GST-HG131 (C09-1135-185)

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 animalIn VitroGST-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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Northern-Blot Concentration: 500, 166.67, 55.56, 18.52, 6.17, 2.06, 0.68, 0.23, and 0 nM Incubation Time: 4, 8, 16, 24, 48 hours Result: Inhibited HBV antigens through inhibition of HBV RNAs.In VivoGST-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 CL(iv) (mL/min/kg) V dss (iv) (L/kg) T 1/2 (h) C max (po) (nM) AUC 0-last (po) (nM·h) Bioavailability (F%) Mouse 75 5.8 2.5 1055 876 91.6 Rat 28 1.72 2.0 659 1832 71.1 Dog 4.04 1.08 3.39 4850 26500 93.2 MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:EC50: 28.2 nM (HBsAg),16.0 nM (HBeAg). Specification: 0.99 Molecular Formula: C23H29NO7 Molecular Weight: 431.48