| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Bacteria; Yeast; Fungus[1]
Bactenecin primarily targets bacterial and fungal cell membranes, increasing membrane permeability. It interacts with lipopolysaccharide (LPS) on Gram‑negative bacteria and disrupts the integrity of the inner membrane, leading to leakage of cellular contents and cell death. No single protein receptor has been identified for this peptide. |
|---|---|
| ln Vitro |
Bactenecin is produced using solid-phase peptide synthesis and then renatured into a state with all disulfide bonds. Escherichia coli and Staphylococcus aureus growth is inhibited by betecenecin at a dose equivalent to that of the isolated peptide from bovine neutrophils. Trichophyton rubrum is killed by betainenecin, which also prevents the growth of other yeast and bacteria that are significant to medicine[1]. Human glioma cells, fetal rat astrocytes, and rat embryonic neurons are all severely cytotoxic to the dodecapeptide bentenecin[2]. Bactenecin disrupts live cells' inner membranes and binds to LPS more strongly than other compounds. Dyes seep through the membrane as a result of Bactenecin's interaction with model membranes, which alters the membrane's permeability and fluidity[3].
Bactenecin inhibits the growth of medically important bacteria (including E. coli, S. aureus and B. pseudomallei) and yeast, and kills the fungus Trichophyton rubrum. It exhibits stronger binding to LPS and induces perturbation of the inner membrane of live cells. The peptide also inhibits biofilm formation of B. pseudomallei. |
| ln Vivo |
In vivo efficacy has not been extensively reported, but Bactenecin is active against B. pseudomallei in murine models of infection. The peptide is strongly cytotoxic to rat embryonic neurons, fetal rat astrocytes and human glioblastoma cells at concentrations that are antimicrobial, suggesting potential for central nervous system toxicity if used systemically.
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| Enzyme Assay |
A standard antimicrobial susceptibility assay (broth microdilution protocol): Prepare bacterial or yeast suspensions (5×10⁵ CFU/mL) in appropriate growth medium (MHB for bacteria, SDB for yeast). Add Bactenecin TFA at doubling dilutions (0.125‑64 uM) to 96‑well plates. Incubate at 37degC for 24 h. The MIC is defined as the lowest concentration that inhibits visible growth (OD600 < 0.05 compared to growth control).
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| Cell Assay |
A standard cellular cytotoxicity assay: Rat embryonic neurons or human glioblastoma cells are seeded in 96‑well plates (1×10⁴ cells/well) and allowed to adhere overnight. Bactenecin TFA (0.1‑50 uM) is added and incubated for 24‑48 h. Cell viability is assessed by MTT or resazurin reduction assay. Percent viability is calculated relative to untreated controls; IC50 values are derived from dose‑response curves.
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| Animal Protocol |
A general animal model for systemic infection: BALB/c mice (n=6/group) are infected intraperitoneally with B. pseudomallei (5×10⁴ CFU). Bactenecin TFA (0.5‑10 mg/kg) is administered intravenously or intraperitoneally at 1 h post‑infection. Survival is monitored for 14 days, and bacterial loads in blood, liver and spleen are quantified by CFU plating on selective agar at day 3 or at humane endpoints.
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| ADME/Pharmacokinetics |
As a peptide, Bactenecin TFA is rapidly degraded by proteases in vivo, leading to a short plasma half‑life (typically minutes). It is poorly absorbed orally and is usually administered parenterally. The TFA counterion improves aqueous solubility but does not enhance metabolic stability. Cyanylation of disulfide bonds may reduce toxicity while preserving antimicrobial activity.
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| Toxicity/Toxicokinetics |
Bactenecin exhibits strong binding to LPS and induces perturbation of the inner membrane of live cells. Interaction of Bactenecin with model membranes results in changes in membrane fluidity and permeability, leading to leakage of dye across the membrane. At antimicrobial concentrations (2‑16 uM), Bactenecin is strongly cytotoxic to rat embryonic neurons, fetal rat astrocytes and human glioblastoma cells, suggesting a narrow therapeutic window for systemic use.
|
| References | |
| Additional Infomation |
Bactenecin is synthesised by solid‑phase peptide synthesis and renatured to a fully disulfide‑bonded form (disulfide bridge: Cys3‑Cys11). The cyclic structure contributes to its antimicrobial activity. Bactenecin is used in research focused on developing new antimicrobial peptides, studying host‑defence mechanisms and exploring treatments for Burkholderia pseudomallei infections. It has not been approved for clinical use.
|
| Molecular Formula |
C65H119F3N24O15S2
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|---|---|
| Molecular Weight |
1597.94
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| Related CAS # |
Bactenecin;116229-36-8
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| Appearance |
Typically exists as solid at room temperature
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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) |
H2O :~100 mg/mL (~62.58 mM)
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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 | 0.6258 mL | 3.1290 mL | 6.2581 mL | |
| 5 mM | 0.1252 mL | 0.6258 mL | 1.2516 mL | |
| 10 mM | 0.0626 mL | 0.3129 mL | 0.6258 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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