| Name | Censavudine |
| 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. |
| 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 2 mg/mL (8.06 mM), Sonication is recommended.
H2O : 5 mg/mL (20.14 mM), Sonication is recommended.
DMSO : 45 mg/mL (181.28 mM), Sonication is recommended.
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| Keywords | ReverseTranscriptase | Reverse Transcriptase | Nucleoside reverse transcriptase | HIVProtease | HIV-2 | HIV-1 | HIV Protease | Censavudine |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Emtricitabine | Dolutegravir intermediate-1 | Uridine | Dimethyl fumarate | Lamivudine | Valproic Acid | Vidarabine | (-)-Epigallocatechin Gallate | Decanedioic acid | Dextran sulfate sodium salt (MW 5000) |
| Related Compound Libraries | Bioactive Compound Library | Drug Repurposing Compound Library | Bioactive Compounds Library Max |
United States
