产品
编 号：F689207
分子式：C40H48N8O6S
分子量：768.92
分子式：C40H48N8O6S
分子量：768.92
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CAS No: 1449756-86-8
产品详情
生物活性：
HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity.
体内研究：
HCV-IN-7 (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. HCV-IN-7 (po; 10 mg/kg) has a Cmax of 1 μM and an AUClast of 6 μM for rats. HCV-IN-7 (iv; 1 mg/kg) has a T1/2 of 4 hours, a CL of 6 mL/min/kg, and a Vss of 2 L/kg for dog. HCV-IN-7 (po; 10 mg/kg) has a Cmax of 5 μM and an AUClast of 49 μM for dog.
体外研究：
HCV-IN-7 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 (10 μM) has 12%, 42%, 12% inhibition for CYP2D6, CYP2C9, CYP3A4, respectively. HCV-IN-7 (10 μM) has cytotoxicity of 14%, 22%, 36% in Huh7, HepG2 and HEK cells, respectively. HCV-IN-7 has a less complex central tricyclic core as novel and potent pan-genotypic NS5A inhibitors with good pharmacokinetic profile.
HCV-IN-7 is an orally active and potent pan-genotypic HCV NS5A inhibitor with IC50s of 3-47 pM. HCV-IN-7 shows a superior pan-genotypic profile and a good pharmacokinetic profile coupled with a favorable liver uptake. HCV-IN-7 has anti-viral activity.
体内研究：
HCV-IN-7 (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. HCV-IN-7 (po; 10 mg/kg) has a Cmax of 1 μM and an AUClast of 6 μM for rats. HCV-IN-7 (iv; 1 mg/kg) has a T1/2 of 4 hours, a CL of 6 mL/min/kg, and a Vss of 2 L/kg for dog. HCV-IN-7 (po; 10 mg/kg) has a Cmax of 5 μM and an AUClast of 49 μM for dog.
体外研究：
HCV-IN-7 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 (10 μM) has 12%, 42%, 12% inhibition for CYP2D6, CYP2C9, CYP3A4, respectively. HCV-IN-7 (10 μM) has cytotoxicity of 14%, 22%, 36% in Huh7, HepG2 and HEK cells, respectively. HCV-IN-7 has a less complex central tricyclic core as novel and potent pan-genotypic NS5A inhibitors with good pharmacokinetic profile.
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