture infection model) [1]
Doses: 25 μM; 25 μM plus tobramycin sulfate Route of Administration: Topical application; once daily for 3 or 9 days Experimental Results: No adverse effects were observed on mouse body weight, indicating good biosafety at the tested concentration. There was no statistically significant difference in wound bacterial load compared to the infected control group. Bacteria were almost completely cleared from the wound. |
| References |
| Molecular Formula |
C22H38N2O5
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|---|---|
| Molecular Weight |
410.55
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C1C=C(COCCCCCCC(NO)=O)N(CCCCCCCCC)C=C1O
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4358 mL | 12.1788 mL | 24.3576 mL | |
| 5 mM | 0.4872 mL | 2.4358 mL | 4.8715 mL | |
| 10 mM | 0.2436 mL | 1.2179 mL | 2.4358 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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