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。

GST-HG131 is a specific inbihitor of hepatitis B virus (HBV) surface antigen, belongs to dihydrobenzopyridooxazepine (DBP) series. GST-HG131 exhibits excellent and specific HBV antigens inhibition with EC 50 of 28.2 nM (HBsAg) and 16.0 nM (HBeAg), respectively, but also it is safety for animal.

EC50: 28.2 nM (HBsAg); 16.0 nM (HBeAg)

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

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). Parameter

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

[1]. Hu Y, et al. Discovery and preclinical evaluations of GST-HG131, a novel HBV antigen inhibitor for the treatment of chronic hepatitis B infection. Bioorg Med Chem Lett. 2022 Nov 1;75:128977.