HBV-IN-25 是一种高效的新型HBV cccDNA还原剂，具有口服活性。HBV-IN-25 具有抗 HBeAg 和抗 HBV 活性，IC50值分别为 0.58 μM 和 1.15 μM。HBV-IN-25 水溶性好 (LYSA>452 μg/mL)， PK 性能好，无细胞毒性。

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 IC 50 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 [1].

HBV-IN-25 (8-50 μM, 5 days) has anti-HBeAg potency with an IC 50 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 IC 50 value of 1.15 μM [1].

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 [1]. Pharmacokinetic Parameters of HBV-IN-25 inHBVcircle mouse model (oral, 5, 20, 100, 300 mg/kg, single) [1]. Dose Terminal body weight % versus day 1 Spinal cord inflammation Foci per 20 cells Spinal cord demyelination Score 0–5 Spinal cord apoptotic cells Count per section PK parameter 5 mg/kg PO 20 mg/kg PO 100 mg/kg PO 300 mg/kg PO C max (ng/kg) 828 8157 32200 59900 T max (ng/kg) 0.25 0.5 0.5 2.67 AUC 0 ∞ (ng h/mL) 857 11,818 119,960 453,367 t 1/2 (h) 3.46 3.45 1.82 dose-normalized C max [(ng/mL)/(mg/kg)] 166 408 322 200 Dose-normalized AUC 0 24h [(ng h/mL)/(mg/kg)] 171 591 1200 1511 Animal Model: HBVcircle mouse model [1] Dosage: 5, 20, 100, 300 mg/kg Administration: oral, 5, 20, 100, 300 mg/kg, single Result:

2161364-69-6

C18H14ClNO4

343.76

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years