TMC353121
Based on 8 publication(s) in Google Scholar
TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC50 of 9.9.
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- Pureté: 97.63%
- CAS No.: 857066-90-1
- Formule: C32H42N6O3
- Masse moléculaire:558.71
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TMC353121
More- Nature. 2026 Apr;652(8108):189-200. [Abstract]
- mBio. 2024 Sep 11;15(9):e0138524. [Abstract]
- iScience. 2022 Oct 13;25(11):105354. [Abstract]
- Antimicrob Agents Chemother. 2020 Sep 21;64(10):e00608-20. [Abstract]
- J Virol. 2021 Sep 27;95(20):e0120521. [Abstract]
- J Antimicrob Chemother. 2018 Jul 1;73(7):1823-1829. [Abstract]
- Viruses. 2023 Jul 14;15(7):1548. [Abstract]
- bioRxiv. 2025 March 26.
Activité biologique
pEC50: 9.9 (RSV)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | EC50 |
0.02 ng/mL
Compound: 56d
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Antiviral activity against RSV CI41 replication in HeLa cells
Antiviral activity against RSV CI41 replication in HeLa cells
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[PMID: 18254606] |
| HeLa | EC50 |
0.02 ng/mL
Compound: 56d
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Antiviral activity against RSV CI42 replication in HeLa cells
Antiviral activity against RSV CI42 replication in HeLa cells
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[PMID: 18254606] |
| HeLa | EC50 |
0.03 ng/mL
Compound: 56d
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Antiviral activity against RSV Cl11 replication in HeLa cells
Antiviral activity against RSV Cl11 replication in HeLa cells
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[PMID: 18254606] |
| HeLa | EC50 |
0.04 ng/mL
Compound: 56d
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Antiviral activity against RSV CI57 replication in HeLa cells
Antiviral activity against RSV CI57 replication in HeLa cells
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[PMID: 18254606] |
| HeLa | EC50 |
0.04 ng/mL
Compound: 56d
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Antiviral activity against RSV R6LO replication in HeLa cells
Antiviral activity against RSV R6LO replication in HeLa cells
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[PMID: 18254606] |
| HeLa | EC50 |
0.07 ng/mL
Compound: 56d
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Antiviral activity against RSV LO replication in HeLa cells
Antiviral activity against RSV LO replication in HeLa cells
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[PMID: 18254606] |
| HeLa | EC50 |
279.91 ng/mL
Compound: 56d
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Antiviral activity against RSV R2LO replication in HeLa cells
Antiviral activity against RSV R2LO replication in HeLa cells
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[PMID: 18254606] |
| HeLa | EC50 |
7.03 ng/mL
Compound: 56d
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Antiviral activity against RSV R1LO replication in HeLa cells
Antiviral activity against RSV R1LO replication in HeLa cells
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[PMID: 18254606] |
| M-HeLa | CC50 |
4436 ng/mL
Compound: 56d
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Cytotoxicity against human HeLaM cells by MTT assay
Cytotoxicity against human HeLaM cells by MTT assay
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[PMID: 18254606] |
TMC353121 shows activity against groups A and B RSV and against a panel of clinical isolates with equal potency[1]. TMC353121 is a potent RSV fusion inhibitor in vitro. TMC353121 is active against wild-type RSV (strain LO), with a 50% effective concentration (EC50) of 0.07 ng/mL in HeLaM cells[2].
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.
Chemical Information
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CAS No. 857066-90-1
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Appearance Solid
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Masse moléculaire 558.71
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Formule C32H42N6O3
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Color Pink to red
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SMILES
OC1=CC=C(C)N=C1CN2C3=CC(CNC4=CC(C)=CC=C4CCCO)=CC=C3N=C2NCCCN5CCOCC5
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Nature
2026 Apr;652(8108):189-200. PMID: 41606345 -
mBio
A new mechanism of respiratory syncytial virus entry inhibition by small-molecule to overcome K394R-associated resistance. [Abstract]2024 Sep 11;15(9):e0138524. PMID: 39162560 -
iScience
Ebola and Marburg virus VP35 coiled-coil validated as antiviral target by tripartite split-GFP complementation. [Abstract]2022 Oct 13;25(11):105354. PMID: 36325051 -
Antimicrob Agents Chemother
Inhibitory Effect of PIK-24 on Respiratory Syncytial Virus Entry by Blocking Phosphatidylinositol-3 Kinase Signaling. [Abstract]2020 Sep 21;64(10):e00608-20. PMID: 32718963 -
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 -
J Antimicrob Chemother
Differential antiviral activities of respiratory syncytial virus (RSV) inhibitors in human airway epithelium. [Abstract]2018 Jul 1;73(7):1823-1829. PMID: 29596680 -
Viruses
A Pseudovirus-Based Entry Assay to Evaluate Neutralizing Activity against Respiratory Syncytial Virus. [Abstract]2023 Jul 14;15(7):1548. PMID: 37515234 -
Solvant et solubilité
DMSO : 25 mg/mL (44.75 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (4.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (4.47 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (25.0 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
Protocole
Rats[2]
Sprague-Dawley and cotton rats are given a single-bolus dose of 10 mg/kg TMC353121 intravenously (i.v.). Blood samples are taken from the orbital venous plexus of three Sprague-Dawley rats at 15 min and 1, 8, and 24 h postdose and from six Sprague-Dawley rats and six cotton rats at 3 h postdose. Blood samples are centrifuged at 1,500× g for 10 min, and plasma is separated and frozen until bioanalysis. After blood sampling, the rats are exsanguinated from the vena femoralis under isoflurane-oxygen anesthesia. Then they are euthanized by CO2 asphyxiation, and the lungs are subjected to lavage once via a tracheal cannula with phosphate-buffered saline (PBS) containing 2% bovine serum albumin (BSA) at room temperature at a volume of 5 mL per Sprague-Dawley rat or 2.5 mL per cotton rat. After gentle injection of the lavage fluid into the lungs, the fluid is withdrawn for collection of the bronchoalveolar lavage fluid (BALF) and the lungs are dissected. BALF is collected in order to assess TMC353121 concentrations in the lung epithelial lining fluid (ELF) after correction for the dilution with lavage fluid. A single lavage with a short dwelling time is applied as previously recommended for better accuracy of the determination of ELF dilution. BSA is added to the lavage fluid in order to prevent the adsorption of TMC353121 to syringes or other containers. The BALF is centrifuged at 300× g for 10 min, and the supernatant is separated. BALF supernatant and lung tissue samples are then frozen until bioanalysis. BALF supernatant is referred as BALF throughout this paper.
Mice[3]
Inbred 8- to 12-week-old female BALB/c mice are used. TMC353121 is administered intravenously in saline at doses of 0.25-10 mg/kg, and at various times in relation to the RSV infection. Mice are infected with 2×106 plaque-forming unit (PFU) of plaque-purified human strain RSV A2 (100 μL intranasally). Individual body weight is used to monitor animal health and response to infection, and is recorded daily.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Bonfanti JF, et al. Selection of a respiratory syncytial virus fusion inhibitor clinical candidate. 2. Discovery of a morpholinopropylaminobenzimidazole derivative (TMC353121). J Med Chem. 2008 Feb 28;51(4):875-96. [Content Brief]
[2]. Rouan MC, et al. Pharmacokinetics-pharmacodynamics of a respiratory syncytial virus fusion inhibitor in the cotton rat model. Antimicrob Agents Chemother. 2010 Nov;54(11):4534-9. [Content Brief]
[3]. Olszewska W, et al. Antiviral and lung protective activity of a novel respiratory syncytial virus fusion inhibitor in a mouse model. Eur Respir J. 2011 Aug;38(2):401-8. [Content Brief]
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 | 1.7898 mL | 8.9492 mL | 17.8984 mL | 44.7459 mL |
| 5 mM | 0.3580 mL | 1.7898 mL | 3.5797 mL | 8.9492 mL | |
| 10 mM | 0.1790 mL | 0.8949 mL | 1.7898 mL | 4.4746 mL | |
| 15 mM | 0.1193 mL | 0.5966 mL | 1.1932 mL | 2.9831 mL | |
| 20 mM | 0.0895 mL | 0.4475 mL | 0.8949 mL | 2.2373 mL | |
| 25 mM | 0.0716 mL | 0.3580 mL | 0.7159 mL | 1.7898 mL | |
| 30 mM | 0.0597 mL | 0.2983 mL | 0.5966 mL | 1.4915 mL | |
| 40 mM | 0.0447 mL | 0.2237 mL | 0.4475 mL | 1.1186 mL |
TMC353121 Related Classifications
HY-11097 Related Classifications
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