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| 1mg |
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This compound is a stable isotope-labeled internal standard and is not a pharmacologically active agent. It is the deuterated form of Zidovudine O-beta-D-glucuronide sodium. The non-deuterated parent compound (Zidovudine O-beta-D-glucuronide) is the major metabolite of Zidovudine, a nucleoside reverse transcriptase inhibitor (NRTI) used to treat HIV infection. Zidovudine works by inhibiting HIV reverse transcriptase, thereby blocking viral DNA synthesis. The glucuronide metabolite is inactive and is formed via glucuronidation by UDP-glucuronosyltransferase (UGT) enzymes, primarily UGT2B7, for elimination. This deuterated internal standard is used for analytical purposes and has no pharmacological activity of its own.
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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].
Zidovudine O-beta-D-glucuronide-d3 sodium is not used for in vitro pharmacological activity studies. Its primary application is in analytical chemistry. The non-deuterated metabolite, Zidovudine O-beta-D-glucuronide, is the major urinary metabolite of Zidovudine in humans. Zidovudine, the parent drug, is a nucleoside analog that competitively inhibits HIV reverse transcriptase and is incorporated into viral DNA, causing chain termination. The deuterated compound is an internal standard for LC-MS methods to accurately quantify Zidovudine and its glucuronide metabolite. |
| ln Vivo |
Zidovudine O-beta-D-glucuronide-d3 sodium is not typically used for in vivo studies as a test article. It is used as an internal standard for pharmacokinetic (PK) studies of Zidovudine. In a typical study, the non-deuterated compound (Zidovudine) is administered to animals or humans, and blood, plasma, urine, or tissue samples are collected. The deuterated internal standard is spiked into the samples before processing to correct for extraction efficiency and matrix effects. The concentration of Zidovudine and its glucuronide metabolite is then quantified by LC-MS/MS by comparing the peak area ratio (analyte to internal standard) to a standard curve. The compound is not administered by itself in animal experiments.
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| Enzyme Assay |
The standard protocol for using Zidovudine O-beta-D-glucuronide-d3 sodium as an internal standard involves preparing stock solutions in methanol or acetonitrile at a concentration of 0.1-1 mg/mL. Working solutions are prepared by serial dilution. For bioanalytical LC-MS/MS assays, an aliquot of the internal standard working solution (e.g., 10-50 ng/mL final concentration) is added to each sample (plasma, urine, tissue homogenate) before protein precipitation or solid-phase extraction. The sample is then processed by adding organic solvent (e.g., acetonitrile or methanol) to precipitate proteins, followed by centrifugation. The supernatant is collected, evaporated under nitrogen, and reconstituted in mobile phase. The reconstituted sample is injected into an LC-MS/MS system equipped with a C18 reverse-phase column. The mass spectrometer is operated in positive or negative ion mode, monitoring the transition for the deuterated internal standard (mass shift of +3 Da relative to the non-deuterated compound). A standard curve is prepared by spiking known concentrations of non-deuterated Zidovudine O-beta-D-glucuronide (or Zidovudine) into blank matrix, along with a fixed concentration of the deuterated internal standard. The peak area ratio is plotted against concentration.
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| ADME/Pharmacokinetics |
This compound is an internal standard; therefore, its pharmacokinetics are not studied. The deuterated internal standard is used to accurately measure the concentration of Zidovudine and its glucuronide metabolite in biological samples. Zidovudine, the parent drug, has a plasma half-life of approximately 1 hour in humans and is eliminated primarily by renal excretion following glucuronidation. The glucuronide metabolite has a longer half-life (approximately 3 hours) and accumulates in patients with renal impairment. The molecular weight of Zidovudine O-beta-D-glucuronide-d3 sodium is 468.37, and the molecular formula is C16H17D3N5NaO10. The compound should be stored at -20degC in a sealed container, protected from moisture. In solvent, it should be stored at -80degC for 6 months or -20degC for 1 month.
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| Toxicity/Toxicokinetics |
Toxicological data for the deuterated internal standard are not relevant because it is used at trace concentrations in analytical assays (typically ng/mL to ug/mL levels) and has no pharmacological activity. The non-deuterated parent drug Zidovudine has known toxicities including bone marrow suppression (anemia, neutropenia), nausea, and headache. However, the deuterated internal standard is not used for therapeutic purposes. Standard safety precautions for handling chemical reagents should be followed.
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| References |
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| Additional Infomation |
Zidovudine O-beta-D-glucuronide-d3 sodium is a research-grade isotopically labeled compound and is not approved for clinical use. It is intended for use as an internal standard in LC-MS/MS assays for the quantification of Zidovudine and its metabolites in biological matrices. Zidovudine (AZT) is a nucleoside reverse transcriptase inhibitor (NRTI) used clinically for the treatment of HIV infection. The deuterated internal standard is valuable for drug metabolism and pharmacokinetic (DMPK) studies. The compound should be stored at -20degC in a sealed container, protected from moisture and light. The related CAS number for the unlabeled compound is 133525-01-6.
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| Molecular Formula |
C16H17D3N5NAO10
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| Molecular Weight |
468.37
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| Appearance |
White to light yellow 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 | 2.1351 mL | 10.6753 mL | 21.3506 mL | |
| 5 mM | 0.4270 mL | 2.1351 mL | 4.2701 mL | |
| 10 mM | 0.2135 mL | 1.0675 mL | 2.1351 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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