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Censavudine (OBP-601) is a nucleoside analog, a nucleoside reverse transcriptase inhibitor, used for the prevention and treatment of human immunodeficiency virus 1 (HIV-1).Censavudine inhibits HIV-2 and HIV-1. Censavudine inhibits HIV-2 and HIV-1 with EC50 ranges of 30-81 nM and 450-890 nM, respectively.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,960 | Backorder | |
50 mg | $2,550 | Backorder | |
100 mg | $3,990 | Backorder |
Description | Censavudine (OBP-601) is a nucleoside analog, a nucleoside reverse transcriptase inhibitor, used for the prevention and treatment of human immunodeficiency virus 1 (HIV-1).Censavudine inhibits HIV-2 and HIV-1. Censavudine inhibits HIV-2 and HIV-1 with EC50 ranges of 30-81 nM and 450-890 nM, respectively. |
Targets&IC50 | HIV-1NL4-3:890 nM(EC50), HIV-2 (ROD9):74 nM(EC50), HIV-1:450-890 nM, HIV-2:30-81 nM (EC50) |
In vitro | In a single-cycle assay, BMS-986001 demonstrates greater activity against HIV-2ROD9 compared to HIV-1NL4-3. The mean EC50s for BMS-986001 are 74 nM for HIV-2ROD9 and 890 nM for HIV-1NL4-3. In a 4-day infection of an immortalized T cell line (CEMss), HIV-2ROD9 exhibits greater sensitivity to BMS-986001, with a mean EC50 of 0.14 nM, which is 30-fold lower than the EC50 for HIV-1NL4-3 (4.2 nM)[2]. Furthermore, BMS-986001 maintains full activity against HIV-2 variants with genomes encoding the single amino acid changes K65R and Q151M in reverse transcriptase[2]. |
In vivo | Comparing the pharmacokinetic parameters of Censavudine (BMS-986001) at doses ranging from 100 to 750 mg/kg, the dried blood spot (DBS) assay and plasma assay are utilized. Across all dose groups in rats, the ratios of AUC(0-24 h) and Cmax for BMS-986001 in DBS compared to plasma remain consistent at 0.83-0.91 and 0.81-0.97, respectively. The Tmax in rat DBS and plasma also consistently occurs at about 1 h[1]. |
Alias | OBP-601, OBP601, OBP 601, BMS-986001, BMS986001, BMS 986001 |
Molecular Weight | 248.23 |
Formula | C12H12N2O4 |
Cas No. | 634907-30-5 |
Smiles | [H][C@]1(O[C@](CO)(C=C1)C#C)n1cc(C)c(=O)[nH]c1=O |
Relative Density. | 1.42 g/cm3 (Predicted) |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 5 mg/mL (20.14 mM), Sonication is recommended. DMSO: 45 mg/mL (181.28 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/DMSO
DMSO
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