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.
1072959-67-1Relevant 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.