555555
Rho Kinase Inhibitor V
N-(4-(1H-pyrazol-4-yl)phenyl)-2,3-dihydrobenzo[b][1,4]dioxine-2-carboxamide
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Merck KGaA
Frankfurter Str. 250
64293 Darmstadt
Germany
Phone: +49 6151 72-0
Fax: +49 6151 72 2000
15 February 2012
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A cell-permeable pyrazolyl carboxamide compound that acts as a potent, ATP-binding pocket-targeting inhibitor of ROCK-II (IC50 = 1.5 nM) and effectively inhibits the myosin light chain 2 phosphorylation on Thr18/Ser19 in A7r5 cells (IC50 = 72 nM). It afftects the activities of PKA, MRCK, Akt1 (IC50 = 0.186, 1.19, and 1.41 µM, respectively) and CYP-450 enzymes (% inhibition of 2C9/2D6/3A4/1A2 at 10 µM = 87/40/1/20, respectively) only at much higher concentrations.
Feng, Y., et al. 2008. J. Med. Chem. 51, 6642.
| Product information | |||
|---|---|---|---|
| Form | Light beige solid | ||
| Molar mass | 321.3 | ||
| Protect from Light | Yes | ||
| Packaged under inert gas | Yes | ||
| Purity | ≥97% by HPLC | ||
| Solubility | DMSO or EtOH | ||
| Chemical formula | C18H15N3O3 | ||
| CAS number | 1072906-02-5 | ||
| Store and ship information | |||
|---|---|---|---|
| Storage | +2°C to +8°C | ||
| Ship |
Ambient Temperature Only
Standard Handling |
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