| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Target: Teixobactin binds to lipid II (a precursor of peptidoglycan) and lipid III (precursor of wall teichoic acid) via a highly conserved motif. This binding inhibits the enzymatic transglycosylation and transpeptidation steps of cell wall biosynthesis, leading to cell lysis. By targeting multiple essential precursors, teixobactin exhibits a low propensity for resistance development. Its unique binding mode differs from vancomycin and other glycopeptides, making it effective against resistant strains.
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| ln Vitro |
In Vitro Activity: Teixobactin shows potent antibacterial activity against a broad panel of Gram-positive pathogens, including MRSA, vancomycin-resistant Enterococci (VRE), and Mycobacterium tuberculosis, with MIC values in the range of 0.2-1 μg/mL. It exhibits rapid bactericidal activity and a very low frequency of spontaneous resistance (<10^-10). It does not inhibit Gram-negative bacteria due to outer membrane permeability. In vitro, it also shows synergy with other antibiotics. Detailed MIC data against clinical isolates are available in the primary literature.
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| ln Vivo |
In Vivo Activity: In murine models of systemic MRSA infection, teixobactin (administered intraperitoneally or intravenously) significantly reduces bacterial load and improves survival. In a mouse thigh infection model, it demonstrated dose-dependent efficacy with ED50 values around 1-5 mg/kg. It also showed activity against M. tuberculosis in mouse lung infection models. Pharmacodynamic studies indicate time-dependent killing. The compound has not yet entered human trials, but in vivo efficacy is well-established in preclinical infectious disease models.
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| Enzyme Assay |
In Vitro Enzyme/Receptor Binding Protocol: Binding affinity to lipid II and lipid III is typically measured by surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). For SPR, lipid II is immobilized on a sensor chip, and teixobactin is flowed over at various concentrations to determine KD. Alternatively, fluorescence polarization assays using fluorescently labeled lipid II analogues can be used. Membrane depolarization and peptidoglycan synthesis inhibition assays (using radiolabeled precursors) confirm the mechanism of action.
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| Cell Assay |
In Vitro Cell-Based Assay Protocol: Minimum inhibitory concentration (MIC) assays are performed by broth microdilution according to CLSI guidelines. Bacterial strains (e.g., S. aureus ATCC 29213, MRSA, VRE) are cultured in Mueller-Hinton broth and incubated with serial two-fold dilutions of teixobactin (0.03-64 μg/mL) for 18-24 h at 37°C. MIC is the lowest concentration with no visible growth. Time-kill curves are generated by sampling at 0, 2, 4, 6, 24 h for viable counts. Resistance frequency is determined by plating large inocula on agar containing 4×MIC.
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| Animal Protocol |
In Vivo Animal Assay Protocol: Murine septicemia model: CD-1 mice are infected intraperitoneally with lethal doses of S. aureus. Teixobactin is administered IV or IP at doses ranging from 0.5 to 20 mg/kg, 1 h post-infection. Survival is monitored for 7 days. In thigh infection model, neutropenic mice are infected intramuscularly, and compound is given subcutaneously; thighs are harvested for CFU counting after 24 h. Pharmacokinetic/pharmacodynamic (PK/PD) indices are calculated from plasma concentration-time data.
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| ADME/Pharmacokinetics |
Pharmacokinetics: Teixobactin is a cyclic peptide (MW 1242) with poor oral bioavailability; it is administered parenterally. In mice, IV administration shows a half-life of ~1-2 hours, moderate clearance, and volume of distribution consistent with extracellular fluid. Protein binding is moderate. It does not readily cross the blood-brain barrier. PK parameters (AUC, Cmax, t1/2) have been determined in rodents and dogs. Human PK is not yet available as it is in preclinical stage.
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| Toxicity/Toxicokinetics |
Toxicity: Preclinical toxicity studies in rodents and dogs have shown that teixobactin is well-tolerated at therapeutic doses. No significant nephrotoxicity or hepatotoxicity was observed, unlike polymyxins or vancomycin at high doses. In repeated-dose studies, no target organ toxicity was identified. Hemolysis and immunogenicity have not been major concerns. However, full toxicological profiling is ongoing. As a natural peptide, it may have low immunogenicity. No clinical toxicity data exist.
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| References | |
| Additional Infomation |
Teixobactin is a cyclic peptide isolated from Eleftheria terrae, a previously unculturable bacterial species, and is active against Gram-positive bacteria. It is an antibacterial agent. It is a peptide antibiotic, a cyclic peptide, and a macrocyclic compound. Reports on Teixobactin in Eleftheria terrae have been published, and relevant data are available for reference.
Additional Information: Teixobactin has CAS 1613225-53-8, molecular formula C58H95N15O15, MW 1242.47. It was discovered using iChip technology that allows growth of uncultured soil bacteria. It has a unique cyclodepsipeptide structure with 17 stereocenters. Its development is being pursued by several academic and industrial groups. It is not yet FDA-approved and is for research use. Resistance has not been observed in laboratory evolution studies, making it a promising candidate for treating multidrug-resistant Gram-positive infections. |
| Molecular Formula |
C58H95N15O15
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|---|---|
| Molecular Weight |
1242.46641373634
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| Exact Mass |
1241.71
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| CAS # |
1613225-53-8
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| PubChem CID |
86341926
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
1.522
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| Hydrogen Bond Donor Count |
16
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
32
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| Heavy Atom Count |
88
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| Complexity |
2450
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| Defined Atom Stereocenter Count |
17
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| SMILES |
O1C([C@H]([C@@H](C)CC)NC([C@H](C[C@H]2CN=C(N)N2)NC([C@H](C)NC([C@@H]([C@@H]1C)NC([C@H](CO)NC([C@H]([C@@H](C)CC)NC([C@@H]([C@@H](C)CC)NC([C@@H](CCC(N)=O)NC([C@H](CO)NC([C@H]([C@@H](C)CC)NC([C@@H](CC1C=CC=CC=1)NC)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O
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| InChi Key |
LMBFAGIMSUYTBN-MPZNNTNKSA-N
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| InChi Code |
InChI=1S/C58H95N15O15/c1-12-28(5)42(70-49(79)37(61-11)23-34-19-17-16-18-20-34)53(83)67-39(26-74)51(81)65-36(21-22-41(59)76)48(78)69-44(30(7)14-3)55(85)71-43(29(6)13-2)54(84)68-40(27-75)52(82)73-46-33(10)88-57(87)45(31(8)15-4)72-50(80)38(24-35-25-62-58(60)64-35)66-47(77)32(9)63-56(46)86/h16-20,28-33,35-40,42-46,61,74-75H,12-15,21-27H2,1-11H3,(H2,59,76)(H,63,86)(H,65,81)(H,66,77)(H,67,83)(H,68,84)(H,69,78)(H,70,79)(H,71,85)(H,72,80)(H,73,82)(H3,60,62,64)/t28-,29-,30-,31-,32-,33-,35-,36+,37+,38-,39-,40-,42-,43-,44+,45-,46+/m0/s1
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| Chemical Name |
(2R)-N-[(2R,3S)-1-[[(2S,3S)-1-[[(2S)-1-[[(3S,6S,9S,12R,13S)-6-[[(5S)-2-amino-4,5-dihydro-1H-imidazol-5-yl]methyl]-3-[(2S)-butan-2-yl]-9,13-dimethyl-2,5,8,11-tetraoxo-1-oxa-4,7,10-triazacyclotridec-12-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]-2-[[(2S)-3-hydroxy-2-[[(2S,3S)-3-methyl-2-[[(2R)-2-(methylamino)-3-phenylpropanoyl]amino]pentanoyl]amino]propanoyl]amino]pentanediamide
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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 | 0.8048 mL | 4.0242 mL | 8.0485 mL | |
| 5 mM | 0.1610 mL | 0.8048 mL | 1.6097 mL | |
| 10 mM | 0.0805 mL | 0.4024 mL | 0.8048 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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