Catalog Number: 3726
Alternate Names: GSK429286A
Chemical Name: 4-[4-(Trifluoromethyl)phenyl]-N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-1,4,5,6-tetrahydro-3-pyridinecarboxamide
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.
Technical Data
  • M.Wt:
    432.37
  • Formula:
    C21H16F4N4O2
  • Solubility:
    Soluble to 100 mM in DMSO and to 25 mM in ethanol
  • Purity:
    >97%
  • Storage:
    Store at +4°C
  • CAS No:
    864082-47-3
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline
Background References
  1. Development of dihydropyridone indazole amides as selective rho-kinase inhibitors.
    Goodman et al.
    J.Med.Chem., 2007;50:6
  2. Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease.
    Nichols et al.
    Biochem.J., 2009;424:47

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