JNJ-678 (JNJ-53718678)是一种呼吸道合胞病毒（RSV）融合蛋白抑制剂。
Cas No.:1383450-81-4
Sample solution is provided at 25 µL, 10mM.
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JNJ-678 (JNJ-53718678) is a respiratory syncytial virus (RSV) fusion protein inhibitor[1-2]. JNJ-678 inhibits the fusion of the virus with the host cell membrane by binding to and stabilizing the prefusion conformation of the RSV fusion protein, thereby preventing viral entry into host cells. JNJ-678 is suitable for research related to RSV infection[3-4].
In vitro, human bronchial epithelial cells (HBECs) were infected with RSV. After 6–24 hours, JNJ-678 (100nM) was added, and the incubation continued for 3 days. JNJ-678 significantly inhibited viral replication[5].
In vivo, cotton rats were orally administered a single dose of JNJ-678 (1–100mg/kg) 1 hour prior to intranasal RSV challenge. JNJ-678 significantly reduced infectious virus titers in the lungs[5].
References:
[1] Huntjens DRH, Ouwerkerk-Mahadevan S, Brochot A, et al. Population Pharmacokinetic Modeling of JNJ-53718678, a Novel Fusion Inhibitor for the Treatment of Respiratory Syncytial Virus: Results from a Phase I, Double-Blind, Randomized, Placebo-Controlled First-in-Human Study in Healthy Adult Subjects. Clin Pharmacokinet. 2017 Nov;56(11):1331-1342.
[2] Stevens M, Rusch S, DeVincenzo J, et al. Antiviral Activity of Oral JNJ-53718678 in Healthy Adult Volunteers Challenged With Respiratory Syncytial Virus: A Placebo-Controlled Study. J Infect Dis. 2018 Jul 24;218(5):748-756.
[3] Cockerill GS. JNJ-5371678, Defining a Role for Fusion Inhibitors in the Treatment of Respiratory Syncytial Virus. J Med Chem. 2020 Aug 13;63(15):8043-8045.
[4] Cichero E, Calautti A, Francesconi V, et al. Probing In Silico the Benzimidazole Privileged Scaffold for the Development of Drug-like Anti-RSV Agents. Pharmaceuticals (Basel). 2021 Dec 15;14(12):1307.
[5] Roymans D, Alnajjar SS, Battles MB, et al. Therapeutic efficacy of a respiratory syncytial virus fusion inhibitor. Nat Commun. 2017 Aug 1;8(1):167.
JNJ-678 (JNJ-53718678)是一种呼吸道合胞病毒（RSV）融合蛋白抑制剂[1-2]。JNJ-678通过结合并稳定RSV融合蛋白的预融合构象来抑制病毒与宿主细胞膜的融合，从而阻止病毒进入宿主细胞。JNJ-678可用于呼吸道合胞病毒感染的相关研究[3-4]。
在体外，对支气管上皮细胞（HBECs）感染呼吸道合胞病毒（RSV）6-24小时后，加入JNJ-678（100nM）继续孵育3天。JNJ-678能显著抑制病毒复制[5]。
在体内，JNJ-678（1-100mg/kg；口服）用于处理在RSV感染前1小时接受给药的棉鼠。JNJ-678显著降低了肺中的感染性病毒滴度[5]。
| Cell experiment [1]: | |
Cell lines | Human bronchial epithelial cells (HBECs) |
Preparation Method | HBECs were maintained in appropriate culture medium. Cells were infected with respiratory syncytial virus (RSV) and subsequently treated with JNJ-678 at a concentration of 100nM for 3 days, either 6 hours or 24 hours post-infection. |
Reaction Conditions | 100nM; 3 days. |
Applications | JNJ-678 significantly inhibited viral replication, reducing viral titers. |
| Animal experiment [1]: | |
Animal models | Cotton rats (Sigmodon hispidus) |
Preparation Method | Animals were administered a single oral dose of JNJ-678 (1, 4, 10, 40, 100mg/kg) 1 hour prior to intranasal challenge with respiratory syncytial virus (RSV). Lung and nasal tissue samples were subsequently collected for analysis. |
Dosage form | 1, 4, 10, 40, 100mg/kg; oral; single dose administered 1 hour pre-challenge. |
Applications | JNJ-678 significantly reduced infectious virus titers in the lungs of cotton rats in a dose-dependent manner. |
References: | |
| 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 | 399.3 μL | 1.9963 mL | 3.9927 mL |
| 10 mM | 199.6 μL | 998.2 μL | 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% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet