ROCK-II inhibitor

Product Name: ROCK-II inhibitor
CAS No.: 1273579-40-0
Chemical Name: ROCK-II inhibitor
Synonyms: chroMan 1;ROCK-II inhibitor;Chroman 1, 10 mM in DMSO;(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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ROCK-II inhibitor Suppliers

China 50 United States 8 Global 58

MedChemexpress LLC

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

N,N-DIMETHYLHYDROXYLAMINE HYDROCHLORIDE N,N'-Dimethyl-1,3-propanediamine N,N-Dimethylbenzylamine N,N-Dimethylbenzamide N,N-Dimethylpropionamide

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

1273579-40-0