| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Vidarabine targets viral DNA polymerase, specifically the herpesvirus DNA polymerase. After cellular uptake, vidarabine is sequentially phosphorylated by cellular kinases to vidarabine triphosphate (Ara-ATP). Ara-ATP competitively inhibits viral DNA polymerase with higher affinity than the host cellular DNA polymerase, leading to selective inhibition of viral DNA synthesis. It also incorporates into viral DNA, causing chain termination. The compound has activity against HSV-1, HSV-2, and VZV. Its selectivity for viral polymerase over host polymerases underlies its antiviral efficacy. Resistance can occur via mutations in the viral thymidine kinase or DNA polymerase genes.
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| ln Vitro |
In vitro, Vidarabine demonstrates potent antiviral activity against HSV-1, HSV-2, and VZV in cell culture systems. The compound inhibits viral replication with IC₅₀ values typically in the low micromolar range, depending on the cell line and virus strain. It is also active against certain acyclovir-resistant HSV strains. In addition to antiviral effects, vidarabine has shown immunosuppressive and anticancer activities in some studies. Its cytotoxicity to host cells is relatively low compared to its antiviral potency. The compound is often used as a reference standard in antiviral susceptibility testing and in studies of nucleoside analog mechanisms.
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| ln Vivo |
In vivo, Vidarabine is effective against herpes simplex encephalitis, varicella-zoster infections, and herpes keratitis. It was historically used intravenously for the treatment of HSV encephalitis and neonatal HSV infections, though it has been largely replaced by acyclovir due to better safety and efficacy. Topical vidarabine ointment is used for herpes keratitis. The compound undergoes rapid deamination by adenosine deaminase to its inactive metabolite hypoxanthine arabinoside, which reduces its systemic half-life. Its clinical utility is limited by poor oral bioavailability and dose-limiting neurotoxicity. It is used in veterinary medicine for certain viral infections.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cellular) assays for Vidarabine involve measuring inhibition of viral DNA polymerase activity. The assay typically uses purified HSV DNA polymerase and a synthetic DNA template/primer. Incorporation of radiolabeled dNTPs is measured in the presence of varying concentrations of vidarabine triphosphate (the active form). The compound competitively inhibits dATP incorporation. IC₅₀ values are calculated from inhibition curves. Selectivity is assessed by comparing inhibition of viral polymerase versus host DNA polymerase α. Additionally, deamination by adenosine deaminase can be measured spectrophotometrically by monitoring the conversion to hypoxanthine arabinoside at 265 nm.
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| Cell Assay |
In vitro cellular experiments with Vidarabine are performed using Vero, HeLa, or other susceptible cell lines infected with HSV or VZV. Cells are cultured in appropriate media (e.g., DMEM with 10% FBS) and infected with virus at a suitable MOI. After viral adsorption, cells are treated with serial dilutions of vidarabine (typically 0.1-100 µM) for 48-72 hours. Antiviral activity is assessed by plaque reduction assay, virus yield reduction, or by measuring cytopathic effect (CPE) inhibition. The 50% effective concentration (EC₅₀) and 50% cytotoxic concentration (CC₅₀) are determined, and the selectivity index (SI) is calculated. Cell viability is assessed using MTT or neutral red uptake. Cells are maintained at 37°C in 5% CO₂.
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| Animal Protocol |
In vivo animal studies with Vidarabine have been conducted in mouse models of herpes encephalitis and keratitis. Mice are inoculated intracerebrally or intranasally with HSV, and vidarabine is administered intraperitoneally, intravenously, or topically at various doses and schedules. Efficacy is assessed by survival rates, clinical scores, viral titers in brain tissues, and histopathological examination. For keratitis models, rabbits are infected on the cornea and treated with topical ointment; lesion severity and viral shedding are evaluated. Pharmacokinetic studies measure plasma and tissue concentrations of vidarabine and its metabolite. Due to rapid deamination, combination with deaminase inhibitors (e.g., co-vidarabine) has been explored to enhance efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Vidarabine indicate poor oral bioavailability (<20%) due to first-pass metabolism and deamination. The compound has a molecular weight of 285.26 g/mol and is soluble in water. After intravenous administration, it is rapidly distributed and deaminated by adenosine deaminase to hypoxanthine arabinoside, which is inactive. The plasma half-life of vidarabine is approximately 15-30 minutes, while the metabolite has a longer half-life of 2-4 hours. The compound penetrates the central nervous system, achieving cerebrospinal fluid concentrations about 30-50% of plasma levels. It is excreted primarily in urine as the metabolite. Storage: 2-8°C, protected from light. Purity: ≥98%.
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| Toxicity/Toxicokinetics |
Vidarabine is associated with dose-limiting toxicities including gastrointestinal disturbances (nausea, vomiting), neurotoxicity (tremor, hallucinations, peripheral neuropathy), and myelosuppression (anemia, leukopenia). At high doses, it can cause hepatotoxicity and renal impairment. The compound is contraindicated in patients with hypersensitivity to vidarabine. Standard safety precautions for handling antiviral agents apply, including use of personal protective equipment (gloves, goggles, lab coat) and working in a biological safety cabinet. The compound is for research use and not for human therapeutic use without regulatory approval. Purity: ≥98%. Storage: 2-8°C, protect from light.
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| References | |
| Additional Infomation |
Vidarabine monohydrate is an adenine-arabinoside. It is a nucleoside analog active against herpes simplex virus and varicella-zoster virus. Vidarabine is converted to monophosphate by viral thymidine kinase, and then further modified to triphosphate by host enzymes. Vidarabine triphosphate directly inhibits DNA polymerase and acts as a chain terminator during DNA replication. It is a nucleoside antibiotic isolated from Streptomyces antibioticus. It possesses certain antitumor properties, exhibits broad-spectrum activity against DNA viruses in cell culture, and demonstrates significant antiviral activity against infections caused by various viruses, such as herpesvirus, vaccinia virus, and varicella-zoster virus.
Vidarabine monohydrate (CAS 24356-66-9) is a purine nucleoside antiviral drug, also known as Ara-A. It has molecular formula C₁₀H₁₅N₅O₅ and molecular weight 285.26 g/mol. Vidarabine is active against HSV and VZV by inhibiting viral DNA polymerase after phosphorylation to Ara-ATP. It was FDA‑approved in 1976 for herpes keratitis and later for systemic herpes infections, though now largely replaced by acyclovir. The compound is used as a research standard and in veterinary medicine. Purity: ≥98%. Storage: 2-8°C, protect from light. |
| Molecular Formula |
C₁₀H₁₅N₅O₅
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|---|---|
| Molecular Weight |
285.26
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| Exact Mass |
285.107
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| CAS # |
24356-66-9
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| Related CAS # |
Vidarabine;5536-17-4
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| PubChem CID |
32326
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| Appearance |
White to off-white solid powder
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| Melting Point |
257.0-257.5ºC (0.4 H2O)
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
335
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1=NC(=C2C(=N1)N(C=N2)[C@H]3[C@H]([C@@H]([C@H](O3)CO)O)O)N.O
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| InChi Key |
ZTHWFVSEMLMLKT-CAMOTBBTSA-N
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| InChi Code |
InChI=1S/C10H13N5O4.H2O/c11-8-5-9(13-2-12-8)15(3-14-5)10-7(18)6(17)4(1-16)19-10;/h2-4,6-7,10,16-18H,1H2,(H2,11,12,13);1H2/t4-,6-,7+,10-;/m1./s1
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| Chemical Name |
(2R,3S,4S,5R)-2-(6-aminopurin-9-yl)-5-(hydroxymethyl)oxolane-3,4-diol;hydrate
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| Synonyms |
Vidarabine monohydrate; Vidarabine monohydrate
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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 : ~250 mg/mL (~876.39 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5056 mL | 17.5279 mL | 35.0557 mL | |
| 5 mM | 0.7011 mL | 3.5056 mL | 7.0111 mL | |
| 10 mM | 0.3506 mL | 1.7528 mL | 3.5056 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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