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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Dermaseptin targets microbial cell membranes, disrupting their integrity and leading to cell death. The peptide's mechanism of action involves electrostatic interactions with negatively charged microbial membrane components, followed by membrane insertion and pore formation. This results in membrane disruption, leakage of intracellular contents, and microbial cell death. Dermaseptin exhibits broad-spectrum antimicrobial activity against bacteria, fungi, and protozoa. The peptide's nonhemolytic nature suggests some degree of selectivity for microbial membranes over mammalian cell membranes.
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| ln Vitro |
At micromolar concentrations, the water-soluble, heat-stable, non-hemolytic peptide dermaseptin exhibits strong antimicrobial activity against pathogenic fungi. Dermaseptin's 80% α-helical conformation is indicated by its circular dichroism spectra in hydrophobic media. Secondary structure predictions show that dermaseptin can be configured as an amphipathic α-helix that spans residues 1–27. This perturbation-regulated water structure of the membrane regulates flux. 1]. At micromolar concentrations, dermaseptin has a lytic effect on filamentous fungi, bacteria, yeast, and protozoa. Dermaseptin's superior antibacterial potency can be attributed to a molecular element: the NH2-terminal α-helical amphipathic fragment, which spans residues 1-18 of the molecule [1]. Dermaseptin (5-100 μg/ml; 48 hours) completely prevents the growth of the majority of tested microorganisms, including filamentous fungi, yeasts, bacteria, and parasites, at micromolar concentrations [2]. Dermaseptin treatment for one hour did not penetrate guinea pig lymphocytes up to the highest concentration assayed (200 μg/ml), and after 48 hours of incubation, it did not inhibit the proliferation of human KJ3 cells. ..Rabbit red blood cells were hemolyzed at 350 μg/ml, which resulted in a 50% hemolysis after an hour of treatment with a dose exceeding 200 μg/ml [2]. Aeromonas equi, Pseudomonas aeruginosa, Escherichia coli, Enterococcus faecalis, and L. are among the bacteria that Dermaseptin has antibacterial action against. Microsporum canis (IP1194) and mezicana (NF alpha strain) have MIC values of 50 μg/ml, 100 μg/ml, 25 μg/ml, 15 μg/ml, and 50 μg/ml, respectively [2].
In vitro, dermaseptin exhibits highly potent antimicrobial activity against pathogenic fungi at micromolar concentrations. It is also active against a broad range of bacteria and protozoa. The peptide is water-soluble, thermostable, and nonhemolytic. Its antimicrobial activity is rapid and concentration-dependent. Dermaseptin's mechanism of action involves membrane disruption, leading to cell lysis. The peptide has been shown to be effective against various clinically relevant pathogens. |
| ln Vivo |
In vivo activity of dermaseptin has not been extensively characterized in animal models. As a peptide derived from frog skin, it is part of the amphibian innate immune system. However, specific in vivo efficacy studies in mammalian models have not been reported. The peptide's potential as an antimicrobial therapeutic requires further evaluation in vivo. Currently, limited in vivo data are available.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays are not applicable to dermaseptin, as its antimicrobial mechanism involves direct membrane disruption rather than binding to specific enzymes or receptors. The peptide's activity is assessed by measuring its ability to kill or inhibit the growth of microbial cells. Membrane disruption can be evaluated by measuring leakage of fluorescent dyes or intracellular contents from microbial cells. No specific enzyme or receptor binding assays have been developed for dermaseptin.
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| Cell Assay |
In vitro cell-based assays for dermaseptin typically employ microbial cell cultures, including bacteria (Gram-positive and Gram-negative), fungi (yeast and filamentous fungi), and protozoa. The minimum inhibitory concentration (MIC) is determined by broth microdilution or agar dilution methods. Microbial cells are cultured in appropriate medium and treated with various concentrations of the peptide. After incubation, cell viability is assessed by measuring optical density, colony counting, or using metabolic indicators such as resazurin or MTT. Hemolytic activity is assessed using human erythrocytes.
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| Animal Protocol |
In vivo animal studies with dermaseptin have not been extensively reported. No specific animal models have been used to evaluate its pharmacokinetics, efficacy, or toxicology. The peptide is derived from frog skin and is part of the amphibian innate immune system. Future studies may involve administration of the peptide in rodent models of infection to evaluate its antimicrobial efficacy. Currently, no in vivo data are available.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of dermaseptin have not been characterized. As a peptide with a molecular weight of 3455.06, the compound is likely to have limited oral bioavailability and may be susceptible to proteolytic degradation. The peptide may be cleared rapidly from the circulation by proteases. However, specific PK parameters have not been determined. Further studies are needed to evaluate the compound's PK profile.
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| Toxicity/Toxicokinetics |
The toxicity profile of dermaseptin has been partially characterized. The peptide is nonhemolytic, indicating low toxicity to mammalian erythrocytes. However, specific toxicity data, including acute toxicity, genotoxicity, and chronic toxicity studies, are not available. The peptide's selectivity for microbial membranes over mammalian membranes suggests a favorable safety profile, but further studies are needed. The compound is intended for research use only.
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| References |
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| Additional Infomation |
Dermaseptin is a research-grade antimicrobial peptide isolated from frog skin glands. It exhibits potent antimicrobial activity against bacteria, fungi, and protozoa at micromolar concentrations. The peptide is water-soluble, thermostable, and nonhemolytic. It is not an approved therapeutic drug and has no clinical trial history. The compound is supplied as a lyophilized powder. Molecular formula: C₁₅₂H₂₅₇N₄₃O₄₄S₂; molecular weight: 3455.06. Synonyms include antimicrobial peptide and skin antimicrobial peptide.
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| Molecular Formula |
C152H257N43O44S2
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|---|---|
| Molecular Weight |
3455.09
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| Exact Mass |
3453.866
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| CAS # |
136212-91-4
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| Related CAS # |
Dermaseptin TFA;646451-06-1
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| PubChem CID |
16130489
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| Appearance |
White to off-white solid powder
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| LogP |
-12.2
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| Hydrogen Bond Donor Count |
49
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| Hydrogen Bond Acceptor Count |
52
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| Rotatable Bond Count |
118
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| Heavy Atom Count |
241
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| Complexity |
7840
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| Defined Atom Stereocenter Count |
35
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| SMILES |
CC[C@@H]([C@@H](C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(N[C@H](C(=O)O)CCC(=O)N)=O)[C@H](O)C)=O)=O)CCC(=O)N)=O)CO)=O)NC([C@H]([C@H](O)C)NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(CNC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC(CNC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@H]([C@H](O)C)NC(CNC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@H]([C@H](O)C)NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](N)C)=O)CC(C)C)=O)CC1C2=C(C=CC=C2)NC=1)=O)CCCCN)=O)=O)CCSC)=O)CC(C)C)=O)CCCCN)=O)CCCCN)=O)CC(C)C)=O)=O)=O)CCSC)=O)C)=O)CC(C)C)=O)CC1N=CNC=1)=O)C)=O)=O)CCCCN)=O)C)=O)C)=O)CC(C)C)=O)=O)C)=O)C)=O)C)=O)CC(=O)O)=O)=O)C
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| InChi Key |
YFHLIDBAPTWLGU-CTKMSOPVSA-N
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| InChi Code |
InChI=1S/C152H257N43O44S2/c1-27-77(12)118(147(233)190-110(70-196)146(232)178-98(44-46-111(158)201)131(217)163-68-115(205)192-120(87(22)198)149(235)181-101(152(238)239)45-47-112(159)202)193-151(237)122(89(24)200)195-145(231)109(63-117(207)208)185-129(215)84(19)169-126(212)81(16)168-125(211)80(15)167-113(203)66-164-132(218)102(56-72(2)3)183-128(214)83(18)170-127(213)82(17)172-134(220)94(40-30-34-50-153)174-114(204)67-162-124(210)79(14)171-140(226)108(62-91-65-160-71-166-91)189-143(229)105(59-75(8)9)184-130(216)85(20)173-135(221)99(48-54-240-25)179-148(234)119(86(21)197)191-116(206)69-165-133(219)103(57-73(4)5)186-137(223)96(42-32-36-52-155)175-136(222)95(41-31-35-51-154)176-141(227)106(60-76(10)11)187-138(224)100(49-55-241-26)180-150(236)121(88(23)199)194-139(225)97(43-33-37-53-156)177-144(230)107(61-90-64-161-93-39-29-28-38-92(90)93)188-142(228)104(58-74(6)7)182-123(209)78(13)157/h28-29,38-39,64-65,71-89,94-110,118-122,161,196-200H,27,30-37,40-63,66-70,153-157H2,1-26H3,(H2,158,201)(H2,159,202)(H,160,166)(H,162,210)(H,163,217)(H,164,218)(H,165,219)(H,167,203)(H,168,211)(H,169,212)(H,170,213)(H,171,226)(H,172,220)(H,173,221)(H,174,204)(H,175,222)(H,176,227)(H,177,230)(H,178,232)(H,179,234)(H,180,236)(H,181,235)(H,182,209)(H,183,214)(H,184,216)(H,185,215)(H,186,223)(H,187,224)(H,188,228)(H,189,229)(H,190,233)(H,191,206)(H,192,205)(H,193,237)(H,194,225)(H,195,231)(H,207,208)(H,238,239)/t77-,78-,79-,80-,81-,82-,83-,84-,85-,86+,87+,88+,89+,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,118-,119-,120-,121-,122-/m0/s1
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| Chemical Name |
(2S)-5-amino-2-[[(2S,3R)-2-[[2-[[(2S)-5-amino-2-[[(2S)-2-[[(2S,3S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-6-amino-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]hexanoyl]amino]-3-hydroxybutanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]amino]hexanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-4-methylsulfanylbutanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]propanoyl]amino]acetyl]amino]hexanoyl]amino]propanoyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]acetyl]amino]propanoyl]amino]propanoyl]amino]propanoyl]amino]-3-carboxypropanoyl]amino]-3-hydroxybutanoyl]amino]-3-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]-5-oxopentanoyl]amino]acetyl]amino]-3-hydroxybutanoyl]amino]-5-oxopentanoic acid
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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 : ~25 mg/mL (~7.24 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (14.47 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2894 mL | 1.4471 mL | 2.8943 mL | |
| 5 mM | 0.0579 mL | 0.2894 mL | 0.5789 mL | |
| 10 mM | 0.0289 mL | 0.1447 mL | 0.2894 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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