Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
JNJ-632 is a novel and potent hepatitis B virus (HBV) capsid assembly modulator (CAM). Small molecule induced hepatitis B virus (HBV) capsid assembly modulation is considered an attractive approach for new antiviral therapies against HBV. JNJ-632 has been used as a tool compound to further profile the mode of action. Administration of JNJ-632 (54) in HBV genotype D infected chimeric mice resulted in a 2.77 log reduction of the HBV DNA viral load.
Targets |
HBV
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ln Vitro |
Hepatitis B virus (HBV) inhibition is achieved by JNJ-632, a capsid assembly modulator. HBV DNA HepG2.2.15 and HBV DNA HepG2.117 are inhibited by JNJ-632, with EC50 values of 0.12 and 0.43 μM, respectively. Within the 10-30 μM range, which is regarded as weakly cytotoxic, JNJ-632 exhibits EC20s in the high-content multiparameter cytotoxicity (HepG2)[1].
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ln Vivo |
C57BL/6 mice are used to assess the single dose PK profile of JNJ-632 after both intravenous (IV) and oral (PO) administration. JNJ-632 exhibits a moderate volume of distribution of 1.3 L/kg and a moderate plasma clearance of 34 mL/min/kg.After oral administration of 10 mg/kg, the oral bioavailability is 40%, and after oral administration of 50 mg/kg, it is 66%. 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), JNJ-632 has a moderate terminal elimination half-life. JNJ-632 is also administered subcutaneously to C57BL/6 mice at a dose of 50 mg/kg in order to avoid the first pass metabolism. This causes a concentration of 102 ng/mL in plasma and 1297 ng/g in the liver 24 hours after dosing[1].
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Animal Protocol |
Mice [1]
Male C57BL/6 mice that have been fed are used to assess the pharmacokinetic profile (n=3/group). JNJ-632, formulated as a 0.5 mg/mL solution in PEG400/water (70/30), is administered intravenously (i.v.) to mice at a dose of 2.5 mg/kg. Blood is drawn from the saphenous vein at 0.05, 0.17, 0.5, 1, 2, 4, 7, and 24 hours and placed into microcentrifuge tubes containing EDTA. JNJ-632 is taken orally at 10 and 50 mg/kg; it is prepared as a 0.5 and 2.5 mg/mL suspension in methocel 0.5% w/v. Blood is drawn at 0.5, 1, 2, 4, 7, 9, and 24 hours from the saphenous vein and placed into microcentrifuge tubes containing EDTA. JNJ-632 is given subcutaneously at a dose of 50 mg/kg, and blood is drawn. The plasma was kept at -20°C while the blood samples were promptly centrifuged at 4°C[1]. |
References |
Molecular Formula |
C18H19FN2O4S
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Molecular Weight |
378.417866945267
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Exact Mass |
378.11
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Elemental Analysis |
C, 57.13; H, 5.06; F, 5.02; N, 7.40; O, 16.91; S, 8.47
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CAS # |
1572510-42-9
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Appearance |
Solid powder
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SMILES |
C(NC1=CC=C(F)C(C)=C1)(=O)C1=CC=CC(S(N[C@H]2CCOC2)(=O)=O)=C1
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InChi Key |
JIZGLOVJKCSHTH-HNNXBMFYSA-N
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InChi Code |
InChI=1S/C18H19FN2O4S/c1-12-9-14(5-6-17(12)19)20-18(22)13-3-2-4-16(10-13)26(23,24)21-15-7-8-25-11-15/h2-6,9-10,15,21H,7-8,11H2,1H3,(H,20,22)/t15-/m0/s1
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Chemical Name |
(S)-N-(4-fluoro-3-methylphenyl)-3-(N-(tetrahydrofuran-3-yl)sulfamoyl)benzamide
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Synonyms |
JNJ 632; JNJ632;JNJ-632
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : 76~125 mg/mL ( 200.83~330.32 mM )
Ethanol : ~76 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.08 mg/mL (5.50 mM) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6426 mL | 13.2128 mL | 26.4257 mL | |
5 mM | 0.5285 mL | 2.6426 mL | 5.2851 mL | |
10 mM | 0.2643 mL | 1.3213 mL | 2.6426 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.