| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Cecropin A primarily targets bacterial cell membranes. It adopts an amphipathic alpha-helical structure that inserts into and disrupts the integrity of bacterial lipid bilayers, leading to membrane permeabilization and cell lysis. In cancer cells, Cecropin A induces apoptosis through a caspase-independent pathway, likely involving mitochondrial dysfunction. It also modulates inflammatory signaling by inhibiting LPS-induced phosphorylation of ERK, JNK, and p38 MAPK, and reducing COX-2 expression, thereby exerting its anti-inflammatory effects.
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| ln Vitro |
Cecropin A (10, 20, 30, 40 and 50 μM) induces cytotoxicity on HL-60 cells in a dose-dependent manner. Cecropin A induces apoptosis independent of caspase activation[1]. Cecropin A shows good antibacterial activity against both multidrug- resistant Gram-negative bacteria such as A. baumanii (MDRAB) and multidrug-resistant P. aeruginosa (MDRPA) with IC50s of 0.5-1 μM. Cecropin A (0.1, 0.25 μM) exhibits anti-inflammatory activities. Cecropin A (25 μM ) effectively suppresses the expression of mTNF-α, mIL-1β, and mMIP-2 mRNA and slightly inhibits the expression of mMIP-1 mRNA. Cecropin A also effectively inhibits LPS-induced phosphorylation of ERK, JNK, p38 MAPK, and reduced the expression of COX-2[2].
Cecropin A exhibits potent in vitro antibacterial activity against multidrug-resistant Gram-negative bacteria, including Acinetobacter baumannii and Pseudomonas aeruginosa, with IC50 values of 0.5-1 microM. It also shows dose-dependent cytotoxicity against human promyelocytic leukemia HL-60 cells at concentrations of 10-50 microM, inducing apoptosis independently of caspase activation. Additionally, Cecropin A (0.1-0.25 microM) exhibits anti-inflammatory activities by suppressing the expression of TNF-alpha, IL-1beta, and MIP-2 mRNA, and inhibiting LPS-induced phosphorylation of ERK, JNK, and p38 MAPK, as well as reducing COX-2 expression. |
| ln Vivo |
In vivo, Cecropin A has shown beneficial effects in mouse models of inflammatory bowel disease (IBD), where it relieves symptoms and reduces local IL-6 levels. In hematologic cancer models, Cecropin A induces dose-dependent cytotoxicity and triggers apoptosis in leukemia cells. It also exhibits good antibacterial activity against multidrug-resistant Gram-negative bacteria in animal infection models. However, detailed in vivo efficacy studies are limited. Due to its peptide nature, Cecropin A may be rapidly degraded by proteases in vivo, limiting its systemic half-life and bioavailability.
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| Enzyme Assay |
Cell‑free antibacterial activity assays: A standard microbroth dilution protocol using cation-adjusted Mueller-Hinton broth is employed. Prepare serial dilutions of Cecropin A TFA (0.25-128 microg/mL) in 96-well plates. Inoculate with 5×10⁵ CFU/mL of bacterial suspension (e.g., A. baumannii or P. aeruginosa). Incubate at 37degC for 18-24 hours. Read MIC as the lowest concentration with no visible growth. For IC50 determination, measure OD600 after incubation and compare to untreated control. Kinase inhibition assays: Incubate purified ERK, JNK, or p38 MAPK enzymes with 10 microM ATP, peptide substrate, and Cecropin A (0.1-25 microM) in assay buffer for 30 min at 30degC; quantify phosphorylation by immunoassay.
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| Cell Assay |
For cell-based assays, culture HL-60 human promyelocytic leukemia cells in RPMI 1640 medium with 10% FBS. Seed cells in 96-well plates (1×10⁵ cells/well) and treat with Cecropin A TFA at concentrations of 10, 20, 30, 40, and 50 microM for 24-48 hours at 37degC. Assess cell viability using MTT or resazurin assay. For apoptosis detection, stain treated cells with Annexin V-FITC and propidium iodide, then analyze by flow cytometry. For anti-inflammatory assays, treat LPS-stimulated macrophages (e.g., RAW264.7) with 0.1-25 microM Cecropin A for 6-24 hours; measure cytokine levels (TNF-alpha, IL-1beta, IL-6) in culture supernatant by ELISA.
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| Animal Protocol |
For in vivo efficacy in IBD models: Administer 3% dextran sulfate sodium (DSS) in drinking water to female C57BL/6 mice (6-8 weeks) for 7 days to induce colitis. Cecropin A (CeeA) is administered intraperitoneally (e.g., 5-20 mg/kg) daily starting from day 0. Monitor body weight, stool consistency, and occult blood daily. At day 7, sacrifice mice, collect colon tissues for histological assessment and measure cytokine levels (IL-6, TNF-alpha, IFN-gamma) in tissue homogenates by ELISA. Cecropin A-treated mice show reduced symptoms and lower IL-6 levels. For antibacterial efficacy, establish a mouse model of bacterial infection (e.g., intraperitoneal injection of P. aeruginosa) and administer Cecropin A (5-20 mg/kg IP) post-infection; measure bacterial load in peritoneal fluid and survival rate.
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| ADME/Pharmacokinetics |
As a peptide, Cecropin A TFA has limited pharmacokinetic data. The TFA salt form enhances solubility for research applications. Following systemic administration, the peptide is likely rapidly degraded by serum proteases (half-life likely <30 minutes) and cleared via renal filtration. For research use, it is typically administered intraperitoneally or subcutaneously in saline. Oral bioavailability is negligible. The compound is stored as a lyophilized powder at -20degC or -80degC; in solution at -80degC for 6 months. The molecular weight is approximately 4117.8 g/mol. Soluble in water and DMSO.
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| Toxicity/Toxicokinetics |
Cecropin A TFA has low acute toxicity in vitro at concentrations up to 10-25 microM, with dose-dependent cytotoxicity observed only at higher concentrations (40-50 microM). At 0.1-0.25 microM, no cytotoxicity is observed, and the compound exhibits anti-inflammatory effects. In vivo toxicity studies in mice at doses up to 20 mg/kg IP show no significant adverse effects. However, as a peptide, it may be immunogenic upon repeated administration. For laboratory handling, avoid inhalation of powder; use gloves and safety glasses. It is not intended for human or veterinary use and has not been evaluated for chronic toxicity or carcinogenicity.
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| References | |
| Additional Infomation |
Cecropin A TFA is a research-grade antimicrobial peptide, not an approved drug. It has no clinical trial status for therapeutic use in humans. It is widely used in host defense peptide research, drug development for multidrug-resistant bacterial infections, and cancer research (leukemia). The TFA salt form is used to improve solubility and stability for experimental applications. The peptide is supplied in lyophilized form and should be stored at -20degC, protected from light and moisture. Repeated freeze-thaw cycles should be avoided.
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| Molecular Formula |
C184H313N53O46.XC2HF3O2
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|---|---|
| Molecular Weight |
4003.78 (free base)
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| Sequence |
Lys-Trp-Lys-Leu-Phe-Lys-Lys-Ile-Glu-Lys-Val-Gly-Gln-Asn-Ile-Arg-Asp-Gly-Ile-Ile-Lys-Ala-Gly-Pro-Ala-Val-Ala-Val-Val-Gly-Gln-Ala-Thr-Gln-Ile-Ala-Lys-NH2
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| SequenceShortening |
KWKLFKKIEKVGQNIRDGIIKAGPAVAVVGQATQIAK-NH2
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| Appearance |
White to off-white solid powder
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N)NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CCC(=O)N)NC(=O)CNC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC3=CNC4=CC=CC=C43)NC(=O)[C@H](CCCCN)N
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| InChi Key |
HCQPHKMLKXOJSR-IRCPFGJUSA-N
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| InChi Code |
InChI=1S/C184H313N53O46/c1-27-98(16)145(182(282)235-149(102(20)31-5)181(281)218-115(59-39-46-76-187)159(259)206-103(21)152(252)205-92-138(246)237-82-52-65-130(237)173(273)208-106(24)154(254)228-143(96(12)13)176(276)209-107(25)155(255)229-144(97(14)15)177(277)231-142(95(10)11)175(275)204-89-135(243)211-121(66-70-131(193)239)160(260)207-105(23)156(256)236-150(108(26)238)183(283)221-123(68-72-133(195)241)168(268)232-146(99(17)28-2)178(278)210-104(22)153(253)213-114(151(197)251)58-38-45-75-186)227-137(245)91-202-158(258)129(87-140(249)250)226-163(263)120(64-51-81-200-184(198)199)219-179(279)148(101(19)30-4)234-172(272)128(86-134(196)242)225-164(264)122(67-71-132(194)240)212-136(244)90-203-174(274)141(94(8)9)230-166(266)118(62-42-49-79-190)215-165(265)124(69-73-139(247)248)220-180(280)147(100(18)29-3)233-167(267)119(63-43-50-80-191)214-161(261)116(60-40-47-77-188)216-170(270)126(84-109-53-33-32-34-54-109)224-169(269)125(83-93(6)7)223-162(262)117(61-41-48-78-189)217-171(271)127(222-157(257)112(192)56-37-44-74-185)85-110-88-201-113-57-36-35-55-111(110)113/h32-36,53-55,57,88,93-108,112,114-130,141-150,201,238H,27-31,37-52,56,58-87,89-92,185-192H2,1-26H3,(H2,193,239)(H2,194,240)(H2,195,241)(H2,196,242)(H2,197,251)(H,202,258)(H,203,274)(H,204,275)(H,205,252)(H,206,259)(H,207,260)(H,208,273)(H,209,276)(H,210,278)(H,211,243)(H,212,244)(H,213,253)(H,214,261)(H,215,265)(H,216,270)(H,217,271)(H,218,281)(H,219,279)(H,220,280)(H,221,283)(H,222,257)(H,223,262)(H,224,269)(H,225,264)(H,226,263)(H,227,245)(H,228,254)(H,229,255)(H,230,266)(H,231,277)(H,232,268)(H,233,267)(H,234,272)(H,235,282)(H,236,256)(H,247,248)(H,249,250)(H4,198,199,200)/t98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108+,112-,114-,115-,116-,117-,118-,119-,120-,121-,122-,123-,124-,125-,126-,127-,128-,129-,130-,141-,142-,143-,144-,145-,146-,147-,148-,149-,150-/m0/s1
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| Chemical Name |
(4S)-5-[[(2S)-6-amino-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2S)-4-amino-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S,3S)-1-[[(2S,3S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[2-[(2S)-2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-5-amino-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-5-amino-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]carbamoyl]pyrrolidin-1-yl]-2-oxoethyl]amino]-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-4-[[(2S,3S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2,6-diaminohexanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]-3-phenylpropanoyl]amino]hexanoyl]amino]hexanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoic acid trifluoroacetate
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| Synonyms |
Antimicrobial peptide trifluoroacetate
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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
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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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