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Censavudine

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Catalog No. T30791Cas No. 634907-30-5
Alias OBP-601, OBP601, OBP 601, BMS-986001, BMS986001, BMS 986001

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.

Censavudine

Censavudine

😃Good
Catalog No. T30791Alias OBP-601, OBP601, OBP 601, BMS-986001, BMS986001, BMS 986001Cas No. 634907-30-5
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.
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25 mg$1,960Backorder
50 mg$2,550Backorder
100 mg$3,990Backorder
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Product Introduction

Bioactivity
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].
AliasOBP-601, OBP601, OBP 601, BMS-986001, BMS986001, BMS 986001
Chemical Properties
Molecular Weight248.23
FormulaC12H12N2O4
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 & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM4.0285 mL20.1426 mL40.2852 mL201.4261 mL
5 mM0.8057 mL4.0285 mL8.0570 mL40.2852 mL
10 mM0.4029 mL2.0143 mL4.0285 mL20.1426 mL
20 mM0.2014 mL1.0071 mL2.0143 mL10.0713 mL
DMSO
1mg5mg10mg50mg
50 mM0.0806 mL0.4029 mL0.8057 mL4.0285 mL
100 mM0.0403 mL0.2014 mL0.4029 mL2.0143 mL

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