| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Maculatin 1.1 TFA targets bacterial cell membranes. The peptide adopts an amphipathic alpha-helical structure in membrane environments, enabling interaction with and insertion into lipid bilayers. This mechanism leads to membrane perforation, loss of membrane potential, cytoplasmic leakage, and ultimately bacterial death, without requiring a specific protein receptor.
|
|---|---|
| ln Vitro |
Maculatin 1.1 TFA demonstrates potent in vitro antimicrobial activity with a minimum inhibitory concentration (MIC) of 7 microM against Staphylococcus aureus. The peptide perforates the bacterial membrane of Staphylococcus aureus, causing bacterial death. Activity is primarily against Gram-positive bacteria, with weaker activity against Gram-negatives.
|
| ln Vivo |
Not available. In vivo efficacy of maculatin peptides has been studied in mouse models of bacterial infection. When administered systemically or locally, the peptides can reduce bacterial load and improve survival, though specific in vivo activity data (e.g., ED50, survival rates) for Maculatin 1.1 TFA are not provided in the available literature.
|
| Enzyme Assay |
Standard MIC assays involve culturing Staphylococcus aureus or other bacterial strains in Mueller-Hinton broth, adding Maculatin 1.1 TFA at two-fold serial dilutions (0.2-200 microM) in 96-well plates, incubating at 37degC for 18-24 hours, and measuring optical density at 600 nm to determine the lowest concentration that inhibits visible growth. MIC is typically 7 microM for S. aureus.
|
| Cell Assay |
For membrane disruption assays, typical protocols involve treating Staphylococcus aureus (10⁶ CFU/mL) with Maculatin 1.1 TFA (1-100 microM) for 30-60 minutes, followed by fluorescence staining with SYTOX Green (membrane-impermeable DNA stain) or propidium iodide, and analysis by flow cytometry or fluorescence microscopy to quantify membrane permeabilization.
|
| Animal Protocol |
Not available. For in vivo infection models, standard protocols involve intraperitoneal injection of Maculatin 1.1 TFA (1-20 mg/kg) in mice following or prior to Staphylococcus aureus inoculation, monitoring survival over 7-14 days, and collecting tissues (blood, spleen, kidneys) for bacterial colony counting to determine reduction in bacterial load.
|
| ADME/Pharmacokinetics |
The TFA salt form improves aqueous solubility and handling properties. As a cationic amphipathic peptide, maculatin is susceptible to proteolytic degradation in serum and tissues, with typically short half-lives (minutes to 1-2 hours) in circulation, which may limit systemic therapeutic applications.
|
| Toxicity/Toxicokinetics |
Toxicity of antimicrobial peptides can include hemolysis (due to membrane disruption of red blood cells) and off-target effects on host cells. Maculatin peptides generally exhibit selectivity for bacterial membranes over mammalian cells, but specific toxicity data (e.g., hemolytic concentration HC50, LD50) for Maculatin 1.1 TFA are not reported.
|
| References |
[1]. Sani MA, et al. Maculatin 1.1 disrupts Staphylococcus aureus lipid membranes via a pore mechanism. Antimicrob Agents Chemother. 2013 Aug;57(8):3593-600.
|
| Additional Infomation |
Maculatin 1.1 TFA is a research-grade antimicrobial peptide used to study bacterial membrane disruption, host defense peptide mechanisms, and the development of novel antibiotic agents. It has not entered clinical trials nor received regulatory approval for therapeutic use. The TFA counterion enhances solubility. This product is for laboratory research only.
|
| Molecular Formula |
C103H161N27O23.XC2HF3O2
|
|---|---|
| Appearance |
Typically exists as solid at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
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
|
|---|---|
| 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.) |
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.