GSK429286A N-(6-氟-1H-吲唑-5-基)-2-甲基-6-氧代-4-[4-(三氟甲基)苯基]-1,4,5,6-四氢-3-吡啶甲酰胺
CAS 864082-47-3 MFCD64082473
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分类
- {SNA} Bioactive Small Molecule Alphabetical Index, G, Kinase/Phosphatase Biology, Rho Kinase (ROCK), Serine/Threonine Kinase Biology, Serine/Threonine Kinase Inhibitors, 生物活性小分子, 细胞信号转导和神经科学, 细胞生物学
- Bioactive Small Molecules, Cell Biology, Cell Signaling and Neuroscience, G, Kinase/Phosphatase Biology, Rho Kinase (ROCK), Serine/Threonine Kinase Biology, Serine/Threonine Kinase Inhibitors
产品应用
- GSK429286A is a selective Rho-kinase inhibitor (IC50 values are 14, 780 and 1940 nM for ROCK1, RSK and p70S6K respectively). Reverses adrenalin-induced contraction of the rat aortic ring (IC50 = 190 nM) and causes a dose-dependent decrease in mean arterial blood pressure in spontaneous hypertensive rats. Orally active.
相关文献及参考
- [2]. Nichols RJ et al Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease. Biochem J. 2009 Oct 23;424(1):47-60.
- Goodman KB, Cui H, Dowdell SE, et al., Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J. Med. Chem. 1 , 6-9, (2007)
- Nichols RJ, Dzamko N, Hutti JE, Cantley LC, et al., Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease. Biochem. J. 1 , 47-60, (2009)
- [1]. Goodman KB et al Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J Med Chem. 2007 Jan 11;50(1):6-9.
- [1]. Goodman KB et al Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors. J Med Chem. 2007 Jan 11;50(1):6-9.
- [2]. Nichols RJ et al Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease. Biochem J. 2009 Oct 23;424(1):47-60.
安全信息
GHS Symbol
- P301+P310
- H301 Toxic if swallowed 吞食有毒
- S45 In case of accident or if you feel unwell seek medical advice immediately (show the label where possible) 发生事故时或感觉不适时,立即求医(可能时出示标签);
- R25 Toxic if swallowed 吞咽有毒