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Letermovir

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Chemical Structure| 917389-32-3 同义名 : 莱特莫韦 ;AIC246;MK-8228;Prevymis;MK-8828
CAS号 : 917389-32-3
货号 : A236700
分子式 : C29H28F4N4O4
纯度 : 99%+
分子量 : 572.551
MDL号 : MFCD22572725
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(183.39 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 HCMV (human cytomegalovirus) infection has remained a significant complication during pregnancy and in clinical situations associated with inefficient immunocompetence, such as organ or bone marrow transplantation, cancer, and AIDS. Letermovir inhibits HCMV laboratory strains, clinical isolates, and virus variants resistant to approved drugs with 50% effective concentrations (EC50s) in the low nanomolar range[3]. AIC246 (∼10× the EC50) exerted a marked inhibitory effect on the de novo synthesis of progeny HCMV DNA. AIC246 inhibited the formation of the ∼4-kb terminal fragment in a concentration-dependent manner, indicating that the drug allowed the accumulation of viral concatemeric DNA while further maturation to mature unit-length genomes was prevented. Importantly, C capsids (and consequently C capsid-derived A capsids) were markedly reduced after AIC246 treatment[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.75mL

0.35mL

0.17mL

8.73mL

1.75mL

0.87mL

17.47mL

3.49mL

1.75mL
参考文献

[1]Marschall M, Stamminger T, et al. In vitro evaluation of the activities of the novel anticytomegalovirus compound AIC246 (letermovir) against herpesviruses and other human pathogenic viruses. Antimicrob Agents Chemother. 2012 Feb;56(2):1135-7.

[2]Goldner T, Hewlett G, et al. The novel anticytomegalovirus compound AIC246 (Letermovir) inhibits human cytomegalovirus replication through a specific antiviral mechanism that involves the viral terminase. J Virol. 2011 Oct;85(20):10884-93.

[3]Marschall M, Stamminger T, Urban A, et al. In vitro evaluation of the activities of the novel anticytomegalovirus compound AIC246 (letermovir) against herpesviruses and other human pathogenic viruses. Antimicrob Agents Chemother. 2012;56(2):1135‐1137

[4]Goldner T, Hewlett G, Ettischer N, Ruebsamen-Schaeff H, Zimmermann H, Lischka P. The novel anticytomegalovirus compound AIC246 (Letermovir) inhibits human cytomegalovirus replication through a specific antiviral mechanism that involves the viral terminase. J Virol. 2011;85(20):10884‐10893