JNJ-632,1572510-42-9

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JNJ-632

CAS No. : 1572510-42-9

MCE 国际站：JNJ-632

产品活性：JNJ-632 是一种乙型肝炎病毒 (HBV) 衣壳组装调节剂 (CAM)。

研究领域：Anti-infection

作用靶点：HBV

In Vitro: JNJ-632 is a capsid assembly modulator inhibiting hepatitis B virus (HBV). JNJ-632 inhibits HBV DNA HepG2.2.15 and HBV DNA HepG2.117 with EC₅₀s of 0.12 and 0.43 μM, respectively. In the high-content multiparameter cytotoxicity (HepG2), JNJ-632 shows EC₂₀s in the 10-30 μM range (considered weakly cytotoxic).

In Vivo: The single dose PK profile of JNJ-632 is evaluated in C57BL/6 mice following intravenous (iv) and oral (po) administration. JNJ-632 has a moderate plasma clearance of 34 mL/min/kg and a moderate volume of distribution of 1.3 L/kg. The oral bioavailability is 40% following oral administration of 10 mg/kg and 66% following oral administration of 50 mg/kg. JNJ-632 has moderate terminal elimination half-life with t_1/2s of 0.42±0.06 h, 1.1±0.67 h, 2.4±2.3 h, and 5.3±0.1 h for 2.5 mg/kg (iv), 10 mg/kg (po), 50 mg/kg (po), and 50 mg/kg (sc).To circumvent the first pass metabolism, JNJ-632 is also dosed subcutaneously at 50 mg/kg in C57BL/6 mice and this results in a concentration in plasma after 24 h of dosing of 102 ng/mL and concentration in liver after 24 h of dosing of 1297 ng/g.

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