| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
The primary target of Censavudine is the HIV reverse transcriptase enzyme, which is essential for the replication of the HIV virus. As a nucleoside reverse transcriptase inhibitor (NRTI), Censavudine is a nucleoside analog that is incorporated into the growing viral DNA chain during reverse transcription. This incorporation terminates DNA chain elongation, thereby blocking viral replication. Censavudine is active against HIV-1 and HIV-2 and is effective against HIV strains resistant to abacavir and tenofovir.
|
|---|---|
| ln Vitro |
In single-cycle experiments, BMS-986001's average EC50 was 74 nM for HIV-2ROD9 and 890 nM for HIV-1NL4-3, indicating that it is more potent against HIV-2ROD9 than HIV-1NL4-3. In a 4-day infection of immortalized T cell lines (CEMss), HIV-2ROD9 also shown increased sensitivity to BMS-986001; the average EC50 of HIV-2ROD9 (EC50 of 0.14 nM) was 30-fold lower than that of HIV 1NL4-3 (EC50 of 4.2 nM) [1]. BMS-986001 demonstrates complete efficacy against HIV-2 strains that have single amino acid alterations encoded in their reverse transcriptases, K65R and Q151M [1].
Censavudine demonstrates in vitro antiviral activity against HIV-1 and HIV-2. It is active against HIV strains resistant to both abacavir and tenofovir. However, detailed IC50 or EC50 values for antiviral activity are not extensively reported in the available literature. The compound's mechanism of action as an NRTI is well-established based on its structural similarity to other nucleoside analogs. |
| ln Vivo |
Pharmacokinetic characteristics of sensavudine (BMS-986001; 100-750 mg/kg) derived from dried blood spot (DBS) assays and plasma assays were compared. Across all dose groups in rats, the AUC(0-24 h) and C max of BMS-986001 in DBS were consistent with the ratios in plasma, 0.83-0.91 and 0.81-0.97, respectively. The T max in rat DBS and plasma is also constant at roughly 1 hour [2].
Censavudine has been used in trials studying the treatment of HIV-1 infection. It is a candidate for people with multi-drug resistant (MDR) strains of the virus. However, specific in vivo efficacy data, including clinical trial results, are not extensively detailed in the available literature. The compound has been evaluated in clinical trials for HIV treatment. |
| Enzyme Assay |
In vitro enzyme assays for Censavudine typically involve measuring its inhibition of HIV reverse transcriptase activity. Recombinant HIV reverse transcriptase enzyme is incubated with a template-primer and nucleotide substrates in the presence of varying concentrations of Censavudine. The incorporation of radiolabeled nucleotides into the growing DNA strand is measured to determine the enzyme activity. The IC50 for inhibition is calculated from the dose-response curve.
|
| Cell Assay |
Cellular assays for Censavudine are performed in HIV-susceptible cell lines, such as MT-4 or CEM cells. Cells are infected with HIV-1 or HIV-2 and treated with various concentrations of Censavudine. After several days of culture, viral replication is measured by quantifying viral antigens (e.g., p24 for HIV-1) in the culture supernatant or by assessing the cytopathic effect of the virus on the cells. The compound's antiviral activity is expressed as the EC50.
|
| Animal Protocol |
In vivo animal studies with Censavudine are not extensively documented in the available literature. As an NRTI developed for HIV treatment, the compound would have been evaluated in animal models of HIV infection, such as humanized mouse models or non-human primate models. However, specific protocols and results are not detailed in the available sources. The compound has been evaluated in clinical trials.
|
| ADME/Pharmacokinetics |
Censavudine has a molecular weight of 248.23 and a molecular formula of C12H12N2O4. It is a nucleoside analog that is soluble in DMSO and other organic solvents. The compound is stable when stored at -20°C. However, detailed pharmacokinetic parameters such as absorption, distribution, metabolism, excretion, half-life, and bioavailability are not extensively reported in the available literature.
|
| Toxicity/Toxicokinetics |
Comprehensive toxicology data for Censavudine are not extensively reported. As a compound that has been evaluated in clinical trials, it would have undergone toxicological evaluation, but specific data are not detailed in the available literature. The compound is classified as a research-use-only chemical and is not intended for human consumption.
|
| References |
|
| Additional Infomation |
Sensavudine has been used in clinical trials to investigate the treatment of HIV-1 infection.
Drug Indications Treatment of Eckhardy-Gutier syndrome Censavudine is a research-grade compound that has been evaluated in clinical trials for the treatment of HIV-1 infection. It is a nucleoside reverse transcriptase inhibitor (NRTI) that is active against HIV-1 and HIV-2. Censavudine is active against HIV strains resistant to both abacavir and tenofovir, making it a candidate for people with multi-drug resistant (MDR) strains of the virus. It is not approved for clinical use. |
| Molecular Formula |
C12H12N2O4
|
|---|---|
| Molecular Weight |
248.2347
|
| Exact Mass |
248.08
|
| CAS # |
634907-30-5
|
| Related CAS # |
(2S,5S)-Censavudine
|
| PubChem CID |
3008897
|
| Appearance |
Light yellow to yellow solid powder
|
| LogP |
-0.7
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
18
|
| Complexity |
513
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
O1[C@](C#C[H])(C([H])([H])O[H])C([H])=C([H])[C@]1([H])N1C(N([H])C(C(C([H])([H])[H])=C1[H])=O)=O
|
| InChi Key |
OSYWBJSVKUFFSU-SKDRFNHKSA-N
|
| InChi Code |
InChI=1S/C12H12N2O4/c1-3-12(7-15)5-4-9(18-12)14-6-8(2)10(16)13-11(14)17/h1,4-6,9,15H,7H2,2H3,(H,13,16,17)/t9-,12+/m1/s1
|
| Chemical Name |
1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2H-furan-2-yl]-5-methylpyrimidine-2,4-dione
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~52 mg/mL (~209.48 mM)
H2O : ~10 mg/mL (~40.29 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.83 mg/mL (11.40 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 28.3 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: ≥ 2.83 mg/mL (11.40 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 28.3 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. (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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05613868 | RECRUITING | Drug: TPN-101 | Aicardi-Goutières Syndrome (AGS) | Transposon Therapeutics, Inc. | 2023-03-15 | Phase 2 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
