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TMC353121

Chemical Structure : TMC353121

CAS No.: 857066-90-1

TMC353121 (TMC 353121, TMC-353121)

Catalog No.: PC-42807Not For Human Use, Lab Use Only.

TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC50 of 9.9, shows activity against groups A and B RSV and against a panel of clinical isolates with equal potency (EC50<0.1 ng/mL).

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Biological Activity

TMC353121 is a potent respiratory syncytial virus (RSV) fusion inhibitor with pEC50 of 9.9, shows activity against groups A and B RSV and against a panel of clinical isolates with equal potency (EC50<0.1 ng/mL).
TMC353121 binds at a hydrophobic pocket of the 6HB formed by amino acid residues from both HR1 and HR2 heptad-repeats, stabilizes the interaction of HR1 and HR2 in an alternate conformation of the 6HB.
TMC353121 demonstrates in vivo activity in the cotton rat models, significantly reduces viral load, bronchoalveolar lavage cell accumulation and the severity of lung histopathological change at dose of 0.25-10 mg/Kg.

Physicochemical Properties

M.Wt 558.7143
Formula C32H42N6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-Pyridinol, 2-[[6-[[[2-(3-hydroxypropyl)-5-methylphenyl]amino]methyl]-2-[[3-(4-morpholinyl)propyl]amino]-1H-benzimidazol-1-yl]methyl]-6-methyl-

References

1. Bonfanti JF, et al. J Med Chem. 2008 Feb 28;51(4):875-96.

2. Roymans D, et al. Proc Natl Acad Sci U S A. 2010 Jan 5;107(1):308-13.

3. Rouan MC, et al. Antimicrob Agents Chemother. 2010 Nov;54(11):4534-9.

4. Ispas G, et al. PLoS One. 2015 May 26;10(5):e0126959.

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