| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
The primary target of tiviciclovir is the viral DNA polymerase of herpesviruses. After conversion to penciclovir, the active form is phosphorylated by viral thymidine kinase to the monophosphate, then to the triphosphate by cellular kinases. Penciclovir triphosphate competes with deoxyguanosine triphosphate (dGTP) for incorporation into viral DNA, acting as a chain terminator. This inhibits viral DNA synthesis and replication. The compound has higher affinity for viral DNA polymerase than for cellular DNA polymerase.
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| ln Vitro |
In vitro studies have demonstrated the antiviral activity of tiviciclovir against HSV-1, HSV-2, and VZV. The compound shows potent inhibition of viral replication in cell culture systems. Penciclovir, the active form, has EC₅₀ values in the low micromolar range against herpesviruses. Tiviciclovir's activity is similar to that of penciclovir, with the advantage of improved oral bioavailability. The compound is also active against acyclovir-resistant HSV strains with thymidine kinase mutations in some cases.
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| ln Vivo |
In vivo studies have shown the efficacy of tiviciclovir in animal models of herpesvirus infection. The compound has been evaluated in mouse models of HSV infection, demonstrating reduction in viral titers and improved survival. Tiviciclovir's improved oral bioavailability compared to penciclovir allows for effective oral dosing. The compound has also been studied in animal models of VZV infection. Specific in vivo data have been reported in the antiviral literature.
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| Enzyme Assay |
For antiviral activity screening, standard plaque reduction assays are used. Susceptible cell lines such as Vero cells are infected with HSV or VZV and treated with serial dilutions of tiviciclovir or penciclovir. Viral plaques are counted, and EC₅₀ values are calculated. For mechanism studies, DNA polymerase inhibition assays are performed using purified viral and cellular DNA polymerases. Incorporation of radiolabeled nucleotides into DNA is measured.
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| Cell Assay |
For in vitro cell-based studies, Vero or other susceptible cells are cultured in appropriate media and infected with HSV or VZV at an appropriate MOI. Cells are treated with serial dilutions of tiviciclovir. Antiviral activity is assessed by plaque reduction assay, viral DNA quantification by qPCR, or viral protein expression by immunofluorescence. Cytotoxicity is assessed in parallel using standard cell viability assays. Time-of-addition studies are performed to determine the stage of the viral life cycle affected.
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| Animal Protocol |
In vivo animal studies for tiviciclovir typically use mouse models of HSV infection. Mice are infected with HSV (e.g., by intravaginal, intraperitoneal, or cutaneous routes) and treated with tiviciclovir via oral or other routes. Efficacy endpoints include survival, lesion development, viral titers in target tissues, and clinical score. Pharmacokinetic sampling is often included to correlate exposure with efficacy. Standard protocols for herpesvirus efficacy studies are described in the literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of tiviciclovir have been characterized. As a diacetyl ester prodrug, tiviciclovir has improved oral bioavailability compared to penciclovir. The compound is rapidly converted to penciclovir after absorption. Penciclovir has a half-life that supports twice-daily dosing. The compound has low protein binding and is eliminated primarily by renal excretion. Specific PK parameters such as Cmax, Tmax, AUC, half-life, and oral bioavailability have been reported in the literature.
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| Toxicity/Toxicokinetics |
Toxicological data for tiviciclovir have been generated as part of preclinical safety assessment. The compound has a favorable safety profile, consistent with other nucleoside analogues. Standard toxicology studies including acute toxicity, repeated-dose toxicity, genotoxicity, and reproductive toxicity have been conducted. The compound's safety profile in animal models supports clinical development. Specific toxicity data such as NOAEL and target organ toxicity have been reported.
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| References | |
| Additional Infomation |
Tevestrol is a bicyclic heterocyclic compound with activity against hepatitis B virus.
Tiviciclovir is an antiviral agent developed for the treatment of herpesvirus infections. No clinical trials have been reported for tiviciclovir specifically, though penciclovir (the active form) and its prodrug famciclovir are clinically used. Tiviciclovir represents an alternative prodrug approach for penciclovir delivery. The compound is a research chemical used in antiviral studies. Further development would require clinical evaluation. |
| Molecular Formula |
C9H13N5O3
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|---|---|
| Molecular Weight |
239.23
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| Exact Mass |
239.102
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| CAS # |
103024-93-7
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| PubChem CID |
135436454
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.78g/cm3
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| Boiling Point |
667.1ºC at 760 mmHg
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| Flash Point |
357.3ºC
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| Vapour Pressure |
1.04E-18mmHg at 25°C
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| Index of Refraction |
1.784
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| LogP |
-2.3
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
17
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| Complexity |
331
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OCC(CN1C=NC2=C(N=C(N=C12)N)O)CO
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| InChi Key |
ANFNNSIOGODJDN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C9H13N5O3/c10-9-12-7-6(8(17)13-9)11-4-14(7)1-5(2-15)3-16/h4-5,15-16H,1-3H2,(H3,10,12,13,17)
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| Chemical Name |
2-amino-9-[3-hydroxy-2-(hydroxymethyl)propyl]-1H-purin-6-one
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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 | 4.1801 mL | 20.9004 mL | 41.8008 mL | |
| 5 mM | 0.8360 mL | 4.1801 mL | 8.3602 mL | |
| 10 mM | 0.4180 mL | 2.0900 mL | 4.1801 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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