| Company Name: |
Haoyuan Chemexpress Co., Ltd.
|
| Tel: |
021-58950125 |
| Email: |
info@chemexpress.com |
| Products Intro: |
Product Name:chroman 1
CAS:1273579-40-0
Purity:>98% Package:2660RMB/5mg
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| Company Name: |
MedChemexpress LLC
|
| Tel: |
021-58955995 |
| Email: |
sales@medchemexpress.cn |
| Products Intro: |
Product Name:chroman 1
CAS:1273579-40-0
Purity:>98% Package:2660RMB/5mg
|
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| | ROCK-II inhibitor Basic information |
| Product Name: | ROCK-II inhibitor | | Synonyms: | 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)-;chroMan 1;(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 | | CAS: | 1273579-40-0 | | MF: | C24H28N4O4 | | MW: | 436.5 | | EINECS: | | | Product Categories: | | | 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 |
| 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 |
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