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GSK 429286

Cat No. 3726

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Chemical Name: 4-[4-(Trifluoromethyl)phenyl]-N-(6-Fluoro-1H-indazol-5- yl)-2-methyl-6-oxo-1,4,5,6-tetrahydro-3-pyridinecarboxa mide

Biological Activity

Selective Rho-kinase inhibitor (IC₅₀ values are 14, 780 and 1940 nM for ROCK1, RSK and p70S6K respectively). Reverses adrenalin-induced contraction of the rat aortic ring (IC₅₀ = 190 nM) and causes a dose-dependent decrease in mean arterial blood pressure in spontaneous hypertensive rats. Orally active.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline.

Technical Data

M.Wt:

432.37

Formula:

C₂₁H₁₆F₄N₄O₂

Solubility:

Soluble to 100 mM in DMSO and to 50 mM in ethanol

Purity:

>97 %

Storage:

Store at +4°C

The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis and MSDS.

Resources

Certificate of Analysis / MSDS

Certificate of Analysis: View current batch

Material Safety Data Sheet: View current batch

References

Goodman et al (2007) Development of dihydropyridone indazole amides as selective rho-kinase inhibitors. J.Med.Chem. 50 6. Nichols et al (2009) Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease. Biochem.J. 424 47.

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Keywords: GSK 429286, Selective, Rho-kinases, ROCK, inhibitors, Rho-Associated, Coiled-Coil, Kinases, p160ROCK, ROK, GSK429286, GlaxoSmithKline

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