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| Other Sizes |
| Targets |
Duramycin targets phosphatidylethanolamine (PE), a phospholipid component of cell membranes. It functions as an ion channel modulator, influencing ion transport across epithelial membranes. The compound's mechanism of action in cystic fibrosis involves modulation of chloride ion transport, which may help restore proper mucociliary clearance. As a lantibiotic peptide, it also exhibits antibacterial activity through disruption of bacterial cell membranes.
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| ln Vitro |
Duramycin demonstrates potent in vitro activity as an antimicrobial peptide against a variety of bacteria. It exhibits antibacterial and antiviral properties. The compound's ion channel modulating activity has been characterized in vitro using epithelial cell models, where it influences ion transport across cell membranes. Its ability to bind to phosphatidylethanolamine has been demonstrated in biochemical assays.
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| ln Vivo |
Evaluation of [68Ga]NODAGA-Duramycin as a positron emission tomography (PET) tracer of cell death for whole-body detection of chemotherapy-induced organ damage. Two hours after an intravenous injection of [68Ga]NODAGA-Duramycin, the organ uptake of untreated and treated mice with doxorubicin, busulfan, and cisplatin is examined. Chemotherapy-induced organ damage in mice can be successfully detected non-invasively and with great sensitivity using [68Ga]NODAGA-Duramycin PET/CT[3].
Duramycin has been investigated in vivo for the treatment of cystic fibrosis (CF). It has been evaluated in clinical trials, reaching Phase 3 for cystic fibrosis. The compound has also been studied for dry eye syndromes in Phase 2 clinical trials. [68Ga]NODAGA-Duramycin has been evaluated as a PET tracer for whole-body detection of chemotherapy-induced organ toxicity. |
| Enzyme Assay |
In vitro receptor binding assays for duramycin involve measuring its binding to phosphatidylethanolamine (PE) using techniques such as surface plasmon resonance or fluorescence-based binding assays. The compound's ion channel modulating activity can be assessed using patch-clamp electrophysiology or ion flux assays in epithelial cell models. These assays help characterize the compound's mechanism of action at the molecular level.
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| Cell Assay |
In vitro cellular assays for duramycin involve treating epithelial cell lines with the compound and measuring ion transport using Ussing chamber or fluorescence-based assays. The compound's antimicrobial activity is assessed using standard bacterial growth inhibition assays. Cytotoxicity is evaluated using cell viability assays such as MTT or LDH release. These assays demonstrate the compound's dual activity as an ion channel modulator and antimicrobial peptide.
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| Animal Protocol |
In vivo animal experiments for duramycin involve administering the compound to animal models of cystic fibrosis or other diseases. Efficacy is evaluated by measuring improvements in ion transport, mucociliary clearance, and lung function. [68Ga]NODAGA-Duramycin has been evaluated as a PET tracer for detecting cell death in animal models of chemotherapy-induced organ toxicity. These studies support the compound's clinical development.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for duramycin are derived from preclinical and clinical studies. As a peptide, the compound may have limited oral bioavailability and is typically administered via inhalation or parenteral routes. Its pharmacokinetic properties have been characterized in the context of clinical trials for cystic fibrosis. The compound's distribution, metabolism, and elimination profiles are important considerations for its therapeutic use.
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| Toxicity/Toxicokinetics |
Duramycin has been evaluated for safety in clinical trials for cystic fibrosis and dry eye syndromes. The compound is generally well-tolerated, but adverse effects may include local irritation at the site of administration. Comprehensive toxicological studies have been conducted as part of its clinical development program. The compound is intended for research and clinical use under appropriate regulatory oversight.
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| References | |
| Additional Infomation |
Duramycin (Moli1901; Lancovutide) (CAS#: 1391-36-2) is a lantibiotic peptide derived from Streptomyces cinnamoneus. It is an ion channel modulator investigated for cystic fibrosis. The compound has reached Phase 3 clinical trials for CF and Phase 2 for dry eye syndromes. Its sequence is Cys-Lys-Gln-Cys-Cys-Ala-Phe-Gly-Pro-Phe-{Abu}-Phe-Val-Cys-Asp-Gly-Asn-{Abu}-Lys-NH2.
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| Molecular Formula |
C89H125N23O25S3
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| Molecular Weight |
2013.28
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| Exact Mass |
1997.82
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| CAS # |
1391-36-2
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| Appearance |
White to off-white solid powder
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| Density |
1.0238 (rough estimate)
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| Melting Point |
271-273ºC
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| Index of Refraction |
1.6680 (estimate)
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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 : ~0.5 mg/mL (~0.25 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 | 0.4967 mL | 2.4835 mL | 4.9670 mL | |
| 5 mM | 0.0993 mL | 0.4967 mL | 0.9934 mL | |
| 10 mM | 0.0497 mL | 0.2484 mL | 0.4967 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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