产品
编 号：F749433
分子式：C18H14ClNO4
分子量：343.76
分子式：C18H14ClNO4
分子量：343.76
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CAS No: 2161364-69-6
产品详情
生物活性：
HBV-IN-25 is a good potency, orally active novel HBV cccDNA reducer. HBV-IN-25 has anti-HBeAg potency and anti-HBV activity with IC50 values of 0.58 μM and 1.15 μM, respectively. HBV-IN-25 has good aqueous solubility (LYSA＞452 μg/mL) and good PK property with no cellular toxicity.
体内研究：
HBV-IN-25 (oral, 5, 20, 100, 300 mg/kg, single) has good PK property, and also shows excellent efficacy in significantly reducing HBV antigens, DNA, and intrahepatic cccDNA levels.Pharmacokinetic Parameters of HBV-IN-25 inHBVcircle mouse model (oral, 5, 20, 100, 300 mg/kg, single).DoseTerminal body weight % versus day 1Spinal cord inflammation Foci per 20 cellsSpinal cord demyelination Score 0–5Spinal cord apoptotic cells Count per section
PK parameter5 mg/kg PO20 mg/kg PO100 mg/kg PO300 mg/kg PO
Cmax(ng/kg)82881573220059900
Tmax(ng/kg)0.250.50.52.67
AUC0?∞(ng h/mL)85711,818119,960453,367
t1/2(h)3.463.451.82
dose-normalized Cmax[(ng/mL)/(mg/kg)]166408322200
Dose-normalized AUC0?24h [(ng h/mL)/(mg/kg)]17159112001511
Animal Model:HBVcircle mouse model
Dosage:5, 20, 100, 300 mg/kg
Administration:oral, 5, 20, 100, 300 mg/kg, single
Result:
体外研究：
HBV-IN-25 (8-50 μM, 5 days) has anti-HBeAg potency with an IC50 value of 0.58 μM.HBV-IN-25 (8-50 μM, 5 days) has the anti-HBV activity in PHH is maintained or slightly decreased with IC50 value of 1.15 μM.
HBV-IN-25 is a good potency, orally active novel HBV cccDNA reducer. HBV-IN-25 has anti-HBeAg potency and anti-HBV activity with IC50 values of 0.58 μM and 1.15 μM, respectively. HBV-IN-25 has good aqueous solubility (LYSA＞452 μg/mL) and good PK property with no cellular toxicity.
体内研究：
HBV-IN-25 (oral, 5, 20, 100, 300 mg/kg, single) has good PK property, and also shows excellent efficacy in significantly reducing HBV antigens, DNA, and intrahepatic cccDNA levels.Pharmacokinetic Parameters of HBV-IN-25 inHBVcircle mouse model (oral, 5, 20, 100, 300 mg/kg, single).DoseTerminal body weight % versus day 1Spinal cord inflammation Foci per 20 cellsSpinal cord demyelination Score 0–5Spinal cord apoptotic cells Count per section
PK parameter5 mg/kg PO20 mg/kg PO100 mg/kg PO300 mg/kg PO
Cmax(ng/kg)82881573220059900
Tmax(ng/kg)0.250.50.52.67
AUC0?∞(ng h/mL)85711,818119,960453,367
t1/2(h)3.463.451.82
dose-normalized Cmax[(ng/mL)/(mg/kg)]166408322200
Dose-normalized AUC0?24h [(ng h/mL)/(mg/kg)]17159112001511
Animal Model:HBVcircle mouse model
Dosage:5, 20, 100, 300 mg/kg
Administration:oral, 5, 20, 100, 300 mg/kg, single
Result:
体外研究：
HBV-IN-25 (8-50 μM, 5 days) has anti-HBeAg potency with an IC50 value of 0.58 μM.HBV-IN-25 (8-50 μM, 5 days) has the anti-HBV activity in PHH is maintained or slightly decreased with IC50 value of 1.15 μM.
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