AB-423

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AB-423 是一种新型有效的 II 类 HBV 衣壳抑制剂，可有效抑制 HBV 复制，EC50 为 0.08-0.27 uM，且无明显细胞毒性 (CC50>10 uM)。

AB-423 is a novel potent, class II HBV capsid inhibitor that shows potent inhibition of HBV replication with EC50 of 0.08-0.27 uM, with no significant cytotoxicity (CC50>10 uM); inhibits HBV genotypes A through D and nucleos/tide-resistant variants, causes capsid particles devoid of encapsidated pgRNA and rcDNA in treated HepDES19 cells, prevents the conversion of encapsidated rcDNA to cccDNA presumably by interfering with the capsid uncoating process; dose-dependently reduces serum HBV DNA levels in mouse model of HBV model, shows synergistic antiviral activity combined with entecavir (ETV).HBV Infection Phase 1 Clinical(In Vitro):AB-423 is an inhibitor of HBV capsid assembly. AB-423 shows inhibitory effect on rcDNA production in AML12-HBV10 and HepDE19 cells with EC50s of ～0.260 μM. AB-423 also suppresses cccDNA formation-dependent HBeAg production in the HepBHAe82 assay with an EC50 of 0.267 μM and inhibits HBV DNA levels in culture supernatants of HepG 2.2.15 cells with an EC50 of 0.134 μM. However, AB-423 has no cytotoxicity in any of the three cell lines.(In Vivo):AB-423 (30 and 100 mg/kg, p.o. bid) blocks HBV replication in a mouse model of HBV. AB-423 (100 mg/kg, p.o. bid) with entecavir (ETV, 100 ng/mg, qd, p.o.) or 0.1 mg/kg dose of ARB-1467 potently inhibits serum HBV DNA in an HDI model of HBV in immunodeficient NOD-SCID mice.

AB-423 is an inhibitor of HBV capsid assembly. AB-423 shows inhibitory effect on rcDNA production in AML12-HBV10 and HepDE19 cells with EC50s of ～0.260 μM. AB-423 also suppresses cccDNA formation-dependent HBeAg production in the HepBHAe82 assay with an EC50 of 0.267 μM and inhibits HBV DNA levels in culture supernatants of HepG 2.2.15 cells with an EC50 of 0.134 μM. However, AB-423 has no cytotoxicity in any of the three cell lines.

AB-423 (30 and 100 mg/kg, p.o. bid) blocks HBV replication in a mouse model of HBV. AB-423 (100 mg/kg, p.o. bid) with entecavir (ETV, 100 ng/mg, qd, p.o.) or 0.1 mg/kg dose of ARB-1467 potently inhibits serum HBV DNA in an HDI model of HBV in immunodeficient NOD-SCID mice.

AB423 | AB423

Microbiology/Virology

HBV

HBV

Infection

HBV Infection

1572510-80-5

386.389

C17H17F3N2O3S

>98% (HPLC)

DMSO : 83.3 mg/mL215.59 mM

CCC(C)NS(=O)(=O)C1=CC(=C(C=C1)F)C(=O)NC2=CC(=C(C=C2)F)F

(R)-5-(N-(sec-butyl)sulfamoyl)-N-(3,4-difluorophenyl)-2-fluorobenzamide

(-20℃)

With Ice Pack

≥ 2 years