| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
LTX-109 targets the negatively charged membrane components of bacterial cell walls. It is a peptidomimetic antimicrobial agent. By binding to bacterial membranes, it causes membrane disruption and cell death. Its mechanism is distinct from traditional antibiotics, making it effective against antibiotic-resistant bacteria.
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| ln Vitro |
Voxvoganan (LTX-109), an experimental antibacterial drug, works through a membrane-lytic mechanism based on the biology of innate immune effector cleavage peptides. Voxvoganan exhibits fast bactericidal lytic activity. Voxvoganan possesses in vitro bactericidal efficacy against several S. aureus isolates that are resistant to the various antimicrobial drugs tested in this investigation [2]. Voxvoganan (LTX-109) is a broad-spectrum, fast-acting bactericidal antimicrobial drug that binds to the negatively charged membrane components of bacterial cell walls, causing membrane rupture and cell death. Voxvoganan is a first-in-class chemically produced tiny peptide medicine that is resistant to proteolysis. Voxvoganan, when given topically, has a limited bioavailability but a high safety profile. Voxvoganan is effective against mupirocin-susceptible and resistant Staphylococcus aureus strains [3].
In vitro, LTX-109 is highly effective against S. aureus with a minimum inhibitory concentration (MIC) range of 2 to 4 µg/mL. It demonstrates broad-spectrum antimicrobial activity against Gram-positive bacteria. It is a fast-acting bactericidal agent. It is also being studied for fungal infections. |
| ln Vivo |
In vivo, LTX-109 has been investigated for the treatment of atopic dermatitis, mild eczema/dermatoses, and Gram-positive skin infections. It is a topical antimicrobial agent. It has reached Phase II clinical trials for these indications. Its fast-acting bactericidal activity makes it suitable for topical application.
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| Enzyme Assay |
In vitro antimicrobial susceptibility testing for LTX-109 typically involves broth microdilution or agar dilution methods according to CLSI guidelines. Bacterial cultures are incubated with varying concentrations of the compound for 18-24 hours. The minimum inhibitory concentration (MIC) is determined as the lowest concentration that inhibits visible bacterial growth. Time-kill assays are used to evaluate bactericidal kinetics.
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| Cell Assay |
Cell-based assays for LTX-109 involve culturing bacterial strains (e.g., S. aureus, MRSA) in appropriate media. Bacteria are treated with LTX-109 at concentrations ranging from 0.5 to 16 µg/mL. Bacterial growth is measured by optical density at 600 nm. Membrane disruption is assessed by propidium iodide uptake or LIVE/DEAD staining. Biofilm formation may be evaluated in biofilm models.
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| Animal Protocol |
In vivo animal experiments for LTX-109 typically involve topical application in mouse models of skin infection. Mice are infected with S. aureus or other bacteria, and the compound is applied topically. Bacterial load is measured by colony-forming unit (CFU) counts from skin biopsies. Wound healing and inflammation are assessed by histopathology. Pharmacokinetic parameters are evaluated by measuring compound levels in skin and plasma.
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| ADME/Pharmacokinetics |
As a peptide (molecular weight 788.08), LTX-109 is administered topically. Topical administration results in localized exposure with minimal systemic absorption. Detailed pharmacokinetic parameters including skin penetration and systemic exposure are available in preclinical and clinical literature. The compound has a favorable topical safety profile.
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| Toxicity/Toxicokinetics |
LTX-109 is a topical antimicrobial agent with a favorable safety profile. It has been investigated in Phase II clinical trials for atopic dermatitis and skin infections. No significant systemic toxicity has been reported. Comprehensive toxicological evaluation including skin irritation, sensitization, and systemic toxicity studies has been conducted.
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| References |
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| Additional Infomation |
LTX-109 is a tripeptide, specifically L-arginyl-2,5,7-tri-tert-butyl-L-tryptophanyl-L-arginine 2-phenylacetamide. It possesses antibacterial and peptidominant activities. It is a tripeptide and a monocarboxylic acid amide. LTX-109 has been investigated for the treatment of atopic dermatitis, mild eczema/dermatitis, and Gram-positive bacterial skin infections.
LTX-109 (Lytixar) (CAS#: 1166254-80-3) is a broad-spectrum, fast-acting bactericidal antimicrobial peptide. It targets bacterial cell membranes. It is effective against S. aureus (MIC = 2-4 µg/mL). It has reached Phase II clinical trials for skin infections and atopic dermatitis. Molecular weight: 788.08. |
| Molecular Formula |
C43H69N11O3
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|---|---|
| Molecular Weight |
788.079869031906
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| Exact Mass |
787.558
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| CAS # |
1166254-80-3
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| Related CAS # |
1166254-80-3;Lytixar HCl;
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| PubChem CID |
25242323
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
9.388
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| Hydrogen Bond Donor Count |
9
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
21
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| Heavy Atom Count |
57
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| Complexity |
1350
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C(N)(=O)[C@H](CCCNC(N)=N)N(C(=O)[C@H](CC1C2=C(C(C(C)(C)C)=CC(C(C)(C)C)=C2)NC=1C(C)(C)C)NC(=O)[C@H](CCCNC(N)=N)N)CCC1=CC=CC=C1
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| InChi Key |
ZVOYWSKEBVVLGW-ZDCRTTOTSA-N
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| InChi Code |
InChI=1S/C43H69N11O3/c1-41(2,3)27-23-28-29(35(43(7,8)9)54-34(28)30(24-27)42(4,5)6)25-33(53-36(55)31(44)17-13-20-50-39(45)46)38(57)52-32(18-14-21-51-40(47)48)37(56)49-22-19-26-15-11-10-12-16-26/h10-12,15-16,23-24,31-33,54H,13-14,17-22,25,44H2,1-9H3,(H,49,56)(H,52,57)(H,53,55)(H4,45,46,50)(H4,47,48,51)/t31-,32-,33-/m0/s1
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| Chemical Name |
(S)-2-amino-5-guanidino-N-((S)-1-(((S)-5-guanidino-1-oxo-1-(phenethylamino)pentan-2-yl)amino)-1-oxo-3-(2,5,7-tri-tert-butyl-1H-indol-3-yl)propan-2-yl)pentanamide
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| Synonyms |
Lytixar LTX-109 LTX 109 LTX109
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.2689 mL | 6.3445 mL | 12.6891 mL | |
| 5 mM | 0.2538 mL | 1.2689 mL | 2.5378 mL | |
| 10 mM | 0.1269 mL | 0.6345 mL | 1.2689 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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