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ROCK-II inhibitor

Product Name
ROCK-II inhibitor
CAS No.
1273579-40-0
Chemical Name
ROCK-II inhibitor
Synonyms
chroMan 1;ROCK-II inhibitor;(S)-N-(2-(2-(Dimethylamino)ethoxy)-4-(1H-pyrazol-4-yl)phenyl)-6-methoxychroman-3-carboxamide;(3S)-N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-3,4-dihydro-6-methoxy-2H-1-benzopyran-3-carboxamide;2H-1-Benzopyran-3-carboxamide, N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-3,4-dihydro-6-methoxy-, (3S)-;glaucoma,Chroman1,injury,cord,inhibit,ROCK,Rho-associated protein kinase,rho kinase,Chroman-1,Rho-kinase,ROK,Chroman 1,spinal,Rho-associated kinase,Inhibitor
CBNumber
CB12624292
Molecular Formula
C24H28N4O4
Formula Weight
436.5
MOL File
1273579-40-0.mol
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ROCK-II inhibitor Property

Boiling point:
675.9±55.0 °C(Predicted)
Density 
1.256±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
Soluble in DMSO
form 
Solid
pka
13.08±0.70(Predicted)
color 
White to pink
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Tocris
Product number
7163
Product name
Chroman1
Purity
≥98%(HPLC)
Packaging
10
Price
$316
Updated
2021/12/16
ChemScene
Product number
CS-0775
Product name
Chroman1
Purity
99.90%
Packaging
5mg
Price
$343
Updated
2021/12/16
ApexBio Technology
Product number
A3310
Product name
chroman1
Packaging
5mg
Price
$419
Updated
2021/12/16
ChemScene
Product number
CS-0775
Product name
Chroman1
Purity
99.90%
Packaging
10mg
Price
$678
Updated
2021/12/16
ApexBio Technology
Product number
A3310
Product name
chroman1
Packaging
10mg
Price
$827
Updated
2021/12/16
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ROCK-II inhibitor Chemical Properties,Usage,Production

Biological Activity

chroman 1 is a highly potent rock-ii inhibitor. rock is a member of the agc kinase family of serine/threonine kinases that is comprised of two highly homologous isoforms, which are rock-i and rock-ii.. as one of the downstream effectors of rhoa, rock regulates stress fiber formation and actin cytoskeletal organization via phosphorylation of myosin light chain. currently, there is plenty of interest in the inhibition of rho kinase (rock) to treat various diseases.

in vitro

chroman 1 was found to be a sub-nanomolar rock-ii inhibitor with excellent to moderate selectivity over related kinases studied as a preliminary assessment, such as akt1, protein kinase a (pka), and the highly homologous cdc42-binding kinase. in addition, chroman 1 also showed good in-vitro activity in the functional cell-based myosin light chain bis-phosphorylation assay [1].

in vivo

pharmacokinetic evaluation in rats showed that chroman 1 had moderately improved oral bioavailability (27–35%) relative to its lead compounds, which were benzodioxane and chroman. in addition, chroman 1 also displayed an unique intriguing pharmacokinetic profile, which was with high systemic exposure through oral delivery [1].

IC 50

<1 nm for rock-ii

References

[1] chen yt,bannister td,weiser a,griffin e,lin l,ruiz c,cameron md,schürer s,duckett d,schrter t,lograsso p,feng y. chroman-3-amides as potent rho kinase inhibitors. bioorg med chem lett.2008 dec 15;18(24):6406-9.

ROCK-II inhibitor Preparation Products And Raw materials

Raw materials

Preparation Products

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1273579-40-0, ROCK-II inhibitorRelated Search:


  • ROCK-II inhibitor
  • chroMan 1
  • (3S)-N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-3,4-dihydro-6-methoxy-2H-1-benzopyran-3-carboxamide
  • 2H-1-Benzopyran-3-carboxamide, N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-3,4-dihydro-6-methoxy-, (3S)-
  • (S)-N-(2-(2-(Dimethylamino)ethoxy)-4-(1H-pyrazol-4-yl)phenyl)-6-methoxychroman-3-carboxamide
  • glaucoma,Chroman1,injury,cord,inhibit,ROCK,Rho-associated protein kinase,rho kinase,Chroman-1,Rho-kinase,ROK,Chroman 1,spinal,Rho-associated kinase,Inhibitor
  • 1273579-40-0