产品
编 号:F751070
分子式:C24H19ClFN5O3
分子量:479.89
产品类型
结构图
CAS No: 2305897-84-9
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产品详情
生物活性:
HBV-IN-4, a phthalazinone derivative, is a potent and orally active HBV DNA replication inhibitor with an IC50 of 14 nM. HBV-IN-4 induces the formation of genome-free capsids and has potent anti-HBV potencies.
体内研究:
HBV-IN-4 (Compound 19f; 50-150 mg/kg; oral administration; twice a day; for 4 weeks; Balb/c male mice) treatment achieves 2.67 log viral load reduction in AAV-HBV/mouse model.HBV-IN-4 (compound 19f) exhibits favorable drug characteristics with low plasma clearance (CL=4.1 mL/min/kg), excellent drug exposure (AUC0-t=49 744 h?ng/L), T1/2 (2.15 hours) and oral bioavailability (F=60.4%) using 20 mg/kg oral administration in mice. HBV-IN-4 also shows good distribution in liver exposure.Animal Model:Balb/c male mice (8-week-old) injected with a recombinant adenoassociated virus (AAV
Dosage:50 mg/kg, 150 mg/kg
Administration:Oral administration; twice a day; for 4 weeks
Result:Resulted in a 2.67 log reduction of the HBV DNA viral load during a 4-week treatment.
体外研究:
HBV-IN-4 (compound 19f; 0-1 μM; 8 days) treatment inhibits the various forms (relaxed circular [rc] and single-stranded [ss] HBV DNA) in a dose-dependent manner in HepG2.2.15 cells. HBV-IN-4 treatment could also reduce capsidassociated DNAs dose-dependently. HBV-IN-4 could induce the formation of genome-free capsids, including a phenotype of faster-migrating ones.