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产品价格:电议      采购度:159      原产地:美洲
发布时间:2023/10/8 9:13:23 所属地区:国外 国外
简要描述:
BAY-549 (Azaindole 1) 是有口服活性,ATP-竞争型的 ROCK 抑制剂,对 ROCK-1 和 ROCK-2 的 IC50 值分别为 和 nM。
标签:ROCK-IN-2
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CAS No. : 867017-68-3
MCE 站:BAY-549
产品活性:BAY-549 (Azaindole 1) 是有口服活性,ATP-竞争型的 ROCK 抑制剂,对 ROCK-1 和 ROCK-2 的 IC50 值分别为 0.6 和 1.1 nM。
研究领域:Cell Cycle/DNA Damage | Stem Cell/Wnt | Cytoskeleton | TGF-beta/Smad
作用靶点: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 1.1nM, respectively, and also inhibits murine ROCK-2 or rat ROCK-2 with IC50s of 2.4 and 0.8nM, respectively. BAY-549 also inhibits receptor tyrosine kinases TRK and FLT3, with IC50s of 252 and 303nM, respectively, but shows slight inhibition of MLCK and ZIP-kinase with IC50s of 7.4μM and 4.1μM, 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 65nM.
In Vivo: BAY-549 (Azaindole 1) (0.03, 0.1, 0.3mg/kg, i.v.) results in a dose-dependent and long-lasting decrease in blood pressure in anaesthetized normotensive rats. BAY-549 (3 and 10mg/kg, p.o.) decreases blood pressure dose-dependently and persistently both in normotensive and hypertensive rats, and shows such effects even at 1mg/kg in hypertensive rats. BAY-549 (0.1 and 0.3mg/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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更新时间:2024/1/2 10:31:20
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