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MCE 国际站：Delavirdine

产品活性：Delavirdine (U 90152) 是一种有效的口服活性非核苷逆转录酶抑制剂 (NNRTI)。Delavirdine 选择性地抑制 HIV-1 逆转录酶 (HIV-1 RT) (IC₅₀=0.26 μM)，选择性超过 DNA 聚合酶 α (IC₅₀=440 μM) 和 DNA 聚合酶 δ (IC₅₀>550 μM)。Delavirdine 是HIV-1 病毒复制的抑制剂，可以用于艾滋病的相关研究。

研究领域：Anti-infection

作用靶点：HIV | Reverse Transcriptase

In Vitro: Delavirdine has an 50% cytotoxicity at concentrations >100 μM in H9 and PBMC cultures.Delavirdine has low cellular cytotoxicity, causing less than 8% reduction in peripheral blood lymphocyte viability at 100 μM.
Delavirdine inhibits HIV-1 reverse transcriptase (RT) wild type with an IC₅₀ value of 0.26 μM, and it inhibits Y181C-substituted RT and K103N-substituted RT with IC₅₀ values of 8.32 uM and 7.7 uM, respectively.

In Vivo: Delavirdine (U 90152) (oral gavage; 10 mg/kg, 200 mg/kg, 250 mg/kg; single dose) is absorbed and metabolized rapidly, that it constitutes a minor component in circulation, that its pharmacokinetics are nonlinear, and that its metabolism to desalkyl delavirdine is capacity limited or inhibitable in CD-1 mice (PK study).