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Ombitasvir

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Chemical Structure| 1258226-87-7 同义名 : 奥比他韦（ABT-267） ;ABT-267
CAS号 : 1258226-87-7
货号 : A155966
分子式 : C50H67N7O8
纯度 : 98%
分子量 : 894.109
MDL号 : MFCD28386270
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(39.15 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 Hepatitis C virus (HCV) is an enveloped, single-stranded, positive-sense RNA virus in the Flaviviridae family. Ombitasvir is a HCV NS5A inhibitor with pan-genotypic activity. Ombitasvir had EC50s of 14.1 and 5.0 pM against genotype 1a-H77 and 1b-Con1 sub-genomic replicons, respectively. It demonstrated broad genotypic activity, with EC50s of 0.82 to 19.3 pM against genotype 2a, 2b, 3a, 4a, and 5a replicons and 366 pM against a genotype 6a replicon. Among a panel of HCV genotype 1 to 6 isolates, the EC50 of ombitasvir ranged from 0.1 to15.1 pM against NS5A from 66 genotype 1 to 5 isolates. In addition, ombitasvir was active against the genotype 2a JFH-1 replicon, with an EC50 of 0.82 pM. In a 3-day monotherapy study (5, 25, 50, or 200 mg; once daily) in 12 HCV genotype 1-infected patients, decreases in HCV RNA up to 3.1 log10 IU/ml were observed. And wild-type virus was largely suppressed by ombitasvir during 3-day monotherapy, and at doses higher than 5 mg, resistant variant M28V was also suppressed[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.12mL

0.22mL

0.11mL

5.59mL

1.12mL

0.56mL

11.18mL

2.24mL

1.12mL
参考文献

[1]Krishnan P, Beyer J, et al. In vitro and in vivo antiviral activity and resistance profile of ombitasvir, an inhibitor of hepatitis C virus NS5A. Antimicrob Agents Chemother. 2015 Feb;59(2):979-87.

[2]DeGoey DA, Randolph JT, et al. Discovery of ABT-267, a pan-genotypic inhibitor of HCV NS5A. J Med Chem. 2014 Mar 13;57(5):2047-57.

[3]Krishnan P, Beyer J, Mistry N, Koev G, Reisch T, DeGoey D, Kati W, Campbell A, Williams L, Xie W, Setze C, Molla A, Collins C, Pilot-Matias T. In vitro and in vivo antiviral activity and resistance profile of ombitasvir, an inhibitor of hepatitis C virus NS5A. Antimicrob Agents Chemother. 2015 Feb;59(2):979-87