| Identification | Back Directory | [Name]
2-[[6-[[[2-(3-Hydroxypropyl)-5-methylphenyl]amino]methyl]-2-[[3-(morpholin-4-yl)propyl]amino]benzimidazol-1-yl]methyl]-6-methylpyridin-3-ol | [CAS]
857066-90-1 | [Synonyms]
TMC 353121
TMC 353121; TMC-353121
2-[[6-[[[2-(3-Hydroxypropyl)-5-methylphenyl]amino]methyl]-2-[[3-(morpholin-4-yl)propyl]amino]benzimidazol-1-yl]methyl]-6-methylpyridin-3-ol
2-{[6-({[2-(3-Hydroxypropyl)-5-methylphenyl]amino}methyl)-2-{[3-(4-morpholinyl)propyl]amino}-1H-benzimidazol-1-yl]methyl}-6-methyl-3-pyridinol
3-Pyridinol, 2-[[6-[[[2-(3-hydroxypropyl)-5-methylphenyl]amino]methyl]-2-[[3-(4-morpholinyl)propyl]amino]-1H-benzimidazol-1-yl]methyl]-6-methyl- | [Molecular Formula]
C32H42N6O3 | [MDL Number]
MFCD18633233 | [MOL File]
857066-90-1.mol | [Molecular Weight]
558.71 |
| Chemical Properties | Back Directory | [Melting point ]
208℃ | [Boiling point ]
822.4±75.0 °C(Predicted) | [density ]
1.25 | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Powder | [pka]
9.21±0.10(Predicted) | [color ]
Pink to red |
| Hazard Information | Back Directory | [Biological Activity]
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 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. [3] | [target]
RSV | [storage]
Store at -20°C | [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. |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
| Company Name: |
Musechem
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| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
| Company Name: |
DC Chemicals
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| Tel: |
021-58447131 13564518121 |
| Website: |
http://www.approvedhomemanagement.com/ShowSupplierProductsList927327/0.htm |
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