JNJ-632

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

JNJ-632 (JNJ632) 是一种新型有效的 HVV 衣壳组装调节剂和 HBV 复制抑制剂。

JNJ-632 (JNJ632) is a novel potent HVV capsid assembly modulator and HBV replication inhibitor with EC50 of 100-200 nM for genotypes A-D; does not show cytotoxicity for HepG2 cells (CC50>100 uM); dose-dependently reduces intracellular HBV RNA levels as well as HBe/cAg and HBsAg levels in the cell culture supernatant.

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 of0.12 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).

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 t1/2s 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.

JNJ632

Microbiology/Virology

HBV

HBV

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1572510-42-9

378.418

C18H19FN2O4S

>98% (HPLC)

DMSO : 125 mg/mL330.32 mM

O=C(NC1=CC=C(F)C(C)=C1)C2=CC=CC(S(=O)(N[C@@H]3COCC3)=O)=C2

(S)-N-(4-fluoro-3-methylphenyl)-3-(N-(tetrahydrofuran-3-yl)sulfamoyl)benzamide

(-20℃)

With Ice Pack

≥ 2 years