ROCK-IN-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.

ROCK1:0.6 nM (cell free), ROCK2:1.1 nM (cell free)

Azaindole 1 是一种高效的人类ROCK-1和ROCK-2抑制剂（IC50s分别为0.6和1.1?nM），同时也能抑制小鼠和大鼠的ROCK-2（IC50s分别为2.4和0.8nM）。此外，它还能抑制受体酪氨酸激酶TRK和FLT3，其IC50s分别为252和303nM，但对MLCK和ZIP-激酶的抑制作用较弱，IC50s分别为7.4μM和4.1μM。Azaindole 1能在体外引起血管舒张，并以浓度依赖的方式抑制兔隐通动脉对苯肾上腺素的应答（IC50为65nM）。

Azaindole 1（静脉注射0.03、0.1、0.3mg/kg）在麻醉的正常血压大鼠中导致剂量依赖性和持久性的血压降低。Azaindole 1（口服3和10mg/kg）在正常血压和高血压大鼠中均能剂量依赖性和持续性地降低血压，即使在高血压大鼠中，1mg/kg的剂量也显示出此类效应。Azaindole 1（静脉注射0.1和0.3mg/kg的剂量）通过剂量相关的方式降低了麻醉犬的平均动脉血压，并且只导致心率的适度且与剂量无关的增加。

Male Wistar rats (300-350?g) are anesthetized with thiopental 100?mg/kg intraperitoneally (i.p.). A tracheotomy is performed and catheters are inserted into the femoral artery for blood pressure and heart rate measurements and into the femoral vein for test drug administration. The animals are ventilated with room air and their body temperature is controlled. Azaindole 1 is administered intravenously (i.v.) in doses of 0.03-0.1?mg/kg. The vehicle Transcutol/Cremophor EL/physiological saline (19/10/80 = v/v/v) without test drug is used as control. The volume administered is 1?mL/kg. Six animals are treated per group.