| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
Purity: ≥98%
| Targets |
Desciclovir targets viral DNA polymerase after its conversion to acyclovir in vivo. Acyclovir, the active form, is a nucleoside analogue that is selectively phosphorylated by viral thymidine kinase in herpesvirus-infected cells. The phosphorylated acyclovir (acyclovir triphosphate) inhibits viral DNA polymerase by competing with deoxyguanosine triphosphate (dGTP) and by incorporating into the growing DNA chain, causing chain termination. This inhibits viral DNA replication and prevents the virus from multiplying. Desciclovir is a prodrug that is converted to acyclovir by xanthine oxidase, making it orally active. The compound is active against HSV-1, HSV-2, and VZV.
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| ln Vitro |
In vitro studies have demonstrated that Desciclovir is a prodrug of acyclovir with activity against viruses of the Herpesviridae family. It is converted to acyclovir in vivo by xanthine oxidase. The antiviral activity of Desciclovir is attributed to its conversion to acyclovir, which inhibits viral DNA polymerase. In vitro assays using herpesvirus-infected cells have confirmed the antiviral activity of acyclovir, the active metabolite of Desciclovir. The compound's potency and selectivity for herpesvirus-infected cells make it a valuable tool for antiviral research. Desciclovir is primarily used as a research compound to study the pharmacology of acyclovir and its prodrugs.
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| ln Vivo |
In vivo studies have demonstrated that Desciclovir is an orally active prodrug of acyclovir. It is absorbed from the gastrointestinal tract and is converted to acyclovir by xanthine oxidase. The compound's oral bioavailability makes it a valuable alternative to acyclovir, which has limited oral bioavailability. Desciclovir has been studied in animal models of herpesvirus infections, where it has demonstrated efficacy in reducing viral replication and disease severity. However, specific in vivo data for Desciclovir are limited, as it is primarily a research compound and acyclovir is the clinically approved drug. Desciclovir is not approved for clinical use and is strictly a research compound.
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| Enzyme Assay |
Non-cellular enzyme assays for Desciclovir typically involve measuring the activity of xanthine oxidase, the enzyme responsible for converting Desciclovir to acyclovir. These assays use purified xanthine oxidase and measure the conversion of Desciclovir to acyclovir by HPLC or mass spectrometry. The compound is tested at various concentrations to determine the kinetics of the conversion. These assays are essential for characterizing the prodrug properties of Desciclovir and for studying the pharmacology of acyclovir and its prodrugs. The selectivity of xanthine oxidase for Desciclovir over other substrates can also be assessed in these assays.
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| Cell Assay |
In vitro cell-based assays for Desciclovir typically use herpesvirus-infected cell lines, such as Vero cells infected with HSV-1 or HSV-2, to assess the compound's antiviral activity. Cells are infected with the virus and treated with Desciclovir at various concentrations. Viral replication is assessed by measuring the production of viral progeny (plaque reduction assay) or by measuring viral DNA or protein levels. The EC50 for inhibition of viral replication is determined from dose-response curves. Cytotoxicity is assessed using MTT or similar assays to determine the selectivity index. Desciclovir is typically dissolved in DMSO and diluted in culture medium, with DMSO controls included to account for solvent effects.
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| Animal Protocol |
In vivo animal studies for Desciclovir typically involve rodent models of herpesvirus infections, such as HSV-1 or HSV-2 infection in mice or guinea pigs. Animals are infected with the virus and treated with Desciclovir at various doses, typically administered orally. Viral replication, disease severity (e.g., skin lesions, encephalitis), and survival are assessed. The compound's efficacy is compared to that of acyclovir. However, specific published in vivo data for Desciclovir are limited, as it is primarily a research compound and acyclovir is the clinically approved drug. Desciclovir is not approved for clinical use and is strictly a research compound.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies of Desciclovir have shown that it is absorbed from the gastrointestinal tract and is converted to acyclovir by xanthine oxidase. The compound's oral bioavailability makes it a valuable prodrug of acyclovir. Acyclovir is distributed to tissues and is eliminated primarily by renal excretion. The pharmacokinetic profile of Desciclovir is similar to that of acyclovir after conversion. However, detailed PK parameters for Desciclovir are limited, as it is primarily a research compound. Desciclovir is not approved for clinical use and is strictly a research compound.
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| Toxicity/Toxicokinetics |
Toxicological data for Desciclovir are limited, as it is primarily a research compound and acyclovir is the clinically approved drug. Acyclovir is generally well-tolerated at therapeutic doses, with the most common adverse effects being gastrointestinal disturbances, headache, and rash. Nephrotoxicity can occur with high doses, particularly in patients with renal impairment. The safety profile of Desciclovir is expected to be similar to that of acyclovir after conversion. However, specific toxicological data for Desciclovir are not extensively documented. Desciclovir is not approved for clinical use and is strictly a research compound.
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| Additional Infomation |
Desciclovir is a prodrug of acyclovir and is active against viruses of the Herpesviridae family. After absorption from the gastrointestinal tract, deciclovir is converted to acyclovir by xanthine oxidase. Acyclovir is further converted to cyclophosphamide triphosphate by viral thymidine kinase, which competitively inhibits viral DNA polymerase by incorporating into the elongating viral DNA chain, thereby terminating further polymerization.
Desciclovir is a synthetic nucleoside analogue and an orally active prodrug of the antiviral agent acyclovir (ACV). It has the molecular formula C8H11N5O2 and CAS number 84408-37-7. Desciclovir is converted to acyclovir in vivo by xanthine oxidase. It is active against HSV-1, HSV-2, and VZV. Desciclovir is not approved for clinical use and is strictly a research compound for studying the pharmacology of acyclovir and its prodrugs. |
| Molecular Formula |
C8H11N5O2
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|---|---|
| Molecular Weight |
209.20524
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| Exact Mass |
209.091
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| CAS # |
84408-37-7
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| Related CAS # |
84408-37-7
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| PubChem CID |
55256
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.61g/cm3
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| Boiling Point |
529.8ºC at 760 mmHg
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| Flash Point |
274.2ºC
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| Index of Refraction |
1.725
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| LogP |
-1.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
15
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| Complexity |
206
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OCCOCN1C2C(=CN=C(N)N=2)N=C1
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| InChi Key |
OKQHSIGMOWQUIK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H11N5O2/c9-8-10-3-6-7(12-8)13(4-11-6)5-15-2-1-14/h3-4,14H,1-2,5H2,(H2,9,10,12)
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| Chemical Name |
2-[(2-Aminopurin-9-yl)methoxy]ethanol
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| Synonyms |
Desciclovir
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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) |
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 | 4.7799 mL | 23.8994 mL | 47.7989 mL | |
| 5 mM | 0.9560 mL | 4.7799 mL | 9.5598 mL | |
| 10 mM | 0.4780 mL | 2.3899 mL | 4.7799 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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