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Letermovir

CAS No. : 917389-32-3

MCE 国际站：Letermovir

产品活性：Letermovir (AIC246) 是一种有效的 CMV 抑制剂，以病毒末端酶为靶目标，抑制其活性。

研究领域：Anti-infection

作用靶点：CMV

In Vitro: AIC246 has consistent antiviral efficacy, and there is remarkable selectivity of AIC246 for human cytomegaloviruses. AD169 mutant strains and designated rAIC246-1 and rAIC246-2 are highly resistant to Letermovir (AIC246), with EC₅₀s of 5.6 nM, 1.24 μM, 0.37 μM, respectively. Letermovir inhibits HCMV replication through a specific antiviral mechanism that involves the viral gene product UL56. Letermovir inhibits HCMV replication in cell culture by interfering with the proper cleavage/packaging of HCMV progeny DNA. Letermovir inhibits the current gold standard GCV by more than 400-fold with respect to EC₅₀s (mean, 4.5 nM versus 2 μM) and by more than 2,000-fold with respect to EC₉₀ values (mean, 6.1 nM versus 14.5 μM). Letermovir in conbination with anti-HCMV drugs causes additive antiviral effects, but there is no interaction between letermovir and anti-HIV drugs.

In Vivo: Letermovir (10-100 mg/kg/day, p.o.) leads to a dose-dependent reduction of the HCMV titer in transplanted cells compared to that of the placebo-treated control group using the mouse xenograft model.

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