HBV-IN-25,2161364-69-6

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HBV-IN-25

CAS No. : 2161364-69-6

MCE 国际站：HBV-IN-25

产品活性：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。

研究领域：Anti-infection

作用靶点：HBV

In Vitro: 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.

In Vivo: 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).

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
Cmax(ng/kg)	828	8157	32200	59900
Tmax(ng/kg)	0.25	0.5	0.5	2.67
AUC0−∞(ng h/mL)	857	11,818	119,960	453,367
t1/2(h)	3.46	3.45	1.82
dose-normalized Cmax[(ng/mL)/(mg/kg)]	166	408	322	200
Dose-normalized AUC0−24h [(ng h/mL)/(mg/kg)]	171	591	1200	1511

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