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| Targets |
Sorivudine inhibits viral DNA synthesis by acting as a nucleoside analog. It is phosphorylated to its active triphosphate form, which is incorporated into the viral DNA chain during replication, leading to chain termination and inhibition of viral polymerase. Its selective activity against HSV-1 and VZV is due to its higher affinity for the viral thymidine kinase compared to the cellular enzyme.
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| ln Vitro |
Sorivudine (BV-araU) inhibits the wild-type strains VR-3 and UW-268 of HSV-1 and HSV-2, with ID50s (50 percent inhibitory dose) of 0.39 and 0.67 μM, respectively[1]. Sorivudine exhibits antiviral activity against multiple viruses, such as the Epstein-Barr virus, varicella zoster virus, and herpes simplex type 1 virus[1]. Sorivudine (BV-araU) is an analog of pyrimidine nucleoside that, at concentrations of 00001-0.004 mg/ml, exhibits in vitro inhibitory activity against varicella zoster virus (VZV). These concentrations are more than a thousand times lower than what acyclovir 3 needs to inhibit VZV replication. In addition, sorivudine prevents HSV-I replication at concentrations between 0.03-0.1 mg/ml[2]. |
| ln Vivo |
Sorivudine (BV-araU) has been tested for use in treating HSV-l encephalitis in mice when given orally. Treatment prolongs the survival of mice at dosages above 12.5 mg/kg. The mortality rate significantly decreased as we1l with doses greater than 50 mg/kg. The model of simian varicella virus infection in African green monkeys (Cerophithecus aethiops) is a more pertinent one. In this system, sorivudine therapy offered complete protection against viremia and mortality at dosages as low as 20 mg/kg per day administered intramuscularly or 100 mg/kg per day administered orally. There was no indication of neurotoxicity or aberrant hematological or clinical chemistries during the course of these investigations. Effective doses were as low as 0.2 mg/kg daily; however, at lower dosages, breakthrough viremia was observed[2]. |
| Enzyme Assay |
In vitro enzyme assays for Sorivudine typically measure the inhibition of viral DNA polymerase. The compound's active form (the triphosphate) is tested against the purified viral enzyme to determine its potency (IC50). Alternatively, the compound's ability to inhibit viral replication in cell culture is assessed using standard antiviral susceptibility tests.
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| Cell Assay |
In vitro cellular assays for Sorivudine involve treating virus-infected cell cultures (e.g., Vero cells infected with HSV-1 or VZV) with the compound and measuring viral replication. The reduction in viral titer or the expression of viral proteins (e.g., by immunofluorescence) is quantified to determine the compound's antiviral activity and selectivity index.
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| Animal Protocol |
In vivo animal models for Sorivudine include models of herpesvirus infection, such as HSV-1 or VZV infection in mice or guinea pigs. The compound is administered orally, and its effects on viral replication, lesion formation (e.g., skin lesions), and survival are assessed. Pharmacokinetic and toxicity studies are also conducted in these models.
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| ADME/Pharmacokinetics |
Sorivudine has a molecular formula of C11H13BrN2O6 and a molecular weight of 349.13 g/mol. Its chemical name is 5-[(E)-2-Bromovinyl]-1-[(2R,3S,4S,5R)-3,4-Dihydroxy-5-(Hydroxymethyl)Tetrahydrofuran-2-Yl]Pyrimidine-2,4-Dione. It is an orally active antiviral nucleoside analog and should be stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
Sorivudine is an antiviral nucleoside analog with a well-characterized mechanism of action. Potential toxicity includes bone marrow suppression and gastrointestinal disturbances. It has been associated with severe and sometimes fatal drug-drug interactions when co-administered with certain drugs (e.g., 5-fluorouracil). It is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
Sorivudine is an organic molecular entity. Sorivudine was used in clinical trials to study the treatment of varicella and HIV infection. Sorivudine is a synthetic thymidine analog with potent antiviral activity against herpes simplex virus and varicella-zoster virus. Sorivudine is phosphorylated intracellularly to a triphosphate form; this metabolite interferes with viral DNA replication by inhibiting DNA polymerase activity without being incorporated into the elongating viral DNA. Due to the risk of interactions between its metabolites and other drugs, solivudine has been withdrawn from the market.
Sorivudine is an orally-active antiviral nucleoside analog with activity against HSV-1 and VZV. It inhibits viral DNA synthesis. The compound is for research use only and is not approved for human therapeutic use due to safety and drug interaction concerns. |
| Molecular Formula |
C11H13BRN2O6
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|---|---|
| Molecular Weight |
349.137
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| Exact Mass |
347.996
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| Elemental Analysis |
C, 37.84; H, 3.75; Br, 22.89; N, 8.02; O, 27.49
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| CAS # |
77181-69-2
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| PubChem CID |
5282192
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| Appearance |
White to off-white solid powder
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| Density |
1.979g/cm3
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| Melting Point |
182 °C
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| Index of Refraction |
1.746
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| LogP |
-0.9
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
480
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| Defined Atom Stereocenter Count |
4
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| SMILES |
Br/C(/[H])=C(/[H])\C1C(N([H])C(N(C=1[H])[C@]1([H])[C@]([H])([C@@]([H])([C@@]([H])(C([H])([H])O[H])O1)O[H])O[H])=O)=O
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| InChi Key |
GCQYYIHYQMVWLT-HQNLTJAPSA-N
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| InChi Code |
InChI=1S/C11H13BrN2O6/c12-2-1-5-3-14(11(19)13-9(5)18)10-8(17)7(16)6(4-15)20-10/h1-3,6-8,10,15-17H,4H2,(H,13,18,19)/b2-1+/t6-,7-,8+,10-/m1/s1
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| Chemical Name |
5-[(E)-2-bromoethenyl]-1-[(2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione
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| Synonyms |
Sorivudine; Bravavir; BV-araU; BVAU; ARYS-01; JA-001; ARYS01; JA001; SQ32756; YN72; DRU0136; DRU-0136; SQ-32756; YN-72
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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 : ~125 mg/mL (~358.0 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.96 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 (5.96 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.96 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8642 mL | 14.3209 mL | 28.6418 mL | |
| 5 mM | 0.5728 mL | 2.8642 mL | 5.7284 mL | |
| 10 mM | 0.2864 mL | 1.4321 mL | 2.8642 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00002358 | Completed | Drug: Sorivudine | HIV Infections Chickenpox |
Bristol-Myers Squibb | N/A | Phase 3 |
| NCT00000953 | Completed | Drug: Sorivudine Drug: Acyclovir |
HIV Infections Chickenpox |
National Institute of Allergy and Infectious Diseases (NIAID) |
N/A | Phase 2 |
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