| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Roxithromycin-d7 targets the 50S ribosomal subunit of susceptible bacteria. The unlabeled parent compound, Roxithromycin, binds to the bacterial 50S ribosomal subunit, inhibiting protein synthesis by blocking the translocation of peptides. This bactericidal mechanism is typical for macrolide antibiotics. The deuterated version is not used for antimicrobial activity studies but serves as an analytical tracer.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as quantitative tracers while the drugs were being developed. Because deuteration may have an impact on a drug's pharmacokinetics and metabolic profile, it has drawn attention [1].
Roxithromycin-d7 is not used for biological activity assessment; it is an internal standard. The unlabeled parent, Roxithromycin, is a potent macrolide antibiotic with activity against Gram-positive and some Gram-negative bacteria. It inhibits the growth of bacteria such as Streptococcus pneumoniae, Staphylococcus aureus, and Mycoplasma pneumoniae. It is commonly used as a reference standard in bioassays to measure antibacterial activity. |
| ln Vivo |
Roxithromycin-d7 is used as an internal standard for PK studies of Roxithromycin. The unlabeled parent compound, Roxithromycin, is an orally active macrolide antibiotic used to treat a variety of respiratory tract, skin, and soft tissue infections. It is known for having a longer plasma half-life than erythromycin, allowing for less frequent dosing. The antibiotic acts by binding to the 50S ribosomal subunit, as described for its mechanism.
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| Enzyme Assay |
Roxithromycin-d7 is an internal standard for LC-MS/MS. A fixed concentration (e.g., 10-50 ng/mL) of the d7 internal standard is added to biological samples (e.g., plasma, urine). Samples are extracted (e.g., by protein precipitation with acetonitrile or liquid-liquid extraction with ethyl acetate) to remove proteins. The extracted sample is injected onto an LC-MS/MS system. Detection is performed in positive ion mode (ESI+). The d7 internal standard has a mass shift of +7 Da from the parent Roxithromycin (molecular weight is approximately 837.06). The peak area ratio is used for quantification.
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| Cell Assay |
Roxithromycin-d7 is not used in cell-based assays. The unlabeled parent compound, Roxithromycin, is used in antibacterial susceptibility testing. According to CLSI guidelines, bacteria (e.g., S. aureus ATCC 29213, S. pneumoniae ATCC 49619) are cultured in Mueller-Hinton broth. Roxithromycin is serially diluted 2-fold in a 96-well plate (0.008-128 ug/mL). A bacterial suspension (5×10⁵ CFU/mL) is added to each well. The MIC (minimum inhibitory concentration) is determined after 18-24 h of incubation as the lowest concentration that inhibits visible bacterial growth.
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| Animal Protocol |
Roxithromycin-d7 is used as an internal standard for PK studies. A standard animal protocol: Male Sprague-Dawley rats (200-250 g) are administered a single oral (p.o., 10-20 mg/kg) or intravenous (i.v., 2-5 mg/kg) dose of Roxithromycin. Blood samples are collected at multiple time points (0-24 h). Plasma is separated, and a fixed concentration of Roxithromycin-d7 is added. Samples are extracted and analyzed by LC-MS/MS. PK parameters (Cmax, Tmax, AUC, t½, F%) are calculated using non-compartmental analysis.
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| ADME/Pharmacokinetics |
Roxithromycin-d7 has a molecular weight that is approximately 7 Da higher than Roxithromycin (which is about 837.06). The powder should be stored at -20degC for up to 3 years, protected from light and moisture. In solvent, it is stable for 6 months at -80degC or 1 month at -20degC. The compound is typically soluble in DMSO and acetonitrile. Detailed PK parameters are not provided for the labeled version.
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| Toxicity/Toxicokinetics |
Roxithromycin is generally well-tolerated, with the most common adverse effects being gastrointestinal disturbances (diarrhea, nausea, abdominal pain), taste disturbances, and skin rash. The deuterated version is used in trace amounts as an analytical standard and does not pose additional safety risks beyond standard chemical handling. Patients with known hypersensitivity to macrolide antibiotics should avoid exposure.
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| References | |
| Additional Infomation |
Roxithromycin-d7 (RU-28965-d7) is a research-grade stable isotope-labeled compound and is not approved for clinical use. It is used as an internal standard for the quantification of the macrolide antibiotic Roxithromycin. This product is for research use only and not for human diagnostic or therapeutic applications.
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| Molecular Formula |
C41H69D7N2O15
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|---|---|
| Molecular Weight |
844.09
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| Related CAS # |
Roxithromycin;80214-83-1
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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 |
| 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 | 1.1847 mL | 5.9235 mL | 11.8471 mL | |
| 5 mM | 0.2369 mL | 1.1847 mL | 2.3694 mL | |
| 10 mM | 0.1185 mL | 0.5924 mL | 1.1847 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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