JNJ-632
目录号 : GC19208
A modulator of HBV capsid assembly
Cas No.:1572510-42-9
Sample solution is provided at 25 µL, 10mM.
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JNJ-632 is a hepatitis B virus (HBV) capsid assembly modulator (CAM).
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 uM, respectively. In the high-content multiparameter cytotoxicity (HepG2), JNJ-632 shows EC20s in the 10-30 uM range (considered weakly cytotoxic)[1].
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].
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.
Animal experiment: | 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. | |
| Cas No. | 1572510-42-9 | SDF | |
| Canonical SMILES | O=C(NC1=CC=C(F)C(C)=C1)C2=CC=CC(S(=O)(N[C@@H]3COCC3)=O)=C2 | ||
| 分子式 | C18H19FN2O4S | 分子量 | 378.42 |
| 溶解度 | DMSO : 125 mg/mL (330.32 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet