ChemicalBook > CAS DataBase List > 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-(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
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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)
color 
Pink to red
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0682
Product name
TMC353121
Purity
98.97%
Packaging
5mg
Price
$180
Updated
2021/12/16
ApexBio Technology
Product number
A3878
Product name
TMC353121
Packaging
5mg
Price
$219
Updated
2021/12/16
ChemScene
Product number
CS-0682
Product name
TMC353121
Purity
98.97%
Packaging
10mg
Price
$336
Updated
2021/12/16
American Custom Chemicals Corporation
Product number
API0014174
Product name
TMC-353121
Purity
95.00%
Packaging
5MG
Price
$345.4
Updated
2021/12/16
ApexBio Technology
Product number
A3878
Product name
TMC353121
Packaging
10mg
Price
$411
Updated
2021/12/16
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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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857066-90-1, 2-[[6-[[[2-(3-Hydroxypropyl)-5-methylphenyl]amino]methyl]-2-[[3-(morpholin-4-yl)propyl]amino]benzimidazol-1-yl]methyl]-6-methylpyridin-3-olRelated Search:


  • 2-[[6-[[[2-(3-Hydroxypropyl)-5-methylphenyl]amino]methyl]-2-[[3-(morpholin-4-yl)propyl]amino]benzimidazol-1-yl]methyl]-6-methylpyridin-3-ol
  • TMC 353121
  • 2-{[6-({[2-(3-Hydroxypropyl)-5-methylphenyl]amino}methyl)-2-{[3-(4-morpholinyl)propyl]amino}-1H-benzimidazol-1-yl]methyl}-6-methyl-3-pyridinol
  • TMC 353121; TMC-353121
  • 3-Pyridinol, 2-[[6-[[[2-(3-hydroxypropyl)-5-methylphenyl]amino]methyl]-2-[[3-(4-morpholinyl)propyl]amino]-1H-benzimidazol-1-yl]methyl]-6-methyl-
  • 857066-90-1
  • C32H42N6O3