Censavudine (OBP-601; BMS-986001), a nucleoside analog , is a nucleoside reverse transcriptase inhibitor. Censavudine is a potent HIV inhibitor with EC 50 ranges from 30 nM to 81 nM and 450 nM to 890 nM for HIV-2 and HIV-1 , respectively In Vitro BMS-986001 shows greater activity against HIV-2 ROD9 than against HIV-1 NL4-3 ; the mean EC 50 s for BMS-986001 are 74 nM for HIV-2 ROD9 and 890 nM for HIV-1 NL4-3 in the single-cycle assay. HIV-2 ROD9 also showes greater sensitivity to BMS-986001 in 4-day infections of an immortalized T cell line (CEMss), with the mean EC 50 for HIV-2 ROD9 (EC 50 of 0.14 nM) being 30-fold lower than that for HIV-1 NL4-3 (EC 50 of 4.2 nM). BMS-986001 also exhibits full activity against HIV-2 variants whose genomes encoded the single amino acid changes K65R and Q151M in reverse transcriptase. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo The pharmacokinetic parameters of Censavudine (BMS-986001; 100-750 mg/kg) generated from the dried blood spot (DBS) assay and the plasma assay is compared. The ratios of the AUC (0-24 h) and C max for BMS-986001 in DBS compared to those in plasma are consistent at 0.83-0.91 and 0.81-0.97, respectively, across all dose groups in rats. The T max in rat DBS and plasma are also consistent at about 1 h. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:HIV-2 30-81 nM (EC 50 ) HIV-1 450-890 nM (IC 50 )
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Censavudine
CAS number：634907-30-5 molecular formula：C12H12N2O4
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| Chinese alias | 塞沙夫定 | ||
| English alias | Censavudine | 4'-ethynyl stavudine | Censavudine (USAN) | 4'-Ethynyl D4T | OSYWBJSVKUFFSU-SKDRFNHKSA-N | UNII-6IE83O6NGA | BMS-986001 | CHEMBL124363 | 1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2,5-dihydrofuran-2-yl]-5-methylpyrimidine-2,4(1H,3H)-dione | THYM | ||
| CAS number | 634907-30-5 | molecular formula | C12H12N2O4 |
| molecular weight | 248.23 g/mol | Exact mass | ≥98% |
| PSA | 78.900 Ų | logp | -0.7 |
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