| Size | Price | |
|---|---|---|
| 5mg | ||
| Other Sizes |
| Targets |
Dihydropteroate synthase (DHPS). As an internal standard, Sulfamethizole-d4 has no inherent pharmacological activity. It is used as an analytical reference standard, not as a therapeutic agent.
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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].
Not applicable. Sulfamethizole-d4 is used exclusively as an internal standard in analytical chemistry. It has no biological activity of its own and does not undergo pharmacological evaluation. |
| ln Vivo |
Not applicable. Sulfamethizole-d4 is not used for in vivo efficacy studies. It may be added to biological samples (e.g., plasma, urine, tissue homogenates) from animals dosed with sulfamethizole to enable accurate quantification of the parent drug by LC-MS/MS.
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| Enzyme Assay |
Not applicable. Sulfamethizole-d4 is used as a calibrator in mass spectrometry. It is not involved in receptor or enzyme binding assays.
|
| Cell Assay |
Cell-based assays are not applicable. Sulfamethizole-d4 is exclusively an analytical reference standard for LC-MS and GC-MS quantification.
|
| Animal Protocol |
Animals are dosed with the parent drug, sulfamethizole. Biological samples (e.g., plasma, urine) are collected at various time points. The samples are spiked with a known amount of Sulfamethizole-d4, processed (protein precipitation, extraction), and analyzed by LC-MS/MS. The concentration of sulfamethizole is calculated from the peak area ratio of sulfamethizole to the internal standard.
|
| ADME/Pharmacokinetics |
Not applicable. Sulfamethizole-d4 is an analytical standard. The non-deuterated parent drug, sulfamethizole, has an oral bioavailability of 85-100%, a half-life of approximately 6-8 h in humans, and is excreted primarily unchanged in the urine.
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| Toxicity/Toxicokinetics |
Not applicable. Sulfamethizole-d4 is intended for research use as an internal standard and is not for human consumption. The non-deuterated parent drug, sulfamethizole, is a broad-spectrum sulfonamide antibiotic (MIC90s = 1.25-5,000 ug/mL against clinical isolates of E. coli and K. pneumoniae). Sulfamethizole-d4 is not intended 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.
[2]. Watanabe, H. and J.W. Hastings, Inhibition of bioluminescence in Photobacterium phosphoreum by sulfamethizole and its stimulation by thymine. Biochim Biophys Acta, 1990. 1017(3): p. 229-34. [3]. Kerrn, M.B., N. Frimodt-Moller, and F. Espersen, Effects of sulfamethizole and amdinocillin against Escherichia coli strains (with various susceptibilities) in an ascending urinary tract infection mouse model. Antimicrob Agents Chemother, 2003. 47(3): p. |
| Additional Infomation |
Sulfamethizole-d4 is a stable isotope-labeled internal standard for pharmaceutical analysis. It is not an active drug and has no therapeutic or diagnostic applications. It is used to improve the accuracy and precision of bioanalytical methods. The compound should be stored at -20degC and is stable for long-term storage. For research use only.
|
| Molecular Formula |
C9H6D4N4O2S2
|
|---|---|
| Related CAS # |
Sulfamethizole;144-82-1
|
| 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)
|
| 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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