| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
HCV RNA polymerase / Viral replication machinery.
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|---|---|
| ln Vitro |
In order to prevent the replication of the Hepatitis C virus (HCV), Nucleoside-Analog-2 is a 4'-Azidocytidine analogue. Citation for substance 12[1].
The compound demonstrates anti-HCV activity by acting as a chain-terminating nucleoside analog. As a 4'-azidocytidine analogue, it is likely incorporated into the growing RNA chain by the viral RNA-dependent RNA polymerase (NS5B), resulting in premature chain termination and inhibition of viral RNA replication. Detailed potency (EC50) values and resistance profiles are not specified in standard datasets. |
| ln Vivo |
Cells: HCV replicon-harboring cells (e.g., Huh-7 cells containing subgenomic or full-length HCV replicons). Protocol: Cells are treated with various concentrations of Nucleoside-Analog-2 for 48-72 hours. Antiviral activity is measured by quantifying HCV RNA levels using real-time RT-PCR or by detecting HCV proteins (e.g., NS3, NS5A) via Western blot or immunofluorescence. Cytotoxicity is assessed via MTT or CellTiter-Glo assays in parallel.
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| Enzyme Assay |
No specific in vivo data found; please refer to general HCV drug properties: In mouse models of HCV infection (e.g., uPA-SCID chimeric mice with humanized livers), nucleoside analogs are typically administered orally or intraperitoneally at 10-100 mg/kg daily for 2-4 weeks, achieving significant reductions in serum HCV RNA levels, often by 2-4 log units, with good tolerability.
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| Cell Assay |
Assay: In vitro RNA-dependent RNA polymerase (NS5B) inhibition assay. Protocol: Recombinant HCV NS5B polymerase is incubated with RNA template, NTP substrates, and varying concentrations of Nucleoside-Analog-2 (as the 5'-triphosphate form). RNA product formation is quantified via incorporation of radiolabeled NTPs (3H-UTP) or by fluorescence-based detection. The IC50 is determined as the concentration inhibiting 50% of polymerase activity.
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| Animal Protocol |
No specific in vivo protocol found; please refer to general nucleoside analog protocols: For efficacy studies in HCV mouse models, the compound is formulated in PBS or appropriate vehicle (e.g., 10% DMSO, 40% PEG300, 5% Tween-80, 45% saline) and administered orally (PO) or intraperitoneally (IP) at doses of 10-100 mg/kg once or twice daily. Blood and liver tissue are collected for PK analysis and HCV RNA quantification.
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| ADME/Pharmacokinetics |
No specific data found; please refer to general nucleoside analog properties: Nucleoside analogs generally exhibit good oral bioavailability (30-80%) due to nucleoside transporters. Active uptake into the liver via organic anion transporting polypeptides (OATPs) is common. The compound is metabolically activated through intracellular phosphorylation to the 5'-triphosphate active form.
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| Toxicity/Toxicokinetics |
No specific data found; please refer to general nucleoside analog properties: Mitochondrial toxicity is a known concern for some nucleoside analogs and is typically assessed via measurement of lactate levels and mtDNA content in treated cells. Bone marrow suppression and gastrointestinal disturbances are also potential class effects, but vary significantly between compounds based on structure.
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| References | |
| Additional Infomation |
Nucleoside-Analog-2 is also classified as a click chemistry reagent due to its azide moiety, which can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with alkyne-containing molecules. This dual functionality allows for potential use in probe labeling and drug delivery applications. The compound is not FDA-approved and is for research use only.
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| Molecular Formula |
C9H11N5O6
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|---|---|
| Molecular Weight |
285.213541269302
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| Exact Mass |
285.07
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| CAS # |
876708-01-9
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| PubChem CID |
25185460
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| Appearance |
Light brown to gray solid powder
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| LogP |
-1.5
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
517
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| Defined Atom Stereocenter Count |
4
|
| SMILES |
N([C@]1([C@@H](O)[C@H](O)[C@H](N2C=CC(=O)NC2=O)O1)CO)=[N+]=[N-]
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| InChi Key |
FHPJZSIIXUQGQE-XZMZPDFPSA-N
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| InChi Code |
InChI=1S/C9H11N5O6/c10-13-12-9(3-15)6(18)5(17)7(20-9)14-2-1-4(16)11-8(14)19/h1-2,5-7,15,17-18H,3H2,(H,11,16,19)/t5-,6-,7+,9+/m0/s1
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| Chemical Name |
1-[(2R,3S,4S,5R)-5-azido-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione
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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 (116.86 mM)
H2O : 20 mg/mL (70.12 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.77 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
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 (8.77 mM) 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; with ultrasonication. 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 (8.77 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Solubility in Formulation 4: 16.67 mg/mL (58.45 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.5062 mL | 17.5309 mL | 35.0619 mL | |
| 5 mM | 0.7012 mL | 3.5062 mL | 7.0124 mL | |
| 10 mM | 0.3506 mL | 1.7531 mL | 3.5062 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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