Description
TMC353121 is a potent inhibitor of respiratory syncytial virus (RSV) fusion with pEC50 value of 9.9.
Product Overview
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). 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. TMC353121 had dose-dependent antiviral activity, which varied from 1log10 reduction ofpeak 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.
Synonyms
TMC 353121; TMC-353121
Molecular Formula
C32H42N6O3
Chemical Name
2-[[6-[[2-(3-hydroxypropyl)-5-methylanilino]methyl]-2-(3-morpholin-4-ylpropylamino)benzimidazol-1-yl]methyl]-6-methylpyridin-3-ol
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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