| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Clarithromycin-13C,d3 retains the antibacterial activity of unlabeled Clarithromycin. It targets the 50S ribosomal subunit of susceptible bacteria, inhibiting protein synthesis. As a labeled compound, it is used to trace metabolic pathways and quantify drug concentrations rather than for direct therapeutic use.
|
|---|---|
| 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[1].
As a stable isotope-labeled analog, Clarithromycin-13C,d3 has the same in vitro antibacterial activity as unlabeled Clarithromycin. Its primary use is as a tracer for quantitation during drug development, rather than for direct antibacterial effect studies. |
| ln Vivo |
Clarithromycin-13C,d3 is used primarily for analytical and pharmacokinetic studies. The deuterium and carbon-13 labels allow for precise quantification of the drug in complex biological matrices, helping to study drug metabolism and disposition. No direct therapeutic effects are studied in vivo.
|
| Enzyme Assay |
For in vitro isotope assays, Clarithromycin-13C,d3 is added to biological samples (e.g., plasma, tissue homogenates) at known concentrations. Samples are processed and analyzed by LC-MS/MS. The mass shift due to the stable isotopes allows for the compound to be distinguished from endogenous compounds and unlabeled drug.
|
| Cell Assay |
For cellular uptake studies, cells are incubated with Clarithromycin-13C,d3 at varying concentrations and for different time points. Cells are then lysed, and the concentration of the labeled compound is measured by LC-MS/MS to determine cellular accumulation. For cytotoxicity, standard MTT assays can be performed.
|
| Animal Protocol |
For in vivo studies, Clarithromycin-13C,d3 is typically administered to animals (e.g., rats or mice) via oral gavage or intravenous injection. Blood samples are collected at various time points post-administration. The plasma is analyzed by LC-MS/MS to quantify the labeled drug and its metabolites, generating a pharmacokinetic profile.
|
| ADME/Pharmacokinetics |
Clarithromycin-13C,d3 has a molecular weight of 751.96 Da (for the 13C and d3 labeled version). The incorporation of stable isotopes can potentially alter the pharmacokinetic and metabolic profiles of a drug. The compound is used as an internal standard for bioanalysis.
|
| Toxicity/Toxicokinetics |
Clarithromycin-13C,d3 is a stable isotope-labeled compound intended for research and analytical purposes only. It is not for human use. As a labeled analog, its toxicity profile is similar to that of unlabeled Clarithromycin, which has known safety data. However, this specific compound is not for therapeutic use.
|
| References |
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
|
| Additional Infomation |
Clarithromycin-13C,d3 is a research-grade reference standard supplied as a lyophilized powder or solid. Its isotopic enrichment is typically ≥99% for 13C and ≥98% for 2H (deuterium). It is used in analytical method development, validation (AMV), quality control (QC), and ANDA-related analytical work. Store at -20degC, protected from light and moisture.
|
| Molecular Formula |
C3713CH66D3NO13
|
|---|---|
| Molecular Weight |
751.96
|
| Related CAS # |
Clarithromycin;81103-11-9
|
| Appearance |
Typically exists as solid at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 1.3299 mL | 6.6493 mL | 13.2986 mL | |
| 5 mM | 0.2660 mL | 1.3299 mL | 2.6597 mL | |
| 10 mM | 0.1330 mL | 0.6649 mL | 1.3299 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.