| Identification | Back Directory | [Name]
ROCK-II inhibitor | [CAS]
1273579-40-0 | [Synonyms]
chroMan 1
ROCK-II inhibitor
(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)- | [Molecular Formula]
C24H28N4O4 | [MDL Number]
MFCD23098792 | [MOL File]
1273579-40-0.mol | [Molecular Weight]
436.5 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 | [storage]
Store at -20°C | [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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| Company Name: |
LETOPHARM LIMITED
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| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
SPIRO PHARMA
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| Telephone: |
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| Website: |
www.spiropharma.com.cn |
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