| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Tiviciclovir hydrochloride targets hepatitis B virus (HBV) through its action as a guanosine analog that interferes with viral DNA polymerase and replication mechanisms. As a nucleoside analog, it is incorporated into viral DNA during replication, leading to chain termination and inhibition of viral genome synthesis. Drug resistance may occur through mutations in viral DNA polymerase that alter drug-target interactions. The compound is designed to improve the effectiveness of antiviral treatments.
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| ln Vitro |
In vitro studies have demonstrated that Tiviciclovir hydrochloride functions as an inhibitor of hepatitis B virus replication. As a guanosine analog, it competes with natural nucleosides for incorporation into growing viral DNA strands, resulting in premature chain termination and inhibition of viral genome synthesis. The compound's antiviral activity is attributed to its ability to target viral DNA polymerase, with resistance potentially arising through mutations that alter the drug-target interaction. Detailed IC50 values and specific cellular assay data are not extensively documented in the available literature.
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| ln Vivo |
In vivo activity of Tiviciclovir hydrochloride has been investigated primarily in the context of hepatitis B virus infection models. As an antiviral guanosine analog, it is expected to reduce viral loads through inhibition of viral DNA polymerase and disruption of viral replication. The compound's effectiveness in vivo is influenced by its pharmacokinetic properties and ability to reach target tissues. Combination strategies with synergistic antiviral agents may enhance its therapeutic efficacy. Detailed in vivo efficacy data, including specific animal model results, are limited in the available literature.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for Tiviciclovir hydrochloride typically involves evaluating its interaction with viral DNA polymerase. The compound, as a guanosine analog, is tested for its ability to inhibit polymerase activity using cell-free systems with purified enzyme and radiolabeled nucleotide substrates. Inhibition is measured by the reduction in nucleotide incorporation into DNA templates. Competition assays with natural substrates may be performed to determine the mechanism of action. Standard assay protocols include appropriate positive controls such as known polymerase inhibitors and vehicle controls.
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| Cell Assay |
In vitro cell-based assays for Tiviciclovir hydrochloride are conducted using HBV-infected cell lines such as HepG2.2.15 cells that stably support HBV replication. Cells are treated with varying concentrations of the compound, and antiviral activity is assessed by measuring HBV DNA levels in culture supernatants using quantitative PCR. Cytotoxicity is evaluated using standard cell viability assays such as MTT or CCK-8 to determine the selectivity index. The compound's ability to inhibit viral antigen secretion (HBsAg, HBeAg) may also be measured by ELISA.
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| Animal Protocol |
In vivo animal studies for Tiviciclovir hydrochloride are typically conducted using HBV transgenic mouse models or hydrodynamic injection HBV mouse models. Animals are administered the compound via oral or intraperitoneal routes at various doses, and antiviral efficacy is evaluated by measuring serum HBV DNA levels, viral antigen levels (HBsAg, HBeAg), and liver histopathology. Pharmacokinetic parameters such as Cmax, Tmax, and half-life are determined from plasma samples. Combination studies with other antiviral agents may be performed to assess synergistic effects.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Tiviciclovir hydrochloride include its formulation as a hydrochloride salt to improve solubility and bioavailability. The compound has a molecular weight of 275.69 g/mol and a molecular formula of C9H14ClN5O3. It appears as a solid with off-white to light yellow color. Storage recommendations include 4°C, sealed storage away from moisture, with in solvent stability of -80°C for 6 months and -20°C for 1 month. Detailed pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution are not extensively documented in the available literature.
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| Toxicity/Toxicokinetics |
Toxicity information for Tiviciclovir hydrochloride is limited in the available literature. As a research-use compound, standard safety precautions should be followed during handling. The compound is designated for research use only and is not for human therapeutic applications. Drug resistance may occur through mutations in viral DNA polymerase that alter drug-target interactions. Cytotoxicity should be evaluated in cell-based assays to determine the therapeutic window. No detailed acute or chronic toxicity data are available from the search results.
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| References | |
| Additional Infomation |
Tiviciclovir hydrochloride (AM188 hydrochloride) is an antiviral guanosine analog investigated as a hepatitis B virus inhibitor. The hydrochloride salt form is designed to improve solubility and bioavailability compared to the free base. The compound may exhibit resistance through mutations in viral DNA polymerase, and combination strategies with synergistic antiviral agents may be explored to enhance efficacy. It is intended for research use only and is not for human therapeutic applications.
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| Molecular Formula |
C9H14CLN5O3
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| Molecular Weight |
275.69
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| Appearance |
Off-white to light yellow solid powder
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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, 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) |
Typically soluble in DMSO (e.g. 10 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 | 3.6273 mL | 18.1363 mL | 36.2726 mL | |
| 5 mM | 0.7255 mL | 3.6273 mL | 7.2545 mL | |
| 10 mM | 0.3627 mL | 1.8136 mL | 3.6273 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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