产品
编 号：F750793
分子式：C23H29NO7
分子量：431.48
分子式：C23H29NO7
分子量：431.48
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2270215-69-3
产品详情
生物活性：
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 EC50 of 28.2 nM (HBsAg) and 16.0 nM (HBeAg), respectively, but also it is safety for animal.
体内研究：
GST-HG131 exhibits low clearance, moderate plasma half-life (T1/2), high plasma exposure (Cmax 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 dogNote: 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).ParameterCL(iv) (mL/min/kg)Vdss(iv) (L/kg)T1/2 (h)Cmax(po) (nM)AUC0-last(po) (nM·h)Bioavailability (F%)
Mouse755.82.5105587691.6
Rat281.722.0659183271.1
Dog4.041.083.3948502650093.2
体外研究：
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.
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.
体内研究：
GST-HG131 exhibits low clearance, moderate plasma half-life (T1/2), high plasma exposure (Cmax 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 dogNote: 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).ParameterCL(iv) (mL/min/kg)Vdss(iv) (L/kg)T1/2 (h)Cmax(po) (nM)AUC0-last(po) (nM·h)Bioavailability (F%)
Mouse755.82.5105587691.6
Rat281.722.0659183271.1
Dog4.041.083.3948502650093.2
体外研究：
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.
产品资料
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