| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
Fialuridine targets viral DNA polymerase. As a nucleoside analog, it is incorporated into viral DNA during replication, causing chain termination and inhibiting viral DNA synthesis. Its metabolites block DNA synthesis in human cytomegalovirus, hepatitis B, and herpes simplex.
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|---|---|
| ln Vitro |
In vitro, fialuridine shows activity against Vaccinia and Cowpox viruses in HFF cells with EC50 values of 1.5 and 0.2 μM, respectively. It is a nucleoside analog with antiviral activity. Its activity is consistent with its mechanism of inhibiting viral DNA polymerase.
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| ln Vivo |
Fialuridine was developed as a potential treatment for hepatitis B virus (HBV) infection. However, clinical trials were terminated due to severe toxicity. In a Phase II clinical trial, 7 out of 15 patients developed liver failure, requiring liver transplantation, and 5 died.
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| Enzyme Assay |
Fialuridine's antiviral activity is assessed using in vitro cell-based assays. In these assays, cells infected with the virus are treated with the compound, and viral replication is measured. EC50 values are determined from dose-response curves.
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| Cell Assay |
Cellular assays for fialuridine involve treating virus-infected cells with the compound and measuring viral DNA or RNA levels. The compound's ability to inhibit viral replication is assessed by quantifying viral nucleic acids using real-time PCR or other methods.
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| Animal Protocol |
In vivo animal model protocols for fialuridine would have involved its administration to animal models of viral infection. However, due to its severe toxicity, clinical development was discontinued.
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| ADME/Pharmacokinetics |
Fialuridine has a molecular weight of 372.09 and a molecular formula of C9H10FIN2O5. Specific pharmacokinetic data is not extensively detailed in the available literature.
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| Toxicity/Toxicokinetics |
Fialuridine was associated with severe hepatotoxicity in clinical trials, leading to liver failure and death in some patients. The compound is not approved for clinical use.
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| References | |
| Additional Infomation |
Firauridine is being investigated in the clinical trial NCT01337466 (Biodistribution and dosimetric assessment of [124I]FIAU). Firauridine is a nucleoside analog of uridine and is active against hepatitis B virus and herpesvirus. Firauridine inhibits viral DNA polymerase and viral replication.
Fialuridine (CAS# 69123-98-4) is a nucleoside analog with antiviral activity that was developed for the treatment of hepatitis B. Clinical development was discontinued due to severe hepatotoxicity. It is not approved for clinical use. |
| Molecular Formula |
C9H10FIN2O5
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|---|---|
| Molecular Weight |
372.0909
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| Exact Mass |
371.961
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| CAS # |
69123-98-4
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| PubChem CID |
50313
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| Appearance |
White to off-white solid powder
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| Density |
2.2±0.1 g/cm3
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| Melting Point |
216-217ºC
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| Index of Refraction |
1.685
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| LogP |
-0.32
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
18
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| Complexity |
418
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| Defined Atom Stereocenter Count |
4
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| SMILES |
C1=C(C(=O)NC(=O)N1[C@H]2[C@H]([C@@H]([C@H](O2)CO)O)F)I
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| InChi Key |
IPVFGAYTKQKGBM-BYPJNBLXSA-N
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| InChi Code |
InChI=1S/C9H10FIN2O5/c10-5-6(15)4(2-14)18-8(5)13-1-3(11)7(16)12-9(13)17/h1,4-6,8,14-15H,2H2,(H,12,16,17)/t4-,5+,6-,8-/m1/s1
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| Chemical Name |
1-[(2R,3S,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-iodopyrimidine-2,4-dione
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| Synonyms |
DRG-0098; FIAU; Fialuridine
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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 : ~100 mg/mL (~268.75 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.72 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 (6.72 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 (6.72 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 | 2.6875 mL | 13.4376 mL | 26.8752 mL | |
| 5 mM | 0.5375 mL | 2.6875 mL | 5.3750 mL | |
| 10 mM | 0.2688 mL | 1.3438 mL | 2.6875 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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