ROCK-II inhibitor
ROCK-II inhibitor Basic information
- Product Name:
- ROCK-II inhibitor
- Synonyms:
-
- 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
- Chroman 1, 10 mM in DMSO
- CAS:
- 1273579-40-0
- MF:
- C24H28N4O4
- MW:
- 436.5
- Mol File:
- 1273579-40-0.mol
ROCK-II inhibitor Chemical Properties
- 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
ROCK-II inhibitor Usage And Synthesis
Uses
Chroman 1 is a highly potent and selective ROCK inhibitor. Chroman 1 is more potent against ROCK2 (IC50=1 pM) than ROCK1 (IC50=52 pM). Chroman 1 also has inhibitory activity against MRCK, with an IC50 of 150 nM[1][2].
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.
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