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| 10mg |
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| Targets |
Maribavir-d6, like its non-deuterated parent compound, targets the pUL97 protein kinase of cytomegalovirus (CMV). Maribavir inhibits histone phosphorylation catalyzed by wild-type pUL97. By inhibiting UL97 kinase activity, Maribavir blocks CMV DNA replication and viral maturation. The deuterium labeling does not alter the compound's target specificity but allows for its use as a tracer or internal standard in analytical studies.
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| ln Vitro |
In vitro, Maribavir-d6 retains the same biological activity as Maribavir, with potent inhibition of wild-type pUL97-catalyzed histone phosphorylation (IC50 = 3 nM). The deuterium labeling does not affect the compound's binding affinity or inhibitory activity. Maribavir-d6 is used in in vitro assays to study CMV replication and antiviral activity. The compound's deuterium label allows for its detection and quantification by mass spectrometry.
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| ln Vivo |
In vivo, Maribavir (the non-deuterated form) is an orally active antiviral agent that inhibits CMV replication. Maribavir-d6 is used as an internal standard in pharmacokinetic studies to quantify Maribavir concentrations in biological samples. The deuterium label provides a mass shift that allows for differentiation from the non-deuterated compound in mass spectrometric analysis. The compound's in vivo antiviral activity is attributed to its inhibition of pUL97 kinase and CMV DNA replication.
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| Enzyme Assay |
In vitro enzyme assays for Maribavir-d6 involve measuring pUL97 kinase activity using histone substrates. The kinase is incubated with ATP and histone substrate in the presence of various concentrations of Maribavir-d6. Histone phosphorylation is measured by detecting phosphorylated histone using phospho-specific antibodies or radiolabeled ATP incorporation. IC50 values are calculated from dose-response curves. Selectivity is assessed by testing against other kinases.
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| Cell Assay |
In vitro cellular assays for Maribavir-d6 involve treating CMV-infected cells with the compound. Viral replication is assessed by measuring viral DNA levels by qPCR or by plaque assay. The compound's effects on CMV replication and viral protein expression are evaluated. Cytotoxicity is assessed using standard cell viability assays. The deuterium label does not affect the compound's cellular activity, and the same assays are used as for non-deuterated Maribavir.
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| Animal Protocol |
In vivo animal studies for Maribavir-d6 are typically pharmacokinetic studies to evaluate the absorption, distribution, metabolism, and excretion of Maribavir using the deuterated form as a tracer or internal standard. The compound is administered orally to animal models, and blood and tissue samples are collected at various time points. Maribavir-d6 concentrations are measured by LC-MS/MS, taking advantage of the mass shift provided by the deuterium label.
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| ADME/Pharmacokinetics |
Maribavir is an orally active drug with favorable pharmacokinetic properties. Maribavir-d6 is used as an internal standard in pharmacokinetic studies to accurately quantify Maribavir concentrations in biological samples. The deuterium label provides a mass shift of 6 Da, allowing for differentiation from the non-deuterated compound in mass spectrometric analysis. The pharmacokinetic profile of Maribavir includes good oral bioavailability and appropriate half-life for once or twice daily dosing.
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| Toxicity/Toxicokinetics |
Toxicological data for Maribavir have been established through preclinical and clinical studies. The compound is approved for clinical use as an antiviral agent. Maribavir-d6, being a deuterated analog, is expected to have a similar safety profile to Maribavir. Deuterium substitution typically does not alter the toxicological properties of a compound. However, comprehensive toxicological assessments for Maribavir-d6 specifically have not been reported, as it is used primarily as an analytical standard.
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| References | |
| Additional Infomation |
Maribavir-d6 is a deuterium-labeled form of Maribavir, an orally active antiviral agent that inhibits CMV DNA replication by inhibiting the protein kinase UL97. Maribavir is a potent inhibitor of wild-type pUL97-catalyzed histone phosphorylation with an IC50 of 3 nM. Maribavir-d6 is used as an internal standard or tracer in analytical and pharmacokinetic studies. Maribavir is approved for clinical use as an antiviral agent for the treatment of cytomegalovirus infection.
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| Molecular Formula |
C15H13D6CL2N3O4
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| Molecular Weight |
382.27
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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) |
DMSO :~100 mg/mL (~261.60 mM; with sonication (<60°C))
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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 | 2.6160 mL | 13.0798 mL | 26.1595 mL | |
| 5 mM | 0.5232 mL | 2.6160 mL | 5.2319 mL | |
| 10 mM | 0.2616 mL | 1.3080 mL | 2.6160 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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