化学性质:
规格 | 10mM (in 1mL DMSO) 5mg 10mg 25mg |
CAS | 911417-87-3 |
别名 | SLx 2119;SLx2119;ROCK inhibitor;KD-025 |
化学名 | 2-(3-(4-((1H-indazol-5-yl)amino)quinazolin-2-yl)phenoxy)-N-isopropylacetamide |
分子式 | C26H24N6O2 |
分子量 | 452.51 |
溶解度 | ≥ 22.65 mg/mL in DMSO, ≥ 26.4 mg/mL in EtOH with ultrasonic and warming |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
SLx-2119(KD-025) is a selective inhibitor of ROCK2 with IC50 of 105 nM [1].
Rho-associated protein kinase (ROCK) is a serine-threonine kinase and is involved in regulating cytoskeletal dynamics. It is associated with many intracellular processes, which are relevant to stroke. ROCK2 is the predominant isoform mainly expressed in vasculature and neurons [2].
In smooth muscle cells isolated from human intestine with radiation-induced fibrosis (RE-SMC), SLx-2119 reduced mRNA level of CTGF. Over-expression of which is associated with fibrotic diseases. While, in SMC isolated from normal human intestine (N-SMC), SLx-2119 didn't change CTGF mRNA level [1].
In focal cerebral ischemia mice, after transient middle cerebral artery occlusion, KD025 reduced infarct volume in a dose-dependant way. And the efficacy maintained for at least 4 weeks. In aged male and female mice, as well as in type 2 diabetes mice, KD025 reduced infarct volume by 34%, 42% and 32% in aged male mice, female mice and diabetic mice respectively compared to vehicle in mice [2].
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