IDX184

• CAT Number: I007266
• CAS Number: 1036915-08-8
• Molecular Formula: C25H35N6O9PS
• Molecular Weight: 626.62
• Purity: ≥95%
• Synonyms: S-[2-[[(2R,3R,4R,5R)-5-(2-amino-6-oxo-1H-purin-9-yl)-3,4-dihydroxy-4-methyloxolan-2-yl]methoxy-(benzylamino)phosphoryl]oxyethyl] 3-hydroxy-2,2-dimethylpropanethioate
• InChI: InChI=1S/C25H35N6O9PS/c1-24(2,13-32)22(35)42-10-9-38-41(37,28-11-15-7-5-4-6-8-15)39-12-16-18(33)25(3,36)21(40-16)31-14-27-17-19(31)29-23(26)30-20(17)34/h4-8,14,16,18,21,32-33,36H,9-13H2,1-3H3,(H,28,37)(H3,26,29,30,34)/t16-,18-,21-,25-,41?/m1/s1
• InChIKey: FGHMGRXAHIXTBM-TWFJNEQDSA-N
• SMILES: CC1(C(C(OC1N2C=NC3=C2N=C(NC3=O)N)COP(=O)(NCC4=CC=CC=C4)OCCSC(=O)C(C)(C)CO)O)O

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].
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].

Reference

[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.
 [Content Brief]

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