Letermovir

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Letermovir (AIC246) 是一种新型抗 CMV 化合物（EC50：在成纤维细胞中约为 5 nM）。它针对病毒终止酶复合物的 pUL56 亚基。

Letermovir (AIC246) is a novel anti-CMV compound (EC50: about 5 nM in fibroblast cells). It targets the pUL56 subunit of the viral terminase complex.(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.

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.

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.

AIC246 | MK-8828

Microbiology/Virology

HCV

HCMV

Others

Cytomegalovirus infections

917389-32-3

572.55

C29H28F4N4O4

>98% (HPLC)

DMSO:70 mg/mL (122.26 mM);Ethanol:2 mg/mL

COc1cccc(c1)N1CCN(CC1)C1=Nc2c(F)cccc2[C@H](CC(O)=O)N1c1cc(ccc1OC)C(F)(F)F

(S)-2-(8-fluoro-3-(2-methoxy-5-(trifluoromethyl)phenyl)-2-(4-(3-methoxyphenyl)piperazin-1-yl)-34-dihydroquinazolin-4-yl)acetic acid

(-20℃)

With Ice Pack

≥ 2 years