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| Cas No.: | 857066-90-1 |
| Synonyms: | TMC 353121; TMC-353121 |
| SMILES: | OC1=CC=C(C)N=C1CN2C3=CC(CNC4=CC(C)=CC=C4CCCO)=CC=C3N=C2NCCCN5CCOCC5 |
| Formula: | C32H42N6O3 |
| M.Wt: | 558.7143 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | TMC353121 is a potent RSV fusion inhibitor with pEC50 of 9.9(t1/2 in lung = 25 h). The activity profile of 56d(TMC353121) was found to be identical to the profile of JNJ-2408068. After iv administration, 56d was rapidly eliminated with a plasma clearance of 5.4 L/h/kg. The plasma concentrations dropped quickly within the first hour after dosing and then much more slowly. The plasma half-life determined between 4 and 24 h (last blood sampling time point) was about 10 h. 56d was shown to be active by intravenous, oral, and aerosol administration in the cotton rat model at doses of 10 mg/kg, 40 mg/kg, and 5 mg/mL, respectively. |