HCV-IN-7 hydrochloride is an orally active and potent pan-genotypic HCV NS5A inhibitor [IC50s: 3-47 pM], exhibiting a superior pan-genotypic profile, a good pharmacokinetic profile, and favorable liver uptake.

HCV NS5A:3-47 pM

HCV-IN-7 hydrochloride (10 μM) has cytotoxicity of 14%, 22%, 36% in Huh7, HepG2 and HEK cells, respectively. ?HCV-IN-7 hydrochloride has a less complex central tricyclic core as novel and potent pan-genotypic NS5A inhibitors with good pharmacokinetic profile.HCV-IN-7 hydrochloride inhibits GT1b (IC50=12 pM), GT2a (IC50=5 pM), GT1a (IC50=27 pM), GT3a (IC50=47 pM), GT4a (IC50=3 pM), GT6a (IC50=28 pM). ?HCV-IN-7 hydrochloride (10 μM) has 12%, 42%, 12% inhibition for CYP2D6, CYP2C9, CYP3A4, respectively.

HCV-IN-7 hydrochloride (po; 10 mg/kg) has a Cmax of 1 μM and an AUClast of 6 μM for rats. ?HCV-IN-7 hydrochloride (iv; 1 mg/kg) has a T1/2 of 4 hours, CL of 6 mL/min/kg, and a Vss of 2 L/kg for dog. ?HCV-IN-7 hydrochloride (po; 10 mg/kg) has a Cmax of 5 μM and an AUClast of 49 μM for dog.?HCV-IN-7 hydrochloride (iv; 1 mg/kg) has a T1/2 of 2 hours, CL of 11 mL/min/kg, and a Vss of 2 L/kg for rats.