| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
TBI-223 targets the bacterial ribosome, specifically the 50S subunit, similar to other oxazolidinone antibiotics. It inhibits bacterial protein synthesis by binding to the 23S rRNA of the 50S ribosomal subunit, preventing the formation of the initiation complex for protein translation. This mechanism of action is effective against both Mycobacterium tuberculosis and Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA). The compound's activity against drug-resistant strains makes it a promising candidate for treating multidrug-resistant tuberculosis.
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| ln Vitro |
TBI-223 displays potent in vitro activity against Mycobacterium tuberculosis (Mtb). It is also effective against methicillin-resistant Staphylococcus aureus (MRSA) in vitro. As an oxazolidinone antibiotic, it demonstrates antibacterial activity through inhibition of bacterial protein synthesis. The compound's activity against drug-resistant strains of Mtb suggests it may overcome resistance mechanisms that limit the efficacy of existing antibiotics such as linezolid. Further detailed MIC values and spectrum of activity data are available in the primary literature.
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| ln Vivo |
TBI-223 has demonstrated in vivo efficacy in mouse models of infection. It is effective against methicillin-resistant Staphylococcus aureus (MRSA) infections in mouse models. As an orally bioavailable compound, TBI-223 can be administered by oral gavage in animal studies. The compound's oral bioavailability makes it suitable for convenient dosing regimens in preclinical studies. In vivo efficacy against Mycobacterium tuberculosis is being evaluated in relevant animal models to support its development as a tuberculosis therapeutic.
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| Enzyme Assay |
For antibacterial susceptibility testing, Mycobacterium tuberculosis or Staphylococcus aureus cultures are grown in appropriate media and treated with TBI-223 at various concentrations. Minimum inhibitory concentration (MIC) is determined by broth microdilution following CLSI guidelines. For protein synthesis inhibition assays, bacterial cell-free translation systems are incubated with the compound and radiolabeled amino acids, and incorporation into nascent proteins is measured by scintillation counting. Ribosome binding assays are conducted using purified 50S ribosomal subunits and radiolabeled TBI-223.
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| Cell Assay |
For in vitro antibacterial activity, bacterial cultures (Mycobacterium tuberculosis or Staphylococcus aureus) are grown in appropriate media at 37°C. Cells are seeded in 96-well plates and treated with TBI-223 at various concentrations (typically 0.1-100 μg/mL). Plates are incubated for 18-24 hours, and bacterial growth is assessed by measuring optical density at 600 nm or by colony counting on agar plates. MIC is determined as the lowest concentration that inhibits visible bacterial growth. For cytotoxicity assessment, mammalian cells are treated with the compound and viability is measured using MTT assays.
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| Animal Protocol |
For in vivo efficacy studies, mice are infected with Mycobacterium tuberculosis or methicillin-resistant Staphylococcus aureus. TBI-223 is administered orally by gavage at various doses (typically 10-100 mg/kg) once or twice daily for 7-28 days. Bacterial load in lungs, spleen, or other organs is determined by colony counting on selective agar plates at study termination. Body weight is monitored for toxicity assessment. For MRSA infection models, survival and bacterial clearance are evaluated. Pharmacokinetic studies are conducted to determine compound exposure in plasma and target tissues.
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| ADME/Pharmacokinetics |
TBI-223 is an orally bioavailable compound with favorable pharmacokinetic properties for an antibiotic. As a small molecule with molecular weight 365.36, it is expected to have good oral absorption and tissue penetration. The compound's oral bioavailability supports convenient dosing in both preclinical and potential clinical settings. Detailed pharmacokinetic parameters such as half-life, Cmax, AUC, and protein binding are being characterized in preclinical studies. The compound's favorable PK profile supports its development as a potential replacement for linezolid in tuberculosis combination therapy.
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| Toxicity/Toxicokinetics |
TBI-223 is an investigational antibiotic intended for research use only and has not been approved for clinical use. As a novel oxazolidinone antibiotic, it is being developed primarily for the treatment of tuberculosis, particularly drug-resistant strains. The compound has shown promising activity against various strains of Mycobacterium tuberculosis including drug-resistant strains. It is being investigated as a potential replacement for linezolid in combination therapies. Standard safety precautions should be followed when handling this compound.
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| References |
[1]. Chauhan A, et al. Comprehensive review on mechanism of action, resistance and evolution of antimycobacterial drugs. Life Sci. 2021;274:119301.
[2]. Motamen S, et al. Analysis of Approaches to Anti-tuberculosis Compounds. ACS Omega. 2020;5(44):28529-28540. Published 2020 Oct 27. |
| Additional Infomation |
TBI-223 is an orally bioavailable oxazolidinone antibiotic targeting Mycobacterium tuberculosis, including drug-resistant strains, with molecular formula C17H20FN3O5 and molecular weight 365.36. The compound inhibits bacterial protein synthesis by binding to the 50S ribosomal subunit. TBI-223 is effective against MRSA in mouse models and is being investigated as a potential replacement for linezolid in tuberculosis combination therapy. It is an investigational compound for research use only and has not been approved for clinical applications.
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| Molecular Formula |
C17H20FN3O5
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|---|---|
| Molecular Weight |
365.356207847595
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| Exact Mass |
365.138
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| CAS # |
2071265-08-0
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| PubChem CID |
126494519
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
565
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| Defined Atom Stereocenter Count |
1
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| SMILES |
COC(=O)NC[C@H]1CN(C(=O)O1)C2=CC(=C(C=C2)N3CC4(C3)COC4)F
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| InChi Key |
ZNBRXLSWXJKKLJ-LBPRGKRZSA-N
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| InChi Code |
InChI=1S/C17H20FN3O5/c1-24-15(22)19-5-12-6-21(16(23)26-12)11-2-3-14(13(18)4-11)20-7-17(8-20)9-25-10-17/h2-4,12H,5-10H2,1H3,(H,19,22)/t12-/m0/s1
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| Chemical Name |
methyl N-[[(5S)-3-[3-fluoro-4-(2-oxa-6-azaspiro[3.3]heptan-6-yl)phenyl]-2-oxo-1,3-oxazolidin-5-yl]methyl]carbamate
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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) |
DMSO : 50 mg/mL (136.85 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.84 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7370 mL | 13.6851 mL | 27.3703 mL | |
| 5 mM | 0.5474 mL | 2.7370 mL | 5.4741 mL | |
| 10 mM | 0.2737 mL | 1.3685 mL | 2.7370 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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