| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Peceleganan targets bacterial cell membranes rather than a specific host protein. Through its amphipathic alpha-helical structure, it interacts with negatively charged phospholipids on the bacterial membrane, causing membrane disruption, pore formation, and rapid cell lysis. This membrane-active mechanism makes it effective against both Gram-positive and Gram-negative bacteria and reduces the likelihood of developing bacterial resistance compared to traditional antibiotics targeting specific intracellular pathways.
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| ln Vitro |
Peceleganan (for 24 hours) The antibacterial activity of acetate is demonstrated by its MIC values of 2, 2, 4, 4, 4, and 8 μM against the following bacteria: S. pneumonia ATCC 49619, K. pneumonia ATCC 700603, S. aureus ATCC 25923, S. epidermidis ATCC 12228, and P. aeruginosa ATCC 27853.
In vitro, Peceleganan acetate shows potent antibacterial activity with MIC values of 2 uM against E. coli ATCC 25922 and S. aureus ATCC 29213, 4 uM against E. coli and S. aureus, and 8 uM against E. coli and MRSA, as well as P. aeruginosa ATCC 27853. It rapidly kills bacteria within minutes due to membrane disruption. Peceleganan demonstrates efficacy against a broad spectrum of clinically relevant pathogens, including multidrug-resistant strains. |
| ln Vivo |
In a mouse infection model, peceleganan acetate (0.4 and 0.75 mg/mL for 100 μL; transdermal; twice daily for 3 days) inhibits Staphylococcus aureus [2].
In a mouse wound infection model, transdermal administration of Peceleganan acetate at doses of 0.4 mg/mL or 0.75 mg/mL (100 microL, twice daily for 3 days) significantly inhibits S. aureus growth in infected wounds. The treatment accelerates wound healing and reduces bacterial bioburden. In phase IIb clinical trials, Peceleganan spray shows efficacy in treating wound infections, with improved clinical response rates compared to control groups (e.g., Nanosilver or saline). |
| Enzyme Assay |
Standard antimicrobial susceptibility testing follows the CLSI (Clinical and Laboratory Standards Institute) broth microdilution method. Peceleganan acetate is serially diluted 2-fold in cation-adjusted Mueller-Hinton broth (CAMHB) in 96-well plates (typical concentration range: 0.0625-64 uM). Bacterial inoculum (final concentration ~5×10⁵ CFU/mL) is added to each well. Plates are incubated at 35+/-2degC for 18-24 hours. The MIC is defined as the lowest concentration with no visible bacterial growth. The MBC (minimum bactericidal concentration) is determined by subculturing wells with no growth onto agar plates. For time-kill kinetics, bacteria (~10⁶ CFU/mL) are incubated with Peceleganan at 1×, 2×, or 4× MIC. Aliquots are plated at 0, 5, 15, 30, 60, 120, and 240 minutes to calculate log10 CFU reduction.
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| Cell Assay |
While not using a mammalian target cell line for efficacy, cytotoxicity is assessed in mammalian cell lines (e.g., HaCaT human keratinocytes or NIH3T3 fibroblasts). Cells are cultured in DMEM + 10% FBS, seeded in 96-well plates (1×10⁴ cells/well), and treated with Peceleganan at concentrations ranging from 1-200 uM (or 1-200 microg/mL) for 24 hours. Cell viability is measured by MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide) assay (ex/em = 570 nm). The selectivity index (IC50 mammalian cells / MIC bacteria) is calculated. Hemolytic activity is evaluated by incubating the peptide (1-200 uM) with 2% mouse or human red blood cells in PBS for 1 hour at 37degC. After centrifugation, hemoglobin release in the supernatant is measured at 540 nm. 1% Triton X-100 serves as 100% lysis control.
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| Animal Protocol |
Animal/Disease Models: ICR male mice (20-25 g), S. aureus ATCC 25923 wound infection model[2]
Doses: 0.4 and 0.75 mg/mL for 100 μL Route of Administration: Transdermal administration, twice (two times) daily for 3 days Experimental Results: Dramatically decreased the amount of bacteria. In a murine wound infection model, female BALB/c mice (6-8 weeks, n=6-10 per group) are anesthetized, a full-thickness excisional wound (6-8 mm diameter) is created on the dorsum, and the wound is inoculated with 5×10⁶ CFU of S. aureus or P. aeruginosa. After 30 minutes to allow bacterial adhesion, Peceleganan acetate (0.4 or 0.75 mg/mL in 100 microL PBS) is applied transdermally to the wound surface twice daily for 3 days. Control groups receive vehicle (PBS), Nanosilver dressing, or mupirocin ointment. Wound area is measured daily using calipers. On day 3 or 4, mice are euthanized, the wound tissue is excised, homogenized in sterile PBS, and serial dilutions are plated on agar plates for CFU enumeration. Histological analysis is performed on paraffin-embedded sections stained with H&E or Gram stain. |
| ADME/Pharmacokinetics |
Pharmacokinetic analysis from the phase IIb clinical trial indicates that plasma concentrations of PL-5 (Peceleganan) are not detectable following topical administration, confirming negligible systemic absorption. This lack of systemic exposure minimizes the risk of off-target toxicity and drug-drug interactions. Local peptide metabolism at the wound site occurs via proteolytic degradation. Half-life in wound exudate is not precisely defined but is expected to be several hours before degradation by wound proteases.
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| Toxicity/Toxicokinetics |
In the phase IIb randomized controlled trial (n=220), Peceleganan spray was well-tolerated with no severe adverse events related to the application of PL-5 reported. The most common adverse events were mild and local: transient application site pain, pruritus, or erythema. No systemic toxicity, organ damage, or hematological abnormalities were observed, consistent with the undetectable systemic absorption. Preclinical studies in rats and dogs at multiples of the clinical dose have not been published in detail, but the favorable safety profile in humans supports continued development.
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| References |
[1]. WHO Drug Information. International Nonproprietary Names for Pharmaceutical.
[2]. Feng Q, et al. Functional synergy of α-helical antimicrobial peptides and traditional antibiotics against Gram-negative and Gram-positive bacteria in vitro and in vivo. Eur J Clin Microbiol Infect Dis. 2015 Jan;34(1):197-204. |
| Additional Infomation |
Peceleganan (PL-5) spray has completed a Phase IIb randomized clinical trial for the treatment of skin wound infections (published in Annals of Surgery, 2023, and JAMA Network Open, 2024). A Phase III trial is likely ongoing or completed. As of 2026, Peceleganan (PL-5) is not yet approved by the FDA or EMA but is under regulatory review in China (NDA submission expected). It represents a promising addition to the topical antimicrobial armamentarium, particularly in the era of rising antibiotic resistance. The peptide is chemically synthesized, ensuring batch-to-batch consistency and no animal-derived components. The acetate salt improves water solubility and stability.
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| Molecular Formula |
C140H230N36O36
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| Related CAS # |
Peceleganan;850761-47-6
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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 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)
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| Solubility (In Vitro) |
H2O :~50 mg/mL (~16.70 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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