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| Cas No.: | 1572510-42-9 |
| Chemical Name: | JNJ-632 |
| Synonyms: | JNJ-632; JNJ 632; JNJ632;CS-2776;N-(4-fluoro-3-methyl-phenyl)-3-[[(3S)-tetrahydrofuran-3-yl]sulfamoyl]benzamide;N-(4-fluoro-3-methylphenyl)-3-[[(3S)-oxolan-3-yl]sulfamoyl]benzamide;Benzamide, N-(4-fluoro-3-methylphenyl)-3-[[[(3S)-tetrahydro-3-furanyl]amino]sulfonyl]-;N-(4-Fluoro-3-methylphenyl)-3-[[[(3S)-tetrahydro-3-furanyl]amino]sulfonyl]benzamide |
| SMILES: | C(NC1=CC=C(F)C(C)=C1)(=O)C1=CC=CC(S(N[C@H]2CCOC2)(=O)=O)=C1 |
| Formula: | C18H19FN2O4S |
| M.Wt: | : 378.418 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | JNJ-632 is a hepatitis B virus (HBV) capsid assembly modulator (CAM). |
| 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[1]. |
| 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)[1]. |
| Animal Administration: | Mice[1] The pharmacokinetic profile is evaluated in fed male C57BL/6 mice (n=3/group). Mice are i.v. injected with JNJ-632 at 2.5 mg/kg, formulated as a 0.5 mg/mL solution in PEG400/water (70/30), and blood samples are collected from the saphenous vein at 0.05, 0.17, 0.5, 1, 2, 4, 7, and 24 hours into EDTA-containing microcentrifuge tubes. JNJ-632 is administered p.o. at 10 and 50 mg/kg, formulated as 0.5 and 2.5 mg/mL suspension in methocel 0.5% w/v, and blood samples are collected from the saphenous vein at 0.5, 1, 2, 4, 7, 9 and 24 hours into EDTA-containing microcentrifuge tubes. JNJ-632 is administered s.c. at 50 mg/kg, and blood samples are collected. The blood samples are immediately centrifuged at 4°C and the plasma was stored at -20°C[1]. |
| References: | [1]. Vandyck K, et al. Synthesis and Evaluation of N-Phenyl-3-sulfamoyl-benzamide Derivatives as Capsid Assembly Modulators Inhibiting Hepatitis B Virus (HBV). J Med Chem. 2018 Jul 26;61(14):6247-6260. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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