| 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.
|
| 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).
|
| 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.
|
| 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.
|
| 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
|
|---|---|
| Molecular Weight |
1597.94
|
| Related CAS # |
Bactenecin;116229-36-8
|
| Sequence |
Arg-Leu-Cys-Arg-Ile-Val-Val-Ile-Arg-Val-Cys-Arg (Disulfide bridge: Cys3-Cys11)RLCRIVVIRVCR (Disulfide bridge: Cys3-Cys11)
|
| SequenceShortening |
RLCRIVVIRVCR (Disulfide bridge: Cys3-Cys11)
|
| Appearance |
White to off-white solid
|
| Source |
Originated from animals: bovine neutrophils
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O :~100 mg/mL (~62.58 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (62.58 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), Clear solution.
(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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