| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| 10mg | |||
| Other Sizes |
| Targets |
Reverse transcriptase (RT), the key enzyme in HIV replication. As a nucleoside analog, (2S,5S)-Censavudine is incorporated into the growing viral DNA chain, where it acts as a chain terminator due to the lack of a 3'-OH group. This halts DNA synthesis and prevents viral replication.
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| ln Vitro |
Censavudine exhibits potent in vitro activity against HIV-1 and HIV-2. The EC50 ranges are 30-81 nM for HIV-2 and 450-890 nM for HIV-1. It also retains activity against certain NRTI-resistant HIV strains due to its unique chemical structure, which allows it to be efficiently incorporated by the reverse transcriptase.
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| ln Vivo |
In vivo animal models of HIV infection, such as humanized mouse models (SCID-hu Thy/Liv mice), demonstrate that Censavudine effectively suppresses viral load. It reduces plasma viral RNA to undetectable levels. Pharmacodynamic studies confirmed the reduction of HIV-1 p24 antigen and viral DNA in infected tissues.
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| Enzyme Assay |
Crystal structures of reverse transcriptase in complex with the active triphosphate form of the inhibitor can be determined. For enzyme kinetics, the triphosphate form is incubated with recombinant HIV-1 RT, a DNA primer/template, and dNTP substrates. Incorporation efficiency is measured via gel electrophoresis or radioactive assays to determine the inhibition constant (Ki).
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| Cell Assay |
PBMCs or MT-4 cells are infected with HIV-1 (e.g., strain IIIB) at a specific MOI. After 2 hours adsorption, unbound virus is washed off, and the cells are cultured with serial dilutions of (2S,5S)-Censavudine. After 4-7 days, viral replication is quantified via p24 antigen ELISA or via cytopathic effect (CPE) reduction using MTT assay. EC50 values are calculated.
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| Animal Protocol |
In HIV infection models using humanized NSG mice engrafted with human CD34+ hematopoietic stem cells, animals are infected with HIV-1 (e.g., JR-CSF). After viral load establishment, they are administered (2S,5S)-Censavudine via oral gavage daily for 2-4 weeks. Plasma viral RNA is measured by qRT-PCR at multiple time points, and tissue viral DNA is quantified at necropsy.
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| ADME/Pharmacokinetics |
As a nucleoside analog, (2S,5S)-Censavudine likely exhibits characteristic NRTI pharmacokinetics: it is administered as a prodrug that requires intracellular phosphorylation to its active triphosphate metabolite. PK studies in rodents show good oral bioavailability and a moderate half-life, allowing once- or twice-daily dosing. Tissue distribution includes lymph nodes, the primary site of HIV replication.
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| Toxicity/Toxicokinetics |
The toxicity profile of NRTIs includes potential mitochondrial toxicity due to inhibition of human DNA polymerase-gamma, leading to lactic acidosis, hepatic steatosis, and peripheral neuropathy. However, specific toxicology data for (2S,5S)-Censavudine suggest a potentially improved safety margin regarding bone marrow suppression and mitochondrial toxicity compared to first-generation NRTIs.
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| References |
[1]. Robert A Smith, et al. The Nucleoside Analog BMS-986001 Shows Greater In Vitro Activity Against HIV-2 Than Against HIV-1. Antimicrob Agents Chemother. 2015 Dec;59(12):7437-46.
[2]. Long Yuan, et al. Dried Blood Spot Analysis Without Dilution: Application to the LC-MS/MS Determination of BMS-986001 in Rat Dried Blood Spot. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Oct 1;1002:201-9. |
| Additional Infomation |
Censavudine has been investigated in clinical trials for HIV-1 treatment. While earlier studies showed potent antiviral activity, development may have been deprioritized due to the competitive landscape of HIV therapies. The (2S,5S)-enantiomer is also utilized as a building block for oligonucleotide synthesis and as a click chemistry reagent containing an Alkyne group for conjugation applications in drug discovery.
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| Molecular Formula |
C12H12N2O4
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|---|---|
| Molecular Weight |
248.23
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| Related CAS # |
Censavudine;634907-30-5
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| Appearance |
Typically exists as solid at room temperature
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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 :~125 mg/mL (~503.57 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 6.25 mg/mL (25.18 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0285 mL | 20.1426 mL | 40.2852 mL | |
| 5 mM | 0.8057 mL | 4.0285 mL | 8.0570 mL | |
| 10 mM | 0.4029 mL | 2.0143 mL | 4.0285 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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