| Size | Price | |
|---|---|---|
| 1mg | ||
| 5mg | ||
| 10mg | ||
| Other Sizes |
| Targets |
As an antimicrobial peptide, Cecropin A TFA targets bacterial cell membranes, leading to membrane disruption and cell lysis. It does not target a specific enzyme or receptor. It also exhibits activity against cancer cells by inducing caspase-independent apoptosis.
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|---|---|
| ln Vitro |
Cecropin A causes dose-dependent cytotoxicity in HL-60 cells at 10, 20, 30, 40, and 50 μM. Apoptosis is induced by cecropin A without the need for caspase activation[1]. Cecropin A exhibits strong antibacterial action with IC50s of 0.5–1 μM against multidrug-resistant P. aeruginosa (MDRPA) and multidrug-resistant A. baumanii (MDRAB). Anti-inflammatory properties are demonstrated by cecropin A (0.1, 0.25 μM). The expression of mTNF-α, mIL-1β, and mMIP-2 mRNA is significantly suppressed by cecropin A (25 μM), while the expression of mMIP-1 mRNA is modestly inhibited. Additionally, cecropin A successfully suppresses the production of COX-2 and phosphorylates ERK, JNK, and p38 MAPK when exposed to LPS[2].
In vitro, Cecropin A (10-50 microM) induces dose-dependent cytotoxicity in HL-60 human promyelocytic leukemia cells and induces apoptosis independent of caspase activation. It shows antibacterial activity against MDR bacteria with IC50s of 0.5-1 microM. It also exhibits anti-inflammatory activity by suppressing TNF-alpha, IL-1beta, and COX-2 expression. |
| ln Vivo |
In vivo, Cecropin A has demonstrated protective effects in animal models of bacterial infection and inflammation. It has been shown to reduce bacterial load and improve survival in infected mice. However, detailed in vivo pharmacokinetic and efficacy data for the TFA salt form are limited.
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| Enzyme Assay |
For in vitro antibacterial assays, Mueller-Hinton agar plates are prepared with bacterial strains. Cecropin A TFA is serially diluted (0.25-256 microg/mL) and added to wells. The minimum inhibitory concentration (MIC) is determined after 18-24 hours of incubation at 35+/-2degC as the lowest concentration with no visible bacterial growth.
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| Cell Assay |
For cell viability assays, HL-60 cells are seeded in 96-well plates (1×10⁵ cells/well) and treated with Cecropin A TFA (0-50 microM) for 24-48 hours. Cell viability is assessed using MTT or resazurin-based assays. For apoptosis analysis, cells are stained with Annexin V-FITC and analyzed by flow cytometry.
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| Animal Protocol |
For animal studies of infection, mice (e.g., BALB/c, 6-8 weeks) are infected intraperitoneally with a lethal dose of bacteria (e.g., E. coli or S. aureus). Cecropin A TFA is administered intraperitoneally or intravenously at doses of 1-10 mg/kg, either prophylactically or therapeutically. Survival is monitored for 7-14 days.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies indicate that Cecropin A has a short plasma half-life (typically <1 hour) due to rapid proteolytic degradation and renal clearance. For the TFA salt form, water solubility is enhanced. Achieving sufficient systemic exposure for in vivo efficacy remains a challenge due to rapid clearance and potential toxicity at high doses.
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| Toxicity/Toxicokinetics |
The TFA salt of Cecropin A is used to improve solubility and stability compared to the free base. While generally considered safe at low concentrations, high doses may cause hemolysis or cytotoxicity to mammalian cells. In animal models, doses up to 10 mg/kg are typically well-tolerated, but careful monitoring is advised.
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| References |
[1]. The antimicrobial peptide cecropin A induces caspase-independent cell death in human promyelocytic leukemia cells. Peptides. 2010 Aug;31(8):1494-503.
[2]. Anti-inflammatory activities of cecropin A and its mechanism of action. Arch Insect Biochem Physiol. 2015 Jan;88(1):31-44. |
| Additional Infomation |
Cecropin A was first isolated in 1980 and is one of the most studied antimicrobial peptides. The TFA salt form is commonly provided for research to improve solubility. Its mechanism of action involves disruption of microbial membranes by forming ion-permeable channels. It is used in studies of drug-resistant bacteria, cancer, and inflammation.
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| Molecular Formula |
C186H314N53O48F3
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|---|---|
| Molecular Weight |
4117.80
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| Related CAS # |
Cecropin A;80451-04-3
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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 |
Typically exists as solid at room temperature
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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
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| Synonyms |
Cecropin A TFA; 80451-04-3; dsim protein, Drosophila; dyak protein, Drosophila; cecropin A1 protein, Drosophila;
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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 |
| 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 (~12.14 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2428 mL | 1.2142 mL | 2.4285 mL | |
| 5 mM | 0.0486 mL | 0.2428 mL | 0.4857 mL | |
| 10 mM | 0.0243 mL | 0.1214 mL | 0.2428 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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