JNJ-632

SKU: orb1226087

Description

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.

Key Properties

• CAS Number: 1572510-42-9
• MW: 378.418
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₉FN₂O₄S
• SMILES: O=C(NC1=CC=C(F)C(C)=C1)C2=CC=CC(S(=O)(N[C@@H]3COCC3)=O)=C2
• Target: HBV
• Solubility: DMSO : 125 mg/mL330.32 mM

Bioactivity

• 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 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.
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• 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 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).
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

JNJ632

Quick Database Links

Gene Symbol

HBV