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GSK269962A

CAS 850664-21-0

925213-63-4 (deleted)

C29H30N8O5 MW 570.61 

Purity: 99 %

Soluble in DMSO to 24 mM

 

(Expert recommendation)

 

 

 

 

Ordering Information:

 

Cat. No. Axon 1167    Prime Source Promotion

 

Qty1: 2 mg (research sample) / €95  $124

Qty2: 5 mg (research sample) / €145  $189

Promotion: 2 x 5 mg @ €200  $260

Qty3: 25 mg (research sample) / €545  $709

Promotion: 2 x 25 mg @ €800  $1040

Qty4: on request contract research synthesis

 

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Biological Activity:

 

Highly potent and selective inhibitor of Rho-Kinase (ROCK), with IC50 values: 1.6 nM toward ROCK1 and 6 nM toward ROCK2 and high kinase selectivity (>30 fold selective for ROCK compared to other protein kinases tested) and with antihypertensive activity; cardiovascular diseases category.

 

GSK269962A has a much improved potency and selectivity in comparison with Y-27632, which has IC50 values of 140-220 nM for ROCK1 and ROCK2.

 

References: online ref 1

 

C Doe et al. Novel Rho Kinase Inhibitors with Anti-inflammatory and Vasodilatory Activities. J. Pharmacol. Exp. Ther. 2007, 320, 89-98. [online]

 

D Schaafsma et al. Rho kinase inhibitors: A novel therapeutical intervention in asthma? Eur. J. Pharmacol. 2008, 585(2-3), 398-406. [online]

 

Chemical Name: N-(3-{[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-1H-imidazo[4, 5-c]pyridin-6-yl]oxy}phenyl)-4-{[2-(4-morpholinyl)ethyl]-oxy}benzamide

 

GSK269962A | ROCK inhibitor | Axon Medchem | Axon 1167 | GSK 269962A | GSK-269962 A

Axon Ligands TM - Research chemicals for biological study. Some high-profile samples could be provided under terms of contract research synthesis.

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Axon Ligands in the field:

 

GSK 269962A | ROCK inhibitor

Y-27632 | ROCK inhibitor

Thiazovivin | ROCK inhibitor

 

 

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