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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
BVDU 5'-Triphosphate ammonium targets the viral DNA polymerase, a crucial enzyme for herpesvirus DNA replication [8L4]. Its mechanism of action involves incorporation into the growing viral DNA chain, acting as a chain terminator [0L30-L31]. The exceptional selectivity for VZV and HSV-1 is due to the preferential phosphorylation of the parent nucleoside by the viral thymidine kinase, leading to high intracellular concentrations of the active triphosphate specifically in infected cells [8L14-L15]. This targeted mechanism minimizes host cell toxicity.
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| ln Vitro |
In vitro studies demonstrate that BVDU 5'-Triphosphate ammonium effectively inhibits viral DNA polymerase activity [0L28-L29]. It shows high potency against VZV and HSV-1 with excellent selectivity, meaning it effectively blocks the replication of these viruses in cell culture models while having minimal impact on host cell function [8L13-L15]. The compound's specificity for virus-infected cells makes it a valuable reference standard for evaluating other nucleoside analogues in antiviral screening assays [0L35-L36].
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| ln Vivo |
Detailed in vivo activity data for BVDU 5'-Triphosphate ammonium are not extensively reported in the available literature. As an active triphosphate metabolite, it is the intracellular effector molecule generated from the parent prodrug BVDU after phosphorylation by viral thymidine kinase. Therefore, its in vivo antiviral effects would typically be studied by administering the parent nucleoside BVDU, which is known to be active in animal models of HSV-1 and VZV infections.
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| Enzyme Assay |
Binding of BVDU 5'-Triphosphate ammonium to viral DNA polymerase is typically assessed using non-cellular enzyme inhibition assays. In this format, purified viral DNA polymerase from HSV-1 or VZV is incubated with the compound, a DNA template primer, and radiolabeled deoxynucleoside triphosphates. The degree of inhibition is measured by quantifying the incorporation of the radiolabel into DNA, allowing for the calculation of IC50 values for viral polymerase inhibition.
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| Cell Assay |
Cellular antiviral assays are conducted using permissive cell lines such as Vero cells infected with HSV-1 or VZV. The infected cells are treated with various concentrations of BVDU 5'-Triphosphate ammonium. After an appropriate incubation period (e.g., 3-5 days), the antiviral effect is measured by methods such as plaque reduction assays, where the number of viral plaques is counted, or by quantifying viral DNA replication using qPCR. The half-maximal inhibitory concentration (IC50) for virus replication is then determined from the dose-response curve.
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| Animal Protocol |
While BVDU 5'-Triphosphate ammonium itself is the active metabolite, in vivo animal studies are typically performed using the parent prodrug, BVDU. In a common mouse model, mice are infected with HSV-1 (e.g., via intracerebral, intraperitoneal, or cutaneous routes) to establish a lethal infection. The mice are then treated with the prodrug BVDU via oral or intraperitoneal administration at various doses. Endpoints include survival rate, development of skin lesions, and viral titers in target organs such as the brain. This in vivo system indirectly assesses the activity of the triphosphate metabolite.
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| ADME/Pharmacokinetics |
As the active triphosphate metabolite, BVDU 5'-Triphosphate ammonium is not the administered form for typical pharmacokinetic studies. The PK properties of its parent drug, BVDU, have been characterized. BVDU is reported to be well-absorbed after oral administration. It then enters infected cells, where it is sequentially phosphorylated by host and viral kinases to reach its pharmacologically active triphosphate form, which is the subject of this entry. The triphosphate itself is negatively charged, cell-impermeable, and metabolically labile.
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| Toxicity/Toxicokinetics |
Comprehensive toxicological data for BVDU 5'-Triphosphate ammonium are not detailed in standard product literature. However, the parent compound BVDU has a well-characterized safety profile in animal models. At high doses, BVDU has been associated with neurotoxicity in some animal species, and as a nucleoside analog that interferes with DNA replication, there is a theoretical risk of host cell genotoxicity. As a research-use compound, standard chemical safety precautions for handling nucleoside triphosphates should be followed, including the use of PPE.
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| References | |
| Additional Infomation |
BVDU 5'-Triphosphate ammonium has a molecular formula of C11H1₉BrN3O14P3 and a molecular weight of 590.11 g/mol [8L17-L18]. It is provided as an ammonium salt, with a purity of ≥98%. It is highly soluble in water (approx. 250 mg/mL) [8L25]. For storage, the powder is stable for up to 3 years at -20degC and 2 years at 4degC; in solution, it can be stored at -80degC for 6 months or at -20degC for 1 month, preferably under nitrogen, away from moisture [8L20-L23].
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| Molecular Formula |
C11H19BRN3O14P3
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| Molecular Weight |
590.11
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| Related CAS # |
BVDU 5′-Triphosphate;77222-61-8
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), 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) |
H2O :~250 mg/mL (~423.65 mM)
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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 | 1.6946 mL | 8.4730 mL | 16.9460 mL | |
| 5 mM | 0.3389 mL | 1.6946 mL | 3.3892 mL | |
| 10 mM | 0.1695 mL | 0.8473 mL | 1.6946 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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