2-[[6-[[[2-(3-Hydroxypropyl)-5-methylphenyl]amino]methyl]-2-[[3-(morpholin-4-yl)propyl]amino]benzimidazol-1-yl]methyl]-6-methylpyridin-3-ol
- Product 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 No.
- 857066-90-1
- Chemical 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
- 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-
- CBNumber
- CB32614369
- Molecular Formula
- C32H42N6O3
- Formula Weight
- 558.71
- MOL File
- 857066-90-1.mol
2-[[6-[[[2-(3-Hydroxypropyl)-5-methylphenyl]amino]methyl]-2-[[3-(morpholin-4-yl)propyl]amino]benzimidazol-1-yl]methyl]-6-methylpyridin-3-ol Property
- 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)
N-Bromosuccinimide Price
- Product number
- A3878
- Product name
- TMC353121
- Packaging
- 5mg
- Price
- $219
- Updated
- 2021/12/16
- Product number
- CS-0682
- Product name
- TMC353121
- Purity
- 98.97%
- Packaging
- 10mg
- Price
- $336
- Updated
- 2021/12/16
- Product number
- API0014174
- Product name
- TMC-353121
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $345.4
- Updated
- 2021/12/16
- Product number
- A3878
- Product name
- TMC353121
- Packaging
- 10mg
- Price
- $411
- Updated
- 2021/12/16
- Product number
- CS-0682
- Product name
- TMC353121
- Purity
- 98.97%
- Packaging
- 5mg
- Price
- $180
- Updated
- 2021/12/16
2-[[6-[[[2-(3-Hydroxypropyl)-5-methylphenyl]amino]methyl]-2-[[3-(morpholin-4-yl)propyl]amino]benzimidazol-1-yl]methyl]-6-methylpyridin-3-ol Chemical Properties,Usage,Production
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
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.
2-[[6-[[[2-(3-Hydroxypropyl)-5-methylphenyl]amino]methyl]-2-[[3-(morpholin-4-yl)propyl]amino]benzimidazol-1-yl]methyl]-6-methylpyridin-3-ol Preparation Products And Raw materials
Raw materials
Preparation Products
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