Fialuridine (Synonyms: FIAU,Fluoroiodoarauracil,5-Iodo-2’-Fluoroarauracil,NSC 678514) |
Catalog No.GC11943
One-Click Copy Product Info
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nucleoside analog with antiviral activity
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 69123-98-4
Sample solution is provided at 25 µL, 10mM.
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Ki: 0.14 and 0.95 μM for herpes simplex virus types 1 and 2, respectively
Fialuridine is a nucleoside analog with antiviral activity.
Nucleoside analogues mimic physiological nucleosides in terms of uptake and metabolism and are incorporated into newly synthesized DNA resulting in synthesis inhibition and chain termination.
In vitro: Previous in-vitro data showed that 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-ethyluracil (FEAU) had activity against herpes simplex virus types 1 and 2 comparable to that of 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-methyluracil (FMAU), fialuridine (FIAU), and acyclovir (ACV). The cellular toxicity of FEAU was found to be much lower than that of FIAU. Biochemical experiments indicated that FEAU had similar affinity toward thymidine kinases encoded by HSV 1 and 2 and a much lower affinity for cellular thymidine kinase than thymidine [1].
In vivo: The in-vivo antiviral efficiency of FEAU was compared with that of FIAU and ACV by using the herpes encephalitis mode. Moreover, ACV and FEAU could significantly increase the number of survivors at doses of 50 and 100 mg/kg per day, respectively, and FIAU showed significant activity at 25 mg/kg per day in the animal model [1].
Clinical trial: In patients with chronic hepatitis B, fialuridine treatment induced a severe toxic reaction demonstrated by hepatic failure, lactic acidosis, pancreatitis, neuropathy, as well as myopathy. Such toxic reaction was probably caused by widespread mitochondrial damage and [2].
References:
[1] Mansuri, M. M.,Ghazzouli, I.,Chen, M.S., et al. 1-(2-Deoxy-2-fluoro-β-D-arabinofuranosyl)-5-ethyluracil. A highly selective antiherpes simplex agent. Journal of Medicinal Chemistry 30(5), 867-871 (1987).
[2] McKenzie R et al. Hepatic failure and lactic acidosis due to fialuridine (FIAU), an investigational nucleoside analogue for chronic hepatitis B. N Engl J Med. 1995 Oct 26;333(17):1099-105.
| Cas No. | 69123-98-4 | SDF | |
| Synonyms | FIAU,Fluoroiodoarauracil,5-Iodo-2’-Fluoroarauracil,NSC 678514 | ||
| Chemical Name | 1-(2-deoxy-2-fluoro-β-D-arabinofuranosyl)-5-iodo-2,4(1H,3H)-pyrimidinedione | ||
| Canonical SMILES | OC[C@@H]1[C@@H](O)[C@H](F)[C@H](N2C=C(I)C(NC2=O)=O)O1 | ||
| Formula | C9H10FIN2O5 | M.Wt | 372.1 |
| Solubility | ≤15mg/ml in DMSO;20mg/ml in dimethyl formamide | Storage | Store at -20°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6874 mL | 13.4372 mL | 26.8745 mL |
| 5 mM | 537.5 μL | 2.6874 mL | 5.3749 mL |
| 10 mM | 268.7 μL | 1.3437 mL | 2.6874 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)