ChemicalBook > CAS DataBase List > N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide

N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide

N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide Structure
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide
  • CAS No.864082-47-3
  • Chemical Name:N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide
  • CBNumber:CB12484722
  • Molecular Formula:C21H16F4N4O2
  • Formula Weight:432.37
  • MOL File:864082-47-3.mol
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide Property
  • Boiling point 688.4±55.0 °C(Predicted)
  • Density 1.468
  • storage temp. Sealed in dry,2-8°C
  • solubility DMSO: ≥10mg/mL
  • pka 12.10±0.40(Predicted)
  • form powder
  • color white to beige
  • CAS DataBase Reference 864082-47-3
Safety
  • Hazard Codes  :T
  • Risk Statements  :25
  • Safety Statements  :45
  • RIDADR  :UN 2811 6.1 / PGIII
  • WGK Germany  :3
  • NFPA 704:
    0
    2 0
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordDanger
  • Hazard statements H301
  • Precautionary statements P301+P310

N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide Chemical Properties,Usage,Production

  • Uses GSK 429286 is a selective Rho-kinase (ROCK) inhibitor.It is orally available and has been shown to dramatically reduce mean arterial pressure in spontaneously hypertensive rats.
  • Definition ChEBI: N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide is a member of (trifluoromethyl)benzenes.
  • Biological Activity gsk429286a is a selective inhibitor of rock1 and rock2 with ic50 value of 14 nm and 63 nm, respectively [1].rho-kinase (rock) is a member of agc (protein kinase a, protein kinase g and protein kinase c) family and plays an important role in promoting actin-myosin-mediated contractile force generation [2].gsk429286a is a potent rock inhibitor and has a different activity with the reported rock inhibitor y27632. using gst method, it is shown that gsk429286a treatment (10 μm) increased mypt phosphrylation at thr850 via inhibiting rock which mediated this phosphorylation process [3].in male sprague-dawley rat model with spontaneously hypertensive, oral administration of gsk429286a (30 mg/kg) marks reduced mean arterial pressure and the maximum decreased was as 50 mmhg after nearly 2 h treatment [4].
  • in vivo

    GSK429286A has 61% oral bioavailability in male Sprague-Dawley rats. Oral administration of GSK429286A at single doses of 3-30 mg/kg dramatically reduces mean arterial pressure in the spontaneously hypertensive rats (SHRs) in a dose-dependent manner, with a maximum decrease of 50 mmHg after approximately 2 hours treatment at dose of 30 mg/kg[1].

  • IC 50 ROCK1: 14 nM (IC50); RSK: 780 nM (IC50); p70S6K: 1940 nM (IC50)
  • storage +4°C
  • References [1]. nichols, r.j., et al., substrate specificity and inhibitors of lrrk2, a protein kinase mutated in parkinson's disease. biochem j, 2009. 424(1): p. 47-60.
    [2]. shi, j., et al., distinct roles for rock1 and rock2 in the regulation of cell detachment. cell death dis, 2013. 4: p. e483.
    [3]. davis, d.a., et al., increased therapeutic potential of an experimental anti-mitotic inhibitor sb715992 by genistein in pc-3 human prostate cancer cell line. bmc cancer, 2006. 6: p. 22.
    [4]. goodman, k.b., et al., development of dihydropyridone indazole amides as selective rho-kinase inhibitors. j med chem, 2007. 50(1): p. 6-9.
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide Preparation Products And Raw materials
Raw materials
Preparation Products
N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide Suppliers
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N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide Spectrum
864082-47-3, N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamideRelated Search:
  • Inhibitors
  • 抑制剂
  • 药靶配体
  • 合成有机化合物配体
  • 细胞生物学试剂
  • 小分子抑制剂
  • 细胞周期
  • 小分子抑制剂，天然产物
  • 化合物GSK429286A,10 MM DMSO 溶液
  • GSK429286A,ROCK1 AND ROCK2抑制剂
  • GSK429286A,ROCK1和ROCK2抑制剂
  • N-(6-氟-1H-吲唑-5-基)-2-甲基-6-氧代-4-(4-(三氟甲基)苯基)-1,4,5,6-四氢吡啶-3-甲酰胺
  • GSK429286A游离
  • ROCK1和ROCK2抑制剂(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
  • 864082-47-3
  • GSK429286A, 10 mM in DMSO
  • GSK429286A, ROCK1 and ROCK2 inhibitor
  • GSK429286A (DMSO solution)
  • N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide USP/EP/BP
  • 3-Pyridinecarboxamide, N-(6-fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-
  • GSK 429286A;GSK-429286A;RHO-15
  • GSK429286A;GSK-429286A;GSK 429286A
  • CS-557
  • N-(6-fluoro-1H-indazol-5-yl)-6-methyl-2-oxo-4-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-pyridine-5-carboxamide
  • N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-(4-(trifluoromethyl)-phenyl)-1,4,5,6-tetrahydrop
  • N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide
  • N-(6-Fluoro-1H-indazol-5-yl)-1,4,5,6-tetrahydro-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-3-pyridinecarboxamide
  • N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide GSK 429286 A
  • GSK 429286 A N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-[4-(trifluoromethyl)phenyl]-1,4,5,6-tetrahydro-3-pyridinecarboxamide
  • N-(6-fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-4-(4-(trifluoromethyl)phenyl)-1,4,5,6-tetrahydropyridine-3-carboxamide
  • RHO-15
  • GSK 429286 A
  • RHO-15(GSK429286A)

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