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TMC353121

Catalog No.
A3878
Potent RSV fusion inhibitor
Grouped product items
SizePriceStock Qty
5mg
$209.00
Ship with 10-15 days
10mg
$391.00
Ship with 10-15 days
50mg
$1,186.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

TMC353121 is a RSV fusion inhibitor. It has been developed from the precursor molecule JNJ-2408068 using a molecular modelling approach. It maintains high activity (pEC50 9.9) and low cytotoxicity, while presenting a shorter retention time in the lung (lung t1/2 25 h). [1]

TMC353121 was found to inhibit RSV by preventing both virus cell fusion and syncytia formation by causing a local disturbance of the natural six-helix bundle conformation of RSV-F protein.

TMC353121 reduces viral load in therapeutic and prophylactic administration. TMC353121 has potent antiviral properties in vivo in a BALB/c mice model and protects against lung infection and virus-induced inflammation.[2]

TMC353121 had dose-dependent antiviral activity, which varied from 1log10 reduction of

peak viral load to complete inhibition of the RSV replication. TMC353121 (0.39 μg/mL) can completely inhibit the shedding of RSV. And a dose-dependent reduction of INFγ, IL6 and MIP1α was associated. TMC353121 administered as CI for 16 days was generally well-tolerated. [3]

References:
1. Bonfanti JF, Meyer C, Doublet F et al.  Selection of a respiratory syncytial virus fusion inhibitor clinical candidate. 2. Discovery of a morpholinopropylaminobenzimidazole derivative (TMC353121). J Med Chem. 2008; 51: 875–896.
2. Olszewska W1, Ispas G, Schnoeller C 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.
3. Ispas G, Koul A, Verbeeck J et al.  Antiviral Activity of TMC353121, a Respiratory Syncytial Virus (RSV) Fusion Inhibitor, in a Non-Human Primate Model. PLoS One. 2015 May 26;10(5):e0126959.

Chemical Properties

StorageStore at -20°C
M.Wt558.71
Cas No.857066-90-1
FormulaC32H42N6O3
SynonymsTMC 353121; TMC-353121
SolubilitySoluble in DMSO
Chemical Name2-[[6-[[2-(3-hydroxypropyl)-5-methylanilino]methyl]-2-(3-morpholin-4-ylpropylamino)benzimidazol-1-yl]methyl]-6-methylpyridin-3-ol
SDFDownload SDF
Canonical SMILESCC1=CC(=C(C=C1)CCCO)NCC2=CC3=C(C=C2)N=C(N3CC4=C(C=CC(=N4)C)O)NCCCN5CCOCC5
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description TMC353121 is a potent inhibitor of respiratory syncytial virus (RSV) fusion with pEC50 value of 9.9.
Targets RSV          
IC50 9.9 (pEC50)          

Quality Control

Quality Control & MSDS

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Chemical structure

TMC353121