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Censavudine

CAS No. : 634907-30-5

MCE 国际站：Censavudine

产品活性：Censavudine (OBP-601; BMS-986001)，一种核苷类似物，是一种核苷逆转录酶 (nucleoside reverse transcriptase) 抑制剂。Censavudine 是一种有效的 HIV 抑制剂，对 HIV-2 和 HIV-1 的 EC₅₀ 范围分别为 30-81 nM 和 450-890 nM。

研究领域：Anti-infection  |  Cell Cycle/DNA Damage

作用靶点：HIV  |  Reverse Transcriptase  |  Nucleoside Antimetabolite/Analog

In Vitro: BMS-986001 shows greater activity against HIV-2_ROD9 than against HIV-1_NL4-3; the mean EC₅₀s 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 EC₅₀ for HIV-2_ROD9 (EC₅₀ of 0.14 nM) being 30-fold lower than that for HIV-1_NL4-3 (EC₅₀ 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.

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.

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