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IDX184

Names

[ CAS No. ]:
1036915-08-8

[ Name ]:
IDX184

[Synonym ]:
5’-O-[(benzylamino)[2-(3-hydroxy-2,2-dimethylpropionylsulfanyl)ethoxy]phosphoryl]-2’-C-methylguanosine
2’-C-methylguanosine-5'-[2-[(3-hydroxy-2,2-dimethyl-1-oxopropyl)thio]ethyl-N-(phenylmethyl)phosphoramidate]
IDX184
2'-C-methylguanosine-5'-[2-[(3-hydroxy-2,2-dimethyl-1-oxopropyl)thio]ethyl-N-benzylphosphoramidate]

Biological Activity

[Description]:

IDX184 is a potent and orally bioavailable inhibitor of HCV replication. IDX184 potently inhibits HCV polymerase (IC50=0.31 μM, Ki=52.3 nM)[1][2].

[Related Catalog]:

Signaling Pathways >> Anti-infection >> HCV
Research Areas >> Infection
Signaling Pathways >> Metabolic Enzyme/Protease >> HCV Protease

[Target]

IC50: 0.31 μM (HCV polymerase)[2] Ki: 52.3 nM (HCV polymerase)[2]


[In Vitro]

IDX184 is a liver-targeted prodrug of the nucleotide 2′-MeG-MP. IDX184 is a liver-targeted nucleotide polymerase inhibitor of hepatitis C virus[1]. IDX184 is a second generation, orally bioavailable nucleotide prodrug designed to provide increased anti-HCV efficacy and safety versus the parent nucleoside. In HCV replicon testing, IDX184 is the most potent inhibitor (EC50=0.3-0.45 μM) compared to any of the 2’ or 4’ modified nucleosides (EC50=4-6 μM) and is also highly inhibitory in the JFH-1 infectious system (EC50=0.06-0.11 μM). IDX184 is not toxic (CC50>100μM) in any tested cell line[2].

[References]

[1]. Xiao-Jian Zhou , et al. Safety and Pharmacokinetics of IDX184, a Liver-Targeted Nucleotide Polymerase Inhibitor of Hepatitis C Virus, in Healthy Subjects. Antimicrob Agents Chemother. 2011 Jan;55(1):76-81.

[2]. IN VITRO ANTIVIRAL ACTIVITY AND PHARMACOLOGY OF IDX184, A NOVEL AND POTENT INHIBITOR OF HCV REPLICATION.

Chemical & Physical Properties

[ Molecular Formula ]:
C25H35N6O9PS

[ Molecular Weight ]:
626.61900

[ Exact Mass ]:
626.19200

[ PSA ]:
259.25000

[ LogP ]:
1.89260

Related Compounds