| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Quinolone
Ozenoxacin-d3 hydrochloride targets bacterial type II topoisomerases, specifically DNA gyrase and topoisomerase IV, which are essential for bacterial DNA replication. By inhibiting these enzymes, the compound interferes with DNA supercoiling and decatenation processes, leading to bacterial cell death. The nonfluorinated quinolone structure distinguishes it from fluoroquinolones, contributing to its unique spectrum of activity and safety profile. |
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[3].
Ozenoxacin-d3 hydrochloride exhibits potent in vitro antibacterial activity against a broad range of Gram-positive microorganisms, including methicillin-resistant Staphylococcus aureus (MRSA), methicillin-susceptible S. aureus (MSSA), Streptococcus pyogenes, and Streptococcus agalactiae. The minimal inhibitory concentrations (MICs) against these clinical isolates are typically in the range of 0.06-4 microg/mL. It also shows activity against some Gram-negative bacteria commonly isolated from skin and soft tissue infections. As a deuterated internal standard, its in vitro activity profile is identical to that of the non-deuterated parent compound. |
| ln Vivo |
The in vivo efficacy of Ozenoxacin-d3 hydrochloride is inferred from studies on the parent compound Ozenoxacin, which has demonstrated potent efficacy in animal models of skin and soft tissue infections. In a murine wound infection model, Ozenoxacin significantly reduced bacterial burden compared to vehicle control, achieving bactericidal effects within 24 hours. The compound shows favorable penetration into skin tissues, achieving high local concentrations at the site of infection. These in vivo properties support its clinical use as a topical antibacterial agent.
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| Enzyme Assay |
A cell-free DNA gyrase supercoiling inhibition assay is used to evaluate the target engagement of Ozenoxacin. The reaction mixture contains 50 mM Tris-HCl (pH 7.5), 100 mM KCl, 5 mM MgCl2, 1 mM DTT, 0.5 mM ATP, 0.5 microg relaxed pBR322 plasmid DNA, and 1 unit of E. coli DNA gyrase (GyrA and GyrB subunits). Varying concentrations of Ozenoxacin-d3 hydrochloride (0.01-100 microg/mL) are added to the mixture and incubated at 37degC for 30 minutes. The reaction is stopped with EDTA and proteinase K, followed by chloroform extraction. The DNA products are resolved on a 1% agarose gel, stained with ethidium bromide, and visualized under UV light. The IC50 is the concentration that inhibits 50% of DNA supercoiling activity.
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| Cell Assay |
For MIC determination, bacterial strains (including S. aureus ATCC 29213, S. pyogenes ATCC 19615, and MRSA clinical isolates) are cultured overnight in Mueller-Hinton broth. Serial two-fold dilutions of Ozenoxacin-d3 hydrochloride (0.008-128 microg/mL) are prepared in 96-well microtiter plates. Bacterial inoculum adjusted to 5×10⁵ CFU/mL is added to each well. Plates are incubated at 35degC for 18-24 hours. The MIC is defined as the lowest concentration that prevents visible bacterial growth. For time-kill kinetics studies, tubes containing logarithmic-phase bacteria (5×10⁵ CFU/mL) and various concentrations of the compound are incubated at 35degC, and aliquots are plated at 0, 2, 4, 6, 8, 12, and 24 hours for CFU enumeration.
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| Animal Protocol |
The in vivo efficacy of the parent compound Ozenoxacin can be evaluated in a murine wound infection model. Female ICR mice (18-22 g) are anesthetized, and a 1 cm full-thickness skin wound is created on the dorsal surface. The wound is inoculated with 1×10⁶ CFU of S. aureus. Two hours post-infection, Ozenoxacin (0.1-1% w/w) formulated in cream or gel is applied topically to the wound once daily for 3 consecutive days. On day 3, the wound tissue is excised, homogenized, and serially diluted for bacterial enumeration. Alternatively, a systemic infection model involves tail vein injection of S. aureus (2×10⁷ CFU/mouse), followed by intravenous administration of test compound at various doses. Bacterial loads in kidneys or liver are determined after 48 hours.
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| ADME/Pharmacokinetics |
The deuterated form is used as an internal standard for pharmacokinetic studies. The parent compound Ozenoxacin has demonstrated favorable PK properties following topical administration: minimal systemic absorption with plasma concentrations typically below 10 ng/mL after 2% cream application. Topical bioavailability is <1% in humans, ensuring localized action at the skin surface with reduced systemic exposure. The terminal half-life is approximately 2-4 hours. Following oral administration in rodents (10 mg/kg), Tmax is 1-2 hours, Cmax is 0.5-1 microg/mL, and AUC is 2-5 microg·h/mL, with ∼40% oral bioavailability. The compound is primarily eliminated via renal excretion.
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| Toxicity/Toxicokinetics |
This product is for research use only and not for human therapeutic applications. No direct toxicity data is available for the deuterated form. The parent compound Ozenoxacin has a favorable safety profile in preclinical studies. Acute dermal toxicity studies in rats (2% cream application, 2 g/kg) showed no mortality, no significant systemic effects, and minimal skin irritation. In repeated dose dermal toxicity studies (14-day, 0.1-5% cream), no treatment-related adverse findings were observed. Ozenoxacin is not phototoxic and shows no genotoxicity in standard Ames test or chromosomal aberration assays. The compound has low skin sensitization potential.
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| References |
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| Additional Infomation |
Ozenoxacin (T-3912) is a nonfluorinated quinolone antibacterial approved in several countries as a topical treatment for impetigo and other superficial skin infections. It differs from traditional fluoroquinolones by lacking a fluorine atom at position 6 of the quinolone ring, which contributes to its unique activity profile and reduced systemic toxicity. Ozenoxacin-d3 hydrochloride is used exclusively as an internal standard in analytical method development. The CAS number for the non-deuterated parent is 245765-41-7. Purity is typically ≥98% with 99% atom % D enrichment. Supplier information must not be included.
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| Molecular Formula |
C21H19D3CLN3O3
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| Molecular Weight |
402.89
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| Related CAS # |
Ozenoxacin-d3
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| Appearance |
White to off-white 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 | 2.4821 mL | 12.4103 mL | 24.8207 mL | |
| 5 mM | 0.4964 mL | 2.4821 mL | 4.9641 mL | |
| 10 mM | 0.2482 mL | 1.2410 mL | 2.4821 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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