製品番号: HY-11097

TMC353121

Name: TMC353121
Brand: MedChemExpress
SKU: HY-11097
Price: 660.00 USD
Availability: InStock
Rating: 5 (8 reviews)

8 Cited Publications

カスタマーレビュー

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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純度 : 97.63%
CAS 番号: 857066-90-1
分子式: C₃₂H₄₂N₆O₃
分子量:558.71

保管条件:

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

TMC353121 構造式

CAS 番号: 857066-90-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (8)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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]

体外実験

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. .

体内実験

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.

化学情報

CAS 番号 857066-90-1
性状 Solid
分子量 558.71
分子式 C₃₂H₄₂N₆O₃
Color Pink to red
SMILES

OC1=CC=C(C)N=C1CN2C3=CC(CNC4=CC(C)=CC=C4CCCO)=CC=C3N=C2NCCCN5CCOCC5
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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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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 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
bioRxiv

2025 March 26.

溶剤 & 溶解度

体外:

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.

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

8 Cited Publications

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TMC353121

MedChemExpress（MCE）の使用を引用している文献 TMC353121

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