| Bioactivity | 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 EC50 of 28.2 nM (HBsAg) and 16.0 nM (HBeAg), respectively, but also it is safety for animal[1]. |
| Target | EC50: 28.2 nM (HBsAg); 16.0 nM (HBeAg) |
| Invitro | GST-HG131 shows moderate permeability in Caco-2 assay, low rat and human plasma protein binding, low clearance in liver microsomal stability assays[1].GST-HG131 shows antiviral activity in primary human hepatocytes (PHH) expressing HBV, inhibits HBV antigens (both HBsAg and HBeAg)[1].GST-HG131 (500 nM) appears to inhibit HBV antigens through inhibition of HBV RNAs in a dose- and time-dependent manner[1].GST-HG131 shows specific HBV inhibition over other viruses, such as hepatitis C virus, herpes simplex virus type 1 and influenza virus H1N1[1]. Western Blot Analysis[1] Cell Line: |
| In Vivo | GST-HG131 exhibits low clearance, moderate plasma half-life (T1/2), high plasma exposure (Cmax and AUC) and oral bioavailability[1].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[1].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[1].PK parameter in mouse, rat, and dog[1]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 |
| Name | GST-HG131 |
| CAS | 2270215-69-3 |
| Formula | C23H29NO7 |
| Molar Mass | 431.48 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |
GST-HG131
CAS: 2270215-69-3 F: C23H29NO7 W: 431.48
GST-HG131 is a specific inbihitor of hepatitis B virus (HBV) surface antigen, belongs to dihydrobenzopyridooxazepine (DB
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