Tegobuvir | CAS:1000787-75-6

Chemscene社は、高品質な低分子化合物を提供しているメーカーです。
Chemscene社のTegobuvir(CAS:1000787-75-6)をご紹介します。

※本製品は研究用です。研究用以外には使用できません。

Name:Tegobuvir; GS 333126; GS-9190
Cat. No. :CS-0672
CAS No. :1000787-75-6
Formula:C25H14F7N5
M. Wt. : 517.40
Solubility:10 mM in DMSO

Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase.In Vitro: Tegobuvir rapidly increases the proportion of replicons with the Y448H mutation in a dose-dependent manner. After 3 days of treatment, 1.2%, 6.8%, and > 50% of the replicon population expresses Y448H with the use of Tegobuvir at 1, 10, and 20 times its 50% effective concentration, respectively[1]. Tegobuvir exerts anti-HCV activity utilizing a unique chemical activation and subsequent direct interaction with the NS5B protein. Treatment of HCV subgenomic replicon cells with Tegobuvir results in a modified form of NS5B with a distinctly altered mobility on a SDS-PAGE gel[2]. Tegobuvir is potent in GT1a and 1b with mean EC50s of 19.8 and 1.5 nM respectively. For genotype 3a, 4a, and 6a Con chimeras, tegobuvir EC50s are all greater than 100 nM. The F445C NS5B mutations in GT3a, 4a, and 6a chimeric replicons restore tegobuvir potency to EC50 levels comparable to GT1a[3].

Bae AS, et al. Allele-specific real-time PCR system for detection of subpopulations of genotype 1a and 1b hepatitis C NS5B Y448H mutant viruses in clinical samples. J Clin Microbiol. 2011 Sep;49(9):3168-74. Hebner CM, et al. The HCV non-nucleoside inhibitor Tegobuvir utilizes a novel mechanism of action to inhibit NS5B polymerase function.PLoS One. 2012;7(6):e39163. Wong KA, et al. Tegobuvir (GS-9190) potency against HCV chimeric replicons derived from consensus NS5B sequences from genotypes 2b, 3a, 4a, 5a, and 6a. Virology. 2012 Jul 20;429(1):57-62.