| Size | Price | Stock | Qty |
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| 1mg |
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| 25mg | |||
| Other Sizes |
| Targets |
Filociclovir targets viral DNA replication by inhibiting HSV thymidine kinase and viral DNA polymerase. It is a nucleoside analog that selectively inhibits viral DNA replication. The compound has broad-spectrum activity against herpesviruses including CMV, HHV-6, and HHV-8, with EC50 values ranging from 0.7 μM to 8 μM.
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| ln Vitro |
In vitro, Filociclovir demonstrates potent antiviral activity against cytomegalovirus (CMV), herpes simplex virus (HHV)-6, and HHV-8 with EC50 values ranging from 0.7 μM to 8 μM. As a nucleoside analog, it selectively inhibits viral DNA replication by targeting viral thymidine kinase and DNA polymerase. The compound shows good selectivity for viral versus host enzymes.
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| ln Vivo |
In vivo, Filociclovir is an antiviral drug candidate that has been evaluated in clinical trials. It has demonstrated antiviral efficacy in animal models of herpesvirus infection. The compound is under investigation for the treatment of herpes simplex virus (HSV) infections and other herpesvirus diseases. Specific in vivo efficacy data are available from preclinical and clinical studies.
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| Enzyme Assay |
The in vitro antiviral assay for Filociclovir involves measuring its ability to inhibit viral replication in infected cell cultures. Cells are infected with CMV, HHV-6, or HHV-8 and treated with varying concentrations of Filociclovir. Viral DNA replication is measured by qPCR or plaque reduction assays. The EC50 is calculated from dose-response curves. Filociclovir shows EC50 values ranging from 0.7 μM to 8 μM against different herpesviruses.
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| Cell Assay |
In vitro cellular assays for Filociclovir involve treating herpesvirus-infected cell lines with varying concentrations of the compound. Viral replication is assessed by measuring viral DNA levels using qPCR or by plaque formation. Cell viability is assessed using MTT assays to determine cytotoxicity. The selectivity index (SI) is calculated as the ratio of cytotoxicity to antiviral activity. Filociclovir demonstrates potent antiviral activity with EC50 values ranging from 0.7 μM to 8 μM.
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| Animal Protocol |
In vivo animal experiments for Filociclovir typically use mouse models of herpesvirus infection. Animals are infected with CMV, HSV, or other herpesviruses and treated with Filociclovir via oral or intraperitoneal routes at various doses. Viral loads in target organs (e.g., liver, lung, brain) are measured by qPCR. Survival rates and clinical signs are monitored to assess efficacy. The compound has been evaluated in preclinical models of herpesvirus infection.
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| ADME/Pharmacokinetics |
Filociclovir has been under investigation in clinical trials, including NCT01433835 for safety and pharmacokinetics of single oral doses in healthy volunteers. As an orally administered nucleoside analog, it is expected to have good oral bioavailability. The compound's molecular weight is 277.28 (C10H11N5O3). Specific PK parameters would be available from clinical pharmacology studies.
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| Toxicity/Toxicokinetics |
Filociclovir has been evaluated in clinical trials, with NCT01433835 completed for safety and pharmacokinetics in healthy volunteers. As an antiviral nucleoside analog, potential adverse effects may include gastrointestinal disturbances, headache, and myelosuppression. Complete toxicology data including acute, repeated-dose, and genotoxicity studies would be available from the compound's development program.
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| References | |
| Additional Infomation |
Filociclovir is being studied in the clinical trial NCT01433835 (Safety and pharmacokinetics of a single oral dose of Filociclovir in healthy volunteers).
Filociclovir (CAS#: 632325-71-4) is a broad-spectrum anti-herpesvirus nucleoside analog also known as MBX-400, ZSM-162, and Cyclopropavir. It demonstrates potent activity against CMV, HHV-6, and HHV-8 with EC50 values of 0.7-8 μM. The compound has been investigated in clinical trials (NCT01433835) but is not yet approved for clinical use. |
| Molecular Formula |
C11H13N5O3
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|---|---|
| Molecular Weight |
263.257
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| Exact Mass |
263.102
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| CAS # |
632325-71-4
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| PubChem CID |
135409256
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| Appearance |
White to off-white solid powder
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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 |
3
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| Heavy Atom Count |
19
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| Complexity |
471
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1/C(=C/N2C=NC3=C2N=C(NC3=O)N)/C1(CO)CO
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| InChi Key |
KMUNHOKTIVSFRA-KXFIGUGUSA-N
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| InChi Code |
InChI=1S/C11H13N5O3/c12-10-14-8-7(9(19)15-10)13-5-16(8)2-6-1-11(6,3-17)4-18/h2,5,17-18H,1,3-4H2,(H3,12,14,15,19)/b6-2-
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| Chemical Name |
2-amino-9-[(Z)-[2,2-bis(hydroxymethyl)cyclopropylidene]methyl]-1H-purin-6-one
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| Synonyms |
MBX400 ZSM162MBX 400 ZSM 162MBX-400MBX-400 ZSM-162 Cyclopropavir
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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 : ~33.33 mg/mL (~126.61 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 | 3.7985 mL | 18.9926 mL | 37.9853 mL | |
| 5 mM | 0.7597 mL | 3.7985 mL | 7.5971 mL | |
| 10 mM | 0.3799 mL | 1.8993 mL | 3.7985 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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