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ROCK-IN-2

CAS No. : 867017-68-3

MCE 站：ROCK-IN-2

产品活性：ROCK-IN-2 (Azaindole 1; TC-S 7001) 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: ROCK-IN-2 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. ROCK-IN-2 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. ROCK-IN-2 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: ROCK-IN-2 (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. ROCK-IN-2 (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. ROCK-IN-2 (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.

相关产品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Stem Cell Signaling Compound Library  |  TGF-beta/Smad Compound Library  |  Anti-Aging Compound Library  |  Reprogramming Compound Library  |  Anti-Cardiovascular Disease Compound Library  |  Cytoskeleton Compound Library  |  Orally Active Compound Library  |  Chemical Probe Library  |  Y-27632 dihydrochloride  |  Chroman 1  |  Fasudil Hydrochloride  |  Narciclasine  |  Ripasudil  |  GSK429286A  |  Y-33075  |  CMPD101  |  H-1152 dihydrochloride  |  Hydroxyfasudil  |  BDP5290  |  SR-3677  |  SB-772077B dihydrochloride  |  Pentanoic acid  |  ZINC00881524  |  Verosudil  |  ROCK-IN-1  |  ROCK2-IN-2

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