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| 5mg |
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| Targets |
Zifanocycline targets the bacterial 30S ribosomal subunit. By binding to this site, it inhibits the normal function of bacterial ribosomes, blocking protein synthesis and thereby exerting its antibacterial effect. It is a member of the tetracycline class of antibiotics (aminomethylcycline subclass) and is designed to overcome common tetracycline resistance mechanisms, including efflux pumps and ribosomal protection proteins. Its mechanism of action is bacteriostatic.
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| ln Vitro |
In vitro, Zifanocycline TFA exhibits broad-spectrum antimicrobial activity against Gram-positive and Gram-negative bacteria, including multidrug-resistant pathogens such as methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-resistant enterococci (VRE), and extended-spectrum beta-lactamase (ESBL)-producing bacteria. Minimum inhibitory concentration (MIC90) values are typically less than 1 microg/mL against several pathogens. Zifanocycline is active against many clinically relevant bacteria, including those resistant to other tetracyclines. It has promising activity for treating resistant infections.
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| ln Vivo |
In vivo, Zifanocycline TFA is an orally active antibiotic. It has been investigated for the treatment of acute bacterial skin and skin structure infections (ABSSSI), community-acquired bacterial pneumonia (CABP), and complicated intra-abdominal infections (cIAI) in preclinical and clinical studies. Its oral bioavailability and broad-spectrum activity make it a promising candidate for treating resistant bacterial infections. Detailed in vivo efficacy data should be obtained from primary literature.
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| Enzyme Assay |
For in vitro antimicrobial susceptibility testing, bacterial strains are cultured overnight in appropriate media (e.g., Mueller-Hinton broth). The minimum inhibitory concentration (MIC) of Zifanocycline TFA is determined using the broth microdilution method according to CLSI guidelines. Serial two-fold dilutions of Zifanocycline (0.016-32 microg/mL) are prepared in 96-well plates. Bacterial suspensions are adjusted to a concentration of 5 × 10^5 CFU/mL and added to each well. Plates are incubated at 35-37degC for 16-20 hours. The MIC is defined as the lowest concentration of the compound that inhibits visible bacterial growth.
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| Cell Assay |
For cytotoxicity assays, mammalian cells (e.g., HepG2 or Vero cells) are treated with Zifanocycline at concentrations of 0.1-100 microg/mL for 24-48 hours. Cell viability is assessed by MTT assay to calculate the CC50 and selectivity index.
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| Animal Protocol |
For in vivo efficacy studies, Zifanocycline TFA is formulated in an appropriate vehicle (e.g., 0.5% methylcellulose or PBS). Animal infection models are used, such as a mouse thigh infection model or a systemic infection model in neutropenic mice. Mice are infected intraperitoneally or intravenously with a bacterial suspension (e.g., S. aureus or E. coli). Zifanocycline is administered orally or subcutaneously at doses ranging from 1-50 mg/kg, typically 1 and 4 hours post-infection. Animals are euthanized 24 hours after infection, and target organs (thigh muscle, spleen) or blood are collected for bacterial CFU enumeration. The reduction in bacterial load compared to vehicle control is calculated.
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| ADME/Pharmacokinetics |
Zifanocycline TFA is orally active and has a favorable pharmacokinetic profile. Although detailed parameters are not provided in the source, tetracycline analogs typically have moderate oral bioavailability (30-70%) and a half-life of 6-12 hours in humans. Zifanocycline is designed to overcome resistance and may have improved PK properties. The molecular weight of the TFA salt is 666.64, and the free base molecular formula is C29H36N4O7 (MW 552.6). For specific PK parameters (Cmax, Tmax, t1/2, AUC), researchers should consult primary literature.
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| Toxicity/Toxicokinetics |
Toxicological data for Zifanocycline TFA are limited. As a tetracycline derivative, it may share class-related toxicities including gastrointestinal disturbances, photosensitivity, and tooth discoloration. In preclinical studies, it is generally well tolerated at therapeutic doses. Comprehensive toxicology studies have been conducted as part of clinical development. Researchers should consult published safety data for detailed information.
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| References |
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| Additional Infomation |
Zifanocycline is a research-grade antibiotic and has been advanced to clinical trials for infectious disease indications. It is not yet approved for clinical use. It is a semi-synthetic aminomethylcycline antibiotic that binds to the 30S ribosomal subunit and inhibits protein synthesis. Zifanocycline is a promising tool for studying antibiotic resistance and for developing new treatments for multidrug-resistant bacterial infections. The free base CAS number is 1420294-56-9, and the TFA salt is used for research purposes. Store at -20degC as a powder, protected from light and moisture.
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| Molecular Formula |
C31H37F3N4O9
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| Molecular Weight |
666.64
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| Related CAS # |
Zifanocycline;1420294-56-9
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| Appearance |
Yellow to brown solid powder
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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) |
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 | 1.5001 mL | 7.5003 mL | 15.0006 mL | |
| 5 mM | 0.3000 mL | 1.5001 mL | 3.0001 mL | |
| 10 mM | 0.1500 mL | 0.7500 mL | 1.5001 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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