Cat. No.: HY-11097

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TMC353121

8 Cited Publications

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Based on 8 publication(s) in Google Scholar

TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC₅₀ of 9.9.

For research use only. We do not sell to patients.

Purity: 97.63%
CAS No.: 857066-90-1
Formula: C₃₂H₄₂N₆O₃
Molecular Weight:558.71

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

TMC353121 Chemical Structure

CAS No.: 857066-90-1

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (8)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC₅₀ of 9.9.

IC₅₀ & Target

pEC50: 9.9 (RSV)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	EC₅₀	0.02 ng/mL Compound: 56d	Antiviral activity against RSV CI41 replication in HeLa cells Antiviral activity against RSV CI41 replication in HeLa cells	[PMID: 18254606]
HeLa	EC₅₀	0.02 ng/mL Compound: 56d	Antiviral activity against RSV CI42 replication in HeLa cells Antiviral activity against RSV CI42 replication in HeLa cells	[PMID: 18254606]
HeLa	EC₅₀	0.03 ng/mL Compound: 56d	Antiviral activity against RSV Cl11 replication in HeLa cells Antiviral activity against RSV Cl11 replication in HeLa cells	[PMID: 18254606]
HeLa	EC₅₀	0.04 ng/mL Compound: 56d	Antiviral activity against RSV CI57 replication in HeLa cells Antiviral activity against RSV CI57 replication in HeLa cells	[PMID: 18254606]
HeLa	EC₅₀	0.04 ng/mL Compound: 56d	Antiviral activity against RSV R6LO replication in HeLa cells Antiviral activity against RSV R6LO replication in HeLa cells	[PMID: 18254606]
HeLa	EC₅₀	0.07 ng/mL Compound: 56d	Antiviral activity against RSV LO replication in HeLa cells Antiviral activity against RSV LO replication in HeLa cells	[PMID: 18254606]
HeLa	EC₅₀	279.91 ng/mL Compound: 56d	Antiviral activity against RSV R2LO replication in HeLa cells Antiviral activity against RSV R2LO replication in HeLa cells	[PMID: 18254606]
HeLa	EC₅₀	7.03 ng/mL Compound: 56d	Antiviral activity against RSV R1LO replication in HeLa cells Antiviral activity against RSV R1LO replication in HeLa cells	[PMID: 18254606]
M-HeLa	CC₅₀	4436 ng/mL Compound: 56d	Cytotoxicity against human HeLaM cells by MTT assay Cytotoxicity against human HeLaM cells by MTT assay	[PMID: 18254606]

In Vitro

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.

In Vivo

After i.v. bolus administration of a single dose of 10 mg/kg to Sprague-Dawley rats, the plasma drug concentration-time profile of TMC353121 exhibits multicompartmental pharmacokinetics. Mean plasma drug concentrations decrease rapidly during the first hours after dosing and then more slowly, with a half-life of about 12 h, as determined for the last part of the curve between 8 and 24 h postdose. TMC353121 is rapidly eliminated from plasma (CL=8.6 liters/h/kg) and extensively distributed (V_ss=55 liters/kg)^[2]. TMC353121 is administered once, i.v. at 2.5 mg/kg or at 0.25 mg/kg. Drug levels are determined in lung tissue, serum, and BAL fluid at different time points. TMC353121 followed multicompartment pharmacokinetics, with a fast decay in serum within the first hour after i.v. injection, followed by a slower decay. The drug is eliminated quickly from the blood resulting in very low blood levels after 24 h. Lung concentrations are much higher than serum concentrations and in BAL fluid the drug is just above the limit of detection at 8 h after injection. Very low drug levels can still be detected in the lung 5 days after treatment^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 857066-90-1
Appearance Solid
Molecular Weight 558.71
Formula C₃₂H₄₂N₆O₃
Color Pink to red
SMILES

OC1=CC=C(C)N=C1CN2C3=CC(CNC4=CC(C)=CC=C4CCCO)=CC=C3N=C2NCCCN5CCOCC5
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Nature

Pre-assembly of biomolecular condensate seeds drives RSV replication. [Abstract]

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 Aug 20:e0138524. PMID: 39162560
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
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
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
bioRxiv

2025 March 26.

Solvent & Solubility

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7898 mL

8.9492 mL

17.8984 mL

5 mM

0.3580 mL

1.7898 mL

3.5797 mL

10 mM

0.1790 mL

0.8949 mL

1.7898 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Protocol

Animal Administration^[2]^[3]

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.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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TMC353121

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) TMC353121

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

TMC353121

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) TMC353121

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

TMC353121 Related Classifications

Cat. No.: HY-11097