Azaindole 1

Research use only, not for human use.

Azaindole 1 is a selective and ATP-competitive ROCK inhibitor with IC50 of 0.6 and 1.1?nM for human ROCK-1 and ROCK-2.

Azaindole 1 is a selective and ATP-competitive ROCK inhibitor with IC50 of 0.6 and 1.1?nM for human ROCK-1 and ROCK-2.

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.

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.

TC-S 7001 | ROCK-IN-2

Cell Cycle/DNA Damage

ROCK

ROCK1|ROCK2

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867017-68-3

402.79

C18H13ClF2N6O

>98% (HPLC)

DMSO:30 mg/mL (74.48 mM; Need ultrasonic);Water:Insoluble

Cc1c[nH]c2nccc(Oc(c(F)cc(Nc3cc(Cl)nc(N)n3)c3)c3F)c12

——

(-20℃)

With Ice Pack

≥ 2 years