Rilematovir
Based on 5 publication(s) in Google Scholar
Rilematovir (JNJ-678) is a novel fusion protein inhibitor. Rilematovir has the potential for respiratory syncytial virus (RSV) research.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.0%
- CAS. Nr.: 1383450-81-4
- Formel: C21H20ClF3N4O3S
- Molecular Weight:500.92
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
Anti-Infection Compound Library
HY-L002
-
Clinical Compound Library
HY-L026
-
Antiviral Compound Library
HY-L027
-
Drug Repurposing Compound Library
HY-L035
-
Pediatric Drug Library
HY-L104
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
Publications Citing Use of MedChemExpress (MCE) Rilematovir
More
Biologische Aktivität
Fusion protein[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | CC50 |
>50 μM
Compound: 53
|
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 3 days by ATPlite assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 3 days by ATPlite assay
|
[PMID: 32407115] |
Rilematovir is a small-molecule respiratory syncytial virus (RSV) fusion inhibitor currently under clinical evaluation in infants hospitalized for RSV infection. Rilematovir binds to RSV F protein in its prefusion conformation. Rilematovir displays very potent antiviral activity and low cytotoxicity. In addition to its activity against the RSV A2 strain, Rilematovir is also highly active against a number of RSV strains from both A and B subtypes. The EC50 in an RSV infection assay using HeLa cells is 460 pM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS. Nr. 1383450-81-4
-
Appearance Solid
-
Molecular Weight 500.92
-
Formel C21H20ClF3N4O3S
-
Color White to off-white
-
SMILES
O=C(N1CC(F)(F)F)N(CC(N2CCCS(=O)(C)=O)=CC3=C2C=CC(Cl)=C3)C4=C1C=CN=C4
-
Synonyms
JNJ-678; JNJ-53718678
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
-
Journal Impact Factor
-
Most Recent
-
ACS Nano
Inhibition of Measles Viral Fusion Is Enhanced by Targeting Multiple Domains of the Fusion Protein. [Abstract]2021 Aug 24;15(8):12794-12803. PMID: 34291895 -
mBio
A new mechanism of respiratory syncytial virus entry inhibition by small-molecule to overcome K394R-associated resistance. [Abstract]2024 Aug 20:e0138524. PMID: 39162560 -
J Virol
Molecular mechanism of resistance to lonafarnib conferred by mutations in the cysteine-rich region of respiratory syncytial virus fusion glycoprotein and discovery of a lonafarnib-derived antiviral PROTAC. [Abstract]2025 Dec 9:e0148725. PMID: 41364004 -
J Virol
Mechanism of Cross-Resistance to Fusion Inhibitors Conferred by the K394R Mutation in Respiratory Syncytial Virus Fusion Protein. [Abstract]2021 Sep 27;95(20):e0120521. PMID: 34379500 -
bioRxiv
Age-related STAT3 signaling regulates severity of respiratory syncytial viral infection in human bronchial epithelial cells. [Abstract]2023 Sep 21:2023.09.20.558606. PMID: 37781574
Lösungsmittel & Löslichkeit
DMSO : 65 mg/mL (129.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.17 mg/mL (4.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.17 mg/mL (4.33 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.17 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
-
Data Sheet (278 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9963 mL | 9.9816 mL | 19.9633 mL | 49.9082 mL |
| 5 mM | 0.3993 mL | 1.9963 mL | 3.9927 mL | 9.9816 mL | |
| 10 mM | 0.1996 mL | 0.9982 mL | 1.9963 mL | 4.9908 mL | |
| 15 mM | 0.1331 mL | 0.6654 mL | 1.3309 mL | 3.3272 mL | |
| 20 mM | 0.0998 mL | 0.4991 mL | 0.9982 mL | 2.4954 mL | |
| 25 mM | 0.0799 mL | 0.3993 mL | 0.7985 mL | 1.9963 mL | |
| 30 mM | 0.0665 mL | 0.3327 mL | 0.6654 mL | 1.6636 mL | |
| 40 mM | 0.0499 mL | 0.2495 mL | 0.4991 mL | 1.2477 mL | |
| 50 mM | 0.0399 mL | 0.1996 mL | 0.3993 mL | 0.9982 mL | |
| 60 mM | 0.0333 mL | 0.1664 mL | 0.3327 mL | 0.8318 mL | |
| 80 mM | 0.0250 mL | 0.1248 mL | 0.2495 mL | 0.6239 mL | |
| 100 mM | 0.0200 mL | 0.0998 mL | 0.1996 mL | 0.4991 mL |
Powered by Bioz