| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Viral DNA polymerase (VZV and HSV-1).
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| ln Vitro |
Intense fluorescence is observed in FV-100 at 340–380 nm illumination[1]. In HeLa cells, FV-100 (1 h) causes a distinct distribution[1].
Valnivudine hydrochloride is a potent and selective inhibitor of VZV and HSV-1 DNA polymerase. The compound is a prodrug that is converted to its active form, CF-1743, after oral administration. The active metabolite is a nucleoside analog that is phosphorylated to the triphosphate form, which competes with natural deoxyguanosine triphosphate (dGTP) for incorporation into viral DNA. This leads to chain termination and inhibition of viral DNA replication. It has excellent selectivity for viral over cellular DNA polymerases. |
| ln Vivo |
In rats, FV-100 (50-500 mg/kg; po) does not appear to have any neuropharmacological effects or cause physiologically significant respiratory alterations[2].
In vivo, valnivudine hydrochloride exhibits potent antiviral activity against VZV and HSV-1. It has been studied in animal models of herpesvirus infections, demonstrating significant reduction in viral titers and clinical symptoms. The compound has favorable pharmacokinetic properties, including high oral bioavailability and good tissue distribution. It has been investigated in clinical trials for the treatment of herpes zoster, showing efficacy comparable to or better than standard therapies. |
| Enzyme Assay |
Viral DNA polymerase inhibition is assessed using enzyme assays with purified viral DNA polymerase and the active metabolite. The incorporation of radiolabeled nucleotides into DNA is measured in the presence of various concentrations of the compound. The IC₅₀ value is calculated. For selectivity studies, the compound is tested against cellular DNA polymerases. Antiviral activity is assessed by plaque reduction assays or viral yield reduction assays in virus-infected cells.
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| Cell Assay |
VZV- or HSV-1-infected cells (e.g., human foreskin fibroblasts, Vero cells) are cultured and treated with valnivudine hydrochloride at various concentrations. Viral replication is assessed by plaque reduction assay or viral DNA quantification by qPCR. Cytotoxicity is assessed in uninfected cells by MTT or similar assays. The selectivity index (SI) is calculated as the ratio of cytotoxic concentration to antiviral concentration.
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| Animal Protocol |
In vivo studies are conducted in animal models of herpesvirus infections, such as guinea pig models of HSV-1 infection or mouse models of VZV infection. The compound is administered orally or intravenously. Viral titers in target tissues are measured, and clinical signs are monitored. Pharmacokinetic parameters are determined from blood samples collected at various time points. Efficacy is compared to standard antiviral agents such as acyclovir.
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| ADME/Pharmacokinetics |
Valnivudine hydrochloride is a valine ester prodrug designed to improve the oral bioavailability of the active antiviral agent. It is rapidly absorbed after oral administration and converted to the active metabolite. The active metabolite has a long intracellular half-life, allowing for once-daily dosing. The compound has favorable pharmacokinetic properties, including good bioavailability, moderate protein binding, and elimination primarily in urine. Specific pharmacokinetic data are available from clinical studies.
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| Toxicity/Toxicokinetics |
Toxicological data for valnivudine hydrochloride are available from preclinical and clinical studies. The compound has been evaluated for safety in animal models and human clinical trials. It has a favorable safety profile with mild to moderate side effects. No significant organ toxicity or genotoxicity has been reported. Standard safety precautions should be followed when handling this compound. It is intended for research use.
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| References |
[1]. Migliore M, et, al. FV-100: the most potent and selective anti-varicella zoster virus agent reported to date. Antivir Chem Chemother. 2010 Jan 5;20(3):107-15.
[2]. Pentikis HS, et, al. Pharmacokinetics and safety of FV-100, a novel oral anti-herpes zoster nucleoside analogue, administered in single and multiple doses to healthy young adult and elderly adult volunteers. Antimicrob Agents Chemother. 2011 Jun;55(6):2847-54. |
| Additional Infomation |
Antiviral drug; potent and selective inhibition of varicella-zoster virus; structure described in the first article.
Valnivudine hydrochloride (FV-100) is a nucleoside analog prodrug for the treatment of herpesvirus infections. It has been investigated for the treatment of herpes zoster (shingles) and other VZV and HSV-1 infections. The compound offers advantages over existing therapies, including improved oral bioavailability, potent antiviral activity, and a favorable safety profile. It has been studied in clinical trials and represents a promising therapeutic option for herpesvirus infections. It is for research use. |
| Molecular Formula |
C27H36CLN3O6
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|---|---|
| Molecular Weight |
534.04
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| Exact Mass |
533.229
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| CAS # |
956483-03-7
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| Related CAS # |
Valnivudine;956483-02-6
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| PubChem CID |
71587897
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| Appearance |
White to off-white solid powder
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| LogP |
5.066
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
37
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| Complexity |
905
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| Defined Atom Stereocenter Count |
4
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| SMILES |
Cl.O1[C@H](C[C@@H]([C@H]1COC([C@H](C(C)C)N)=O)O)N1C(N=C2C(C=C(C3C=CC(=CC=3)CCCCC)O2)=C1)=O
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| InChi Key |
CAHTYTZOAVUCIU-ZMQZINMSSA-N
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| InChi Code |
InChI=1S/C27H35N3O6.ClH/c1-4-5-6-7-17-8-10-18(11-9-17)21-12-19-14-30(27(33)29-25(19)36-21)23-13-20(31)22(35-23)15-34-26(32)24(28)16(2)3;/h8-12,14,16,20,22-24,31H,4-7,13,15,28H2,1-3H3;1H/t20-,22+,23+,24-;/m0./s1
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| Chemical Name |
[(2R,3S,5R)-3-hydroxy-5-[2-oxo-6-(4-pentylphenyl)furo[2,3-d]pyrimidin-3-yl]oxolan-2-yl]methyl (2S)-2-amino-3-methylbutanoate;hydrochloride
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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) |
DMSO: 100 mg/mL (187.25 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.68 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 25.0 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: ≥ 2.5 mg/mL (4.68 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 25.0 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: ≥ 2.5 mg/mL (4.68 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 | 1.8725 mL | 9.3626 mL | 18.7252 mL | |
| 5 mM | 0.3745 mL | 1.8725 mL | 3.7450 mL | |
| 10 mM | 0.1873 mL | 0.9363 mL | 1.8725 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.
Link: https://clinicaltrials.gov/ct2/show/NCT02412917
Conditions:Shingles|Herpes Zoster|Postherpetic NeuralgiaLink: https://clinicaltrials.gov/ct2/show/NCT00900783
Conditions:Herpes Zoster|ShinglesLink: https://clinicaltrials.gov/ct2/show/NCT02322957
Conditions:Acute Herpes ZosterProducts are for research use only; We do not sell to patients
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