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

化学结构图

864082-47-3
SMILES: CC1=C(C(=O)Nc2cc3cn[nH]c3cc2F)C(c2ccc(C(F)(F)F)cc2)CC(=O)N1

化学属性

Mol. Weight432.37
Mol. FormulaC21H16F4N4O2
Appearance White to off-white solid powder
SolubilitySoluble in DMSO, not in water

别名和识别编码

Synonym GSK429286A; GSK 429286A; GSK-429286A. N-(6-Fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-3-pyridinecarboxamide
CAS Number864082-47-3
Chemical NameGSK429286A
Chemical Name TranslationN-(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
FormulaC21H16F4N4O2
IUPAC NameN-(6-fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-(4-(trifluoromethyl)phenyl)-1,4,5,6-tetrahydropyridine-3-carboxamide
InChIKeyOLIIUAHHAZEXEX-UHFFFAOYSA-N
InChIInChI=1S/C21H16F4N4O2/c1-10-19(20(31)28-17-6-12-9-26-29-16(12)8-15(17)22)14(7-18(30)27-10)11-2-4-13(5-3-11)21(23,24)25/h2-6,8-9,14H,7H2,1H3,(H,26,29)(H,27,30)(H,28,31)
Canonical SMILESO=C(C(C(C1=CC=C(C(F)(F)F)C=C1)C2)=C(C)NC2=O)NC3=CC4=C(NN=C4)C=C3F
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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
Precautionary statements
  • P301+P310
Signal word Danger
Hazard statements
  • H301 Toxic if swallowed 吞食有毒
WGK Germany3
Safety Statements
  • 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);
Hazard Codes T
Risk Statements
  • R25 Toxic if swallowed 吞咽有毒
Storage condition Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

系列性分类


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