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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
LL-37 amide TFA primarily targets the formyl peptide receptor-like 1 (FPRL1), a G protein-coupled receptor involved in immune cell chemotaxis. As a selective agonist of FPRL1, it activates FPRL1-mediated immune cell chemotaxis in human monocytes, neutrophils, and T cells that naturally express FPRL1. Additionally, LL-37 amide TFA binds to and disrupts bacterial cell membrane integrity through its cationic and alpha-helical structure, which interacts with negatively charged bacterial membranes. This dual mechanism—receptor-mediated immunomodulation and direct membrane disruption—underlies its broad-spectrum antimicrobial and immunomodulatory activities. The compound also modulates inflammatory responses by inhibiting the release of pro-inflammatory factors such as TNF-α and promotes angiogenesis.
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| ln Vitro |
In vitro, LL-37 amide TFA demonstrates potent antimicrobial activity against a broad spectrum of microorganisms, including bacteria, fungi, and viruses. It effectively inhibits periodontal pathogens with an ED99 value of 8.5-8.7 µg/mL. The compound exhibits anticancer activity and can be used in cancer research. LL-37 amide TFA induces calcium mobilization in human monocytes, neutrophils, and T cells that express FPRL1. It also has anti-biofilm potential and can inhibit gastric cancer tumorigenesis. The peptide's activity is concentration-dependent, and its amidation modification enhances its stability in serum-containing environments compared to the non-amidated form. In addition to its antimicrobial effects, LL-37 amide TFA regulates inflammation and neutralizes lipopolysaccharides from Gram-negative bacteria.
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| ln Vivo |
In vivo, LL-37 amide TFA has been found to protect the cornea from infection and modulate wound healing. The compound's antimicrobial and immunomodulatory activities translate to efficacy in animal models of infection and tissue injury. It is mainly used in research on infection-related diseases such as periodontal disease and deep tissue injuries (pressure ulcers), as well as wound healing. The amidation modification improves its stability in vivo by reducing sensitivity to serum inhibition. LL-37 amide TFA also promotes angiogenesis in vivo, contributing to its wound-healing properties. Its role in the innate immune response makes it a valuable tool for studying host defense mechanisms and developing new therapeutic strategies for infectious and inflammatory diseases.
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| Enzyme Assay |
In vitro enzyme or receptor binding assay protocols for LL-37 amide TFA typically involve assessing its interaction with the formyl peptide receptor-like 1 (FPRL1). Radioligand binding assays can be performed using membranes from cells expressing FPRL1 to determine binding affinity. Functional assays measuring calcium mobilization in FPRL1-expressing cells (e.g., human monocytes, neutrophils, or FPRL1-transfected HEK293 cells) are used to assess receptor activation. Cells are loaded with a calcium-sensitive fluorescent dye, treated with varying concentrations of LL-37 amide TFA, and fluorescence changes are measured. For antimicrobial activity assessment, standard broth microdilution assays are used to determine minimum inhibitory concentrations (MICs) against various bacterial and fungal strains. Membrane disruption can be evaluated using membrane permeability assays with fluorescent dyes such as SYTOX Green or propidium iodide.
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| Cell Assay |
In vitro cell-based assay protocols for LL-37 amide TFA typically involve treating cultured cells to assess its antimicrobial, immunomodulatory, and anticancer activities. For antimicrobial assays, bacterial or fungal cultures are incubated with varying concentrations of the peptide, and cell viability is measured by colony counting or optical density. For immunomodulatory studies, human monocytes, neutrophils, or T cells are treated with LL-37 amide TFA, and cytokine release (e.g., TNF-α) is measured by ELISA. Calcium mobilization is assessed in FPRL1-expressing cells loaded with fluorescent calcium indicators. For anticancer studies, cancer cell lines are treated with the peptide, and cell proliferation, apoptosis, and migration are evaluated using standard assays such as MTT, Annexin V staining, and Transwell migration assays. Cytotoxicity is assessed to determine the compound's safety profile.
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| Animal Protocol |
In vivo animal experimental protocols for LL-37 amide TFA typically involve infection models to assess its antimicrobial efficacy and wound healing models to evaluate its tissue repair properties. For infection studies, mice are infected with bacterial pathogens (e.g., periodontal pathogens), and LL-37 amide TFA is administered locally or systemically. Endpoints include bacterial load quantification, survival rates, and histological analysis of infected tissues. For wound healing studies, full-thickness skin wounds are created in mice, and the peptide is applied topically. Wound closure rates, re-epithelialization, and angiogenesis are assessed. For corneal infection models, the peptide is applied to the infected cornea, and infection resolution and tissue integrity are evaluated. Appropriate controls include vehicle-treated and untreated groups.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of LL-37 amide TFA are characterized by its peptide nature and amidation modification. The compound has a molecular weight of 4492.28 (free base) and is typically soluble in DMSO (e.g., 10 mM). The C-terminal amidation modification reduces its sensitivity to serum inhibition and improves its stability compared to the non-amidated form. As a peptide, LL-37 amide TFA would be expected to have limited oral bioavailability due to susceptibility to proteolytic degradation in the gastrointestinal tract. Following parenteral administration, it would likely be cleared through proteolysis and renal excretion. Specific PK parameters such as half-life, Cmax, AUC, and bioavailability have not been extensively reported. The compound is typically stored as a white to off-white solid powder at -20°C for long-term stability.
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| Toxicity/Toxicokinetics |
Toxicological data for LL-37 amide TFA are limited, as the compound is intended for research use only and is not for human therapeutic or diagnostic applications. The parent peptide LL-37 is known to have hemolytic activity due to its high hydrophobicity and amphiphilicity. Short peptide fragments derived from LL-37 have been designed to reduce hemolytic toxicity while retaining antimicrobial properties. No acute toxicity (LD50), subchronic toxicity, genotoxicity, or reproductive toxicity studies have been reported specifically for LL-37 amide TFA. As with all research chemicals, appropriate safety precautions should be taken when handling the compound, including working in a fume hood, wearing appropriate personal protective equipment, and avoiding inhalation, ingestion, or skin contact. The compound is not intended for human use.
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| References | |
| Additional Infomation |
LL-37 amide TFA is a research-grade antimicrobial peptide that serves as a multifunctional host defense peptide with antibacterial, antiviral, and immunomodulating activities. It is the only cathelicidin-type peptide found in humans and is expressed in bone marrow, testis, granulocytes, and gingival epithelium. The compound is unique among antimicrobial peptides due to its broad-spectrum activity and multifunctional properties. Its mechanism of action involves activation of FPRL1-mediated immune cell chemotaxis and disruption of bacterial cell membrane integrity. LL-37 amide TFA has not entered clinical trials and is not approved for any therapeutic indication. It is mainly used in research on periodontal disease, deep tissue injuries, wound healing, and cancer. The compound is available exclusively for research purposes and is not intended for diagnostic, therapeutic, or human applications.
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| Molecular Formula |
C205H341N61O52.XC2HF3O2
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| Molecular Weight |
4492.28 (free base)
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| Appearance |
White to off-white solid powder
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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 (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)
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| Solubility (In Vitro) |
Typically soluble in DMSO (e.g. 10 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.) |
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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