生物活性 | |||
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描述 | The hepatitis B virus (HBV) is a non-cytopathic, small DNA virus of the Hepadnaviridae family with eight known HBV genotypes categorized from A to H based on sequence diversity. Ab-423, a SBA (sulfamoylbenzamide) class of HBV capsid assembly inhibitor, has inhibitory effect on HBV replication with EC50 of 0.08-0.27 μM and EC90 of 0.33-1.32 μM in living cells. AB-423 showed inhibition of rcDNA production in a concentration dependent manner in several different cell culture models of HBV. Specificly, the antiviral activity of AB-423 was comparable in the AML12-HBV10 and HepDE19 cell culture systems with EC50 values of ~0.26 μM. Treatment of HepDES19 cells with 3 μM AB-423 for 6 days showed a strong inhibition of capsid associated RNA and DNA in comparison to untreated control cells indicating that AB-423 inhibited HBV replication at the step of pgRNA encapsidation. In a biochemical assay, AB-423 accelerated capsid assembly in a dose-responsive manner with an IC50 of 2.9 μM. In vivo, AB-423 (30 or 100 mg/kg; p.o.) blocked HBV replication in a mouse model of HBV[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.59mL 0.52mL 0.26mL |
12.94mL 2.59mL 1.29mL |
25.88mL 5.18mL 2.59mL |
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