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1072959-67-1

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  • N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxin-2-carboxamide

    Cas No: 1072959-67-1

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1072959-67-1 Usage

Uses

SR 3677 is an ATP-competitive inhibitor of Rho-kinases (ROCK-I/ROCK-II) which reduces amyloid-β production. It’s hypothesized that Alzheimer’s Disease, can be treated with this type of treatment, and delay further progression of the disease.

Biological Activity

sr-3677 is a novel, potent and highly selective inhibitor of rho kinase (rock-ii) with the ic50 value of ~0.3nm in enzyme and cell based assays [1].sr-3677 has been reported to selectively inhibit the rock- ii with the ic50 values of ~3nm, ~3nm, 56nm, 3.968μm,1.190μm and 7.491μm for rock-ii,ppmlc, rock-i, pka, mrck and akt1, respectively. in addition, sr-3677 has been shown several key binding elements that contribute to the high potency and selectivity in the docking assay. furthermore, sr-3677 has been revealed to be efficacious in enhancing aqueous humor outflow and in target modulation in the pharmacology studies [1].

references

[1] feng y1, yin y, weiser a, griffin e, cameron md, lin l, ruiz c, schürer sc, inoue t, rao pv, schr?ter t, lograsso p. discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective rho kinase (rock-ii) inhibitors. j med chem. 2008 nov 13;51(21):6642-5. doi: 10.1021/jm800986w. epub 2008 oct 4.

Check Digit Verification of cas no

The CAS Registry Mumber 1072959-67-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,0,7,2,9,5 and 9 respectively; the second part has 2 digits, 6 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1072959-67:
(9*1)+(8*0)+(7*7)+(6*2)+(5*9)+(4*5)+(3*9)+(2*6)+(1*7)=181
181 % 10 = 1
So 1072959-67-1 is a valid CAS Registry Number.

1072959-67-1 Well-known Company Product Price

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  • Sigma

  • (SML0774)  SR 3677  ≥98% (HPLC)

  • 1072959-67-1

  • SML0774-5MG

  • 1,244.88CNY

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  • Sigma

  • (SML0774)  SR 3677  ≥98% (HPLC)

  • 1072959-67-1

  • SML0774-25MG

  • 5,029.83CNY

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1072959-67-1SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 20, 2017

Revision Date: Aug 20, 2017

1.Identification

1.1 GHS Product identifier

Product name N-[2-[2-(dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxine-3-carboxamide

1.2 Other means of identification

Product number -
Other names RS0088

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

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More Details:1072959-67-1 SDS

1072959-67-1Downstream Products

1072959-67-1Relevant articles and documents

Discovery of substituted 4-(pyrazol-4-yl)-phenylbenzodioxane-2-carboxamides as potent and highly selective Rho kinase (ROCK-II) inhibitors

Feng, Yangbo,Yin, Yan,Weiser, Amiee,Griffin, Evelyn,Cameron, Michael D.,Lin, Li,Ruiz, Claudia,Schürer, Stephan C.,Inoue, Toshihiro,Rao, P. Vasanth,Schr?ter, Thomas,LoGrasso, Philip

supporting information; experimental part, p. 6642 - 6645 (2009/10/23)

The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compound 5 (SR-3677) had an IC50 of ~3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibited only 3 out of 70 nonkinase enzymes and receptors. Pharmacology studies showed that 5 was efficacious in both, increasing ex vivo aqueous humor outflow in porcine eyes and inhibiting myosin light chain phosphorylation.

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