JNJ-678 (JNJ-53718678)
(Synonyms: JNJ-678; JNJ-53718678) 目录号 : GC32297
An RSV fusion inhibitor
Cas No.:1383450-81-4
Sample solution is provided at 25 µL, 10mM.
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JNJ-53718678 is an inhibitor of respiratory syncytial virus (RSV) fusion.1 JNJ-53718678 binds to and stabilizes the RSV fusion protein in its prefusion conformation.2 It reduces RSV replication in RSV-infected HeLa cells (IC50 = 0.5 nM) with a 50% cytotoxic concentration (CC50) of greater than 50 ?M.1 JNJ-53718678 (4-100 mg/kg), administered prior to infection, reduces RSV viral titers in lavaged-lung tissue and viral RNA production in the lungs in a semi-permissive cotton rat model of RSV.2 JNJ-53718678 also reduces RSV viral titers in bronchoalveolar lavage fluid (BALF) in a fully replicative neonatal lamb model of RSV when administered at doses of 5 and 25 mg/kg per day.
1.Vendeville, S., Tahri, A., Hu, L., et al.Discovery of 3-({5-Chloro-1-[3-(methylsulfonyl)propyl]-1H-indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro-2H-imidazo[4,5-c]pyridin-2-one (JNJ-53718678), a potent and orally bioavailable fusion inhibitor of respiratory syncytial virusJ. Med. Chem.63(15)8046-8058(2020) 2.Roymans, D., Alnajjar, S.S., Battles, M.B., et al.Therapeutic efficacy of a respiratory syncytial virus fusion inhibitorNat. Commun.8(1)167(2017)
Cell experiment: | The antiviral activity of JNJ-678 (JNJ-53718678) against hMPV is evaluated using a cellular infectious assay in 96-well plates in which Vero/TMPRSS2 cells are infected with recombinant hMPV65. Cells are treated with different concentrations of JNJ-678 (JNJ-53718678) and then infected with recombinant hMPV (1×104 PFU per well). Three days post-virus exposure, viral replication is quantified by measuring fluorescence and the EC50 is calculated[1]. |
Animal experiment: | Rats[1]Cotton rats receive either a single dose at 24 h after viral infection or once-daily doses of 40 mg/kg JNJ-678 (JNJ-53718678) by oral gavage, at 24, 48, and 72 h after viral infection. The decrease of viral replication in all experiments is compared to challenged animals that received only the vehicle[1]. |
References: [1]. Roymans D, et al. Therapeutic efficacy of a respiratory syncytial virus fusion inhibitor. Nat Commun. 2017 Aug 1;8(1):167. | |
| Cas No. | 1383450-81-4 | SDF | |
| 别名 | JNJ-678; JNJ-53718678 | ||
| Canonical SMILES | O=C(N1CC(F)(F)F)N(CC(N2CCCS(=O)(C)=O)=CC3=C2C=CC(Cl)=C3)C4=C1C=CN=C4 | ||
| 分子式 | C21H20ClF3N4O3S | 分子量 | 500.92 |
| 溶解度 | DMSO : 65 mg/mL (129.76 mM);Water : < 0.1 mg/mL (insoluble) | 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 | 1.9963 mL | 9.9816 mL | 19.9633 mL |
| 5 mM | 0.3993 mL | 1.9963 mL | 3.9927 mL |
| 10 mM | 0.1996 mL | 0.9982 mL | 1.9963 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet