GS588 Inhibitor CAS No. 1256388-51-8

Cat. No.	Name	Size	Price	Add Cart
KI3663	GS588	5 mg	$370

Chemical Characteristic

Product Name	GS588
Synonyms	Ledipasvir
CAS No.	1256388-51-8
Molecular Weight	889
Formula	C₄₉H₅₄F₂N₈O₆
Chemical Name	N-[(1S)-1-[[(6S)-6-[5-[9,9-difluoro-7-[2-[(1R,3S,4S)-2-[(2S)-2-[(methoxycarbonyl)amino]-3-methyl-1-oxobutyl]-2-azabicyclo[2.2.1]hept-3-yl]-1H-benzimidazol-6-yl]-9H-fluoren-2-yl]-1H-imidazol-2-yl]-5-azaspiro[2.4]hept-5-yl]carbonyl]-2-methylpropyl]-carbamic
Smiles	C(=O)(NC(C(C)C)C(=O)N1CC2(CC2)C[C@H]1c1ncc([nH]1)c1cc2C(c3c(c2cc1)ccc(c3)c1ccc2nc([nH]c2c1)C1N([C@@H]2CC[C@H]1C2)C(=O)[C@H](C(C)C)NC(=O)OC)(F)F)OC
Chemical Structure

Biological activities

Ledipasvir (formerly GS-5885) is an experimental drug for the treatment of hepatitis C and it is an inhibitor of the hepatitis C virus NS5A protein ^[1]. The ledipasvir/sofosbuvir combination is a direct-acting antiviral agent that interferes with HCV replication and can be used to treat patients with genotypes 1a or 1b without PEG-interferon. In vitro, the IC50 of ledipasvir to NS5A is 141nM ^[2]. In vivo, GS-5885 was well tolerated and resulted in median maximal reductions in HCV RNA ranging from 2.3 log(10) IU/ml (1 mg QD) to 3.3 log(10) IU/ml (10 mg QD in genotype 1b and 30 mg QD) ^[3].

References

[1] Hernandez D, Zhou N, Ueland J , et al. Natural prevalence of NS5A polymorphisms in subjects infected with hepatitis C virus genotype 3 and their effects on the antiviral activity of NS5A inhibitors. J Clin Virol. 2013, 57(1):13-18. [2] Lawitz EJ, Gruener D, Hill JM, et al. A phase 1, randomized, placebo-controlled, 3-day, dose-ranging study of GS-5885, an NS5A inhibitor, in patients with genotype 1 hepatitis C. J Hepatol. 2012, 57(1):24-31. [3] Afdhal N, Zeuzem S, Kwo P, et al. Ledipasvir and sofosbuvir for previously treated HCV genotype 1 infection. N Engl J Med. 2014, 370(16):1483-1493.

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