| 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 |
The primary targets of 3'-Azido-3'-deoxy-5-fluorocytidine are not well-defined as specific receptors or enzymes, as it is primarily used as a chemical reagent rather than a therapeutic agent. However, the compound is described as a potent antiviral medication, primarily used in the treatment of HIV/AIDS, by suppressing viral replication through inhibition of reverse transcriptase. As a cytidine derivative, it may be incorporated into viral DNA during replication, causing chain termination and inhibiting viral proliferation. Its azide moiety also allows for bioorthogonal conjugation reactions, enabling the labeling and functionalization of biomolecules.
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| ln Vitro |
In vitro studies of 3'-Azido-3'-deoxy-5-fluorocytidine are focused on its use as a click chemistry reagent and building block for nucleoside analog synthesis. The compound's azide moiety allows for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-bearing compounds. This makes it useful for labeling nucleosides, nucleotides, and oligonucleotides with fluorescent tags, biotin, or other functional groups. The compound may also have antiviral activity, as it is described as a potent antiviral medication used in the treatment of HIV/AIDS. Its utility in click chemistry makes it a valuable tool for chemical biology and molecular biology research.
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| ln Vivo |
In vivo studies of 3'-Azido-3'-deoxy-5-fluorocytidine are limited, as it is primarily used as a chemical reagent rather than a therapeutic agent. However, the compound is described as an antiviral medication used in the treatment of HIV/AIDS, suggesting potential for in vivo applications. As a nucleoside analog that inhibits reverse transcriptase, it could be studied in animal models of HIV infection or other viral diseases. Further studies are needed to evaluate its pharmacokinetic properties, bioavailability, and efficacy in vivo. The compound's azide moiety could also be used for bioorthogonal labeling in vivo if suitable alkyne-bearing probes are available.
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| Enzyme Assay |
For in vitro enzyme/receptor binding assays, 3'-Azido-3'-deoxy-5-fluorocytidine can be evaluated as a substrate or inhibitor of reverse transcriptase or other nucleic acid polymerases. The compound is incubated with the enzyme, template, and nucleotides at various concentrations. Enzyme activity is quantified by measuring nucleic acid synthesis. IC₅0 values can be determined from dose-response curves. The compound's binding to viral enzymes can be assessed using biophysical methods. Its azide moiety allows for subsequent detection or conjugation via click chemistry. Standard assay conditions include appropriate buffer systems and cofactors.
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| Cell Assay |
For in vitro cellular experiments, 3'-Azido-3'-deoxy-5-fluorocytidine can be tested in virus-infected cells to evaluate its antiviral activity. Cells are cultured in appropriate media and treated with various concentrations of the compound. Viral replication is measured by qPCR, plaque assay, or other detection methods. The compound's effects on cell viability are monitored. Its cellular uptake and metabolism can be assessed using labeled or fluorescent derivatives. The compound's azide moiety allows for detection of incorporation into nucleic acids using click chemistry with alkyne-bearing fluorescent probes.
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| Animal Protocol |
For in vivo animal experiments, 3'-Azido-3'-deoxy-5-fluorocytidine can be administered to animals via various routes including oral gavage, intravenous injection, or intraperitoneal injection, depending on its solubility and pharmacokinetic properties. Its efficacy as an antiviral agent could be evaluated in animal models of viral infections. Typical dosing regimens may range from 1 to 50 mg/kg administered daily or intermittently. Viral load, survival, and immune responses are assessed. Pharmacokinetic parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance are measured. Animal studies should follow appropriate ethical guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of 3'-Azido-3'-deoxy-5-fluorocytidine are not extensively characterized in the literature. As a nucleoside analog with a molecular weight of 286.22 g/mol, it may have limited oral bioavailability and rapid clearance. When administered systemically, the compound would likely be metabolized by nucleoside kinases and other enzymes. Its half-life in circulation would depend on its stability and clearance mechanisms. The presence of the azido and fluoro groups may influence its metabolic stability. Further pharmacokinetic studies would be needed to fully characterize its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
Toxicological data for 3'-Azido-3'-deoxy-5-fluorocytidine are limited, as it is primarily used as a chemical reagent. As a nucleoside analog, its toxicity would depend on its incorporation into nucleic acids and its effects on cellular metabolism. Azide-containing compounds can be toxic at high concentrations, and appropriate safety precautions should be taken. The compound's potential as an antiviral agent suggests it may have a favorable therapeutic index, but comprehensive toxicology studies would be needed. As with all research chemicals, appropriate safety precautions should be taken when handling this compound.
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| References | |
| Additional Infomation |
3'-Azido-3'-deoxy-5-fluorocytidine is a research compound used as a click chemistry reagent and building block for nucleoside analog synthesis. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The compound is a cytidine derivative with an Azide (N3) moiety that can undergo CuAAc with alkyne-bearing compounds. It is also described as a potent antiviral medication used in the treatment of HIV/AIDS.
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| Molecular Formula |
C9H11FN6O4
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|---|---|
| Molecular Weight |
286.21984410286
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| Exact Mass |
286.082
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| CAS # |
2095417-18-6
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| PubChem CID |
137628662
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| Appearance |
White to off-white solid powder
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| LogP |
-1.3
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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 |
3
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| Heavy Atom Count |
20
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| Complexity |
531
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| Defined Atom Stereocenter Count |
4
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| SMILES |
FC1C(N)=NC(N(C=1)[C@H]1[C@@H]([C@@H]([C@@H](CO)O1)N=[N+]=[N-])O)=O
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| InChi Key |
MOEHIWUXKDQZBL-UAKXSSHOSA-N
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| InChi Code |
InChI=1S/C9H11FN6O4/c10-3-1-16(9(19)13-7(3)11)8-6(18)5(14-15-12)4(2-17)20-8/h1,4-6,8,17-18H,2H2,(H2,11,13,19)/t4-,5-,6-,8-/m1/s1
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| Chemical Name |
4-amino-1-[(2R,3R,4S,5S)-4-azido-3-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-fluoropyrimidin-2-one
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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 : ~140 mg/mL (~489.13 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.33 mg/mL (8.14 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 23.3 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: ≥ 2.33 mg/mL (8.14 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 23.3 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: ≥ 2.33 mg/mL (8.14 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 | 3.4938 mL | 17.4691 mL | 34.9382 mL | |
| 5 mM | 0.6988 mL | 3.4938 mL | 6.9876 mL | |
| 10 mM | 0.3494 mL | 1.7469 mL | 3.4938 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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