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BAY-549

CAS No. : 867017-68-3

產(chǎn)品活性：BAY-549 (Azaindole 1) is an orally active and ATP-competitive ROCK inhibitor with IC₅₀s of 0.6 and 1.1?nM for human ROCK-1 and ROCK-2, respectively.

研究領(lǐng)域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt  |  Cytoskeleton  |  TGF-beta/Smad

作用靶點：ROCK

In Vitro: BAY-549 (Azaindole 1) is a highly potent inhibitor of human ROCK-1 and ROCK-2, with IC₅₀s of 0.6 and 1.1?nM, respectively, and also inhibits murine ROCK-2 or rat ROCK-2 with IC₅₀s of 2.4 and 0.8?nM, respectively. BAY-549 also inhibits receptor tyrosine kinases TRK and FLT3, with IC₅₀s of 252 and 303?nM, respectively, but shows slight inhibition of MLCK and ZIP-kinase with IC₅₀s of 7.4?μM and 4.1?μM, respectively. BAY-549 induces vasorelaxation in vitro, and suppresses the phenylephrine-induced contraction of rabbit saphenous artery in a concentration dependent manner with an IC₅₀ value of 65?nM.

In Vivo: BAY-549 (Azaindole 1) (0.03, 0.1, 0.3?mg/kg, i.v.) results in a dose-dependent and long-lasting decrease in blood pressure in anaesthetized normotensive rats. BAY-549 (3 and 10?mg/kg, p.o.) decreases blood pressure dose-dependently and persistently both in normotensive and hypertensive rats, and shows such effects even at 1?mg/kg in hypertensive rats. BAY-549 (0.1 and 0.3?mg/kg, i.v. bolus injections) causes decreased mean arterial blood pressure in a dose-related manner and only leads to a moderate and dose-independent increase in heart rate of anaesthetized dogs.

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