| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Rifampicin-d4 functions similarly to its non-deuterated parent by inhibiting bacterial RNA polymerase, which is essential for RNA synthesis in bacteria. The mechanism involves binding to the beta-subunit of DNA-dependent RNA polymerase, blocking the initiation of RNA synthesis. The deuterium labeling does not alter the mechanism of action.
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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[1].
Rifampicin-d4 is the deuterium labeled Rifampicin, used as a tracer for quantitation during drug development. The non-deuterated parent, Rifampicin, is a potent and broad-spectrum antibiotic against bacterial pathogens, including Mycobacterium tuberculosis and various Gram-positive and Gram-negative bacteria. It also exhibits anti-influenza virus activities. |
| ln Vivo |
In vivo, Rifampicin-d4 is used as an internal standard for PK studies. The non-deuterated parent, Rifampicin, is a widely used antibiotic for treating tuberculosis and other bacterial infections. It is also used in combination with protease inhibitors or reverse transcriptase inhibitors to enhance suppression of HIV replication in research models. The deuterated version is not administered therapeutically.
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| Enzyme Assay |
Rifampicin-d4 is not used in an enzyme binding assay; it is an internal standard for LC-MS/MS. A fixed concentration (e.g., 50-100 ng/mL) of the d4 internal standard is added to biological samples (e.g., plasma, urine). Samples are extracted by protein precipitation or liquid-liquid extraction. LC-MS/MS analysis is performed with a C18 column and a mobile phase of water/acetonitrile with 0.1% formic acid. Detection is in positive ion mode (ESI+). Rifampicin is monitored using MRM transitions (e.g., m/z 823 → 791). The d4 internal standard has a mass shift of +4 Da (m/z 827 → 795). The peak area ratio is used for quantification.
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| Cell Assay |
Rifampicin-d4 is not used in typical cell-based assays. The non-deuterated parent, Rifampicin, is used in antibacterial susceptibility testing. Bacteria (e.g., S. aureus or M. tuberculosis) are cultured in Mueller-Hinton broth or Middlebrook 7H9 medium. Rifampicin is serially diluted (0.008-128 microg/mL) and added to 5×10⁵ CFU/mL bacteria. The MIC is determined after 18-24 h (for S. aureus) or 7-14 days (for M. tuberculosis) as the lowest concentration with no visible growth.
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| Animal Protocol |
Rifampicin-d4 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 dose of Rifampicin (10-50 mg/kg). Blood samples are collected at various time points (0-24 h). Plasma is separated. A fixed concentration of Rifampicin-d4 is added to each sample. 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 |
Rifampicin-d4 has a molecular weight of 826.96 and the molecular formula C43H54D4N4O12. The powder should be stored at -20degC for up to 3 years or at 4degC for up to 2 years. In solvent, it is stable for 6 months at -80degC or 1 month at -20degC. The compound is soluble in DMF (≥20 mg/mL) and DMSO (≥3.3 mg/mL).
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| Toxicity/Toxicokinetics |
The non-deuterated parent, Rifampicin, is generally well-tolerated but can cause hepatotoxicity, gastrointestinal disturbances, and orange-red discoloration of body fluids. Rare but serious adverse effects include thrombocytopenia and hemolytic anemia. The deuterated version is used in trace amounts as an analytical standard and does not pose additional safety risks beyond standard chemical handling.
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| References |
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| Additional Infomation |
Rifampicin-d4 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 Rifampicin, a potent and broad-spectrum antibiotic. This product is for research use only and not for human therapeutic applications. Store as a powder at -20degC or 4degC.
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| Molecular Formula |
C43H54D4N4O12
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| Related CAS # |
Rifampicin;13292-46-1;Rifampicin-d8
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| Appearance |
Typically exists as solid at room temperature
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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.) |
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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