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GST-HG131

CAS No. : 2270215-69-3

MCE 站：GST-HG131

产品活性：GST-HG131 是一种特异性的乙肝病毒 (HBV) 表面抗原抑制剂，属于二氢苯并吡哆醛 (DBP) 类化合物。GST-HG131 抑制 HBsAg 和 HBeAg 的特异性和效力很强 (EC₅₀=28.2 nM, 16.0 nM)。GST-HG131 还具有良好的动物安全性。

研究领域：Anti-infection

作用靶点：HBV

In Vitro: GST-HG131 shows moderate permeability in Caco-2 assay, low rat ａnd human plasma protein binding, low clearance in liver microsomal stability assays.
GST-HG131 shows antiviral activity in primary human hepatocytes (PHH) expressing HBV, inhibits HBV antigens (both HBsAg ａnd HBeAg).
GST-HG131 (500 nM) appears to inhibit HBV antigens through inhibition of HBV RNAs in a dose- ａnd time-dependent manner.
GST-HG131 shows specific HBV inhibition over other viruses, such as hepatitis C virus, herpes simplex virus type 1 ａnd influenza virus H1N1.

In Vivo: GST-HG131 exhibits low clearance, moderate plasma half-life (T1/2), high plasma exposure (C_max ａnd AUC) ａnd oral bioavailability.
GST-HG131 (3, 10, ａnd 30 mg/kg; i.v., tail vein injection; once daily for 4 weeks) shows HBV inhibition in an AAV/HBV mouse model.
GST-HG131 (100, 300, ａnd 1000 mg/kg; p.o.; once daily for 14 d) is well tolerated at 300 mg/kg ａnd 100 mg/kg in rat preliminary toxicology study.
PK parameter in mouse, rat, ａnd dog
Note: Male C57BL/6 mice (iv/po: 0.5 mg/kg), male SD rats (iv/po: 0.5 mg/kg) ａnd Beagle dogs (iv/po: 0.33 mg/kg).

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