ChemicalBook > CAS DataBase List > 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide

4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide

4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide Structure
4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
  • CAS No.817194-38-0
  • Chemical Name:4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
  • CBNumber:CB23163890
  • Molecular Formula:C19H16FN5O2
  • Formula Weight:365.36
  • MOL File:817194-38-0.mol
4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide Property
  • storage temp. Store at -20°C
  • solubility DMSO:57.67(Max Conc. mg/mL);157.83(Max Conc. mM)
    Ethanol:3.0(Max Conc. mg/mL);8.21(Max Conc. mM)
  • form A crystalline solid
  • color Light yellow to khaki
  • UNSPSC Code 12352200
  • NACRES NA.77
Safety
Hazard and Precautionary Statements (GHS)
  • Symbol(GHS)
  • Signal wordWarning
  • Hazard statements H302-H315-H319-H335
  • Precautionary statements P261-P305+P351+P338

4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide Chemical Properties,Usage,Production

  • Uses GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
  • Biological Activity GSK180736A (GSK180736) is a Rho-related, coiled-coil protein kinase inhibitor that binds to GRK2 (G protein-coupled receptor kinase 2) with logIC50 of -6.6. The selectivity for GRK2 is more than 400-fold higher than that for GRK1 and GRK5.
  • in vitro

    GSK180736A inhibits GRK2 with IC50 of 770 nM, 300-fold more potent than GRK5. It is a weak PKA inhibitor with IC50=30 μM; it is a potent ROCK1 inhibitor (IC50=100 nM).

  • target
  • IC 50 ROCK1: 100 nM (IC50); GRK2: 770 nM (IC50)
  • References [1] Waldschmidt HV, et al. Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors. J Med Chem. 2016 Apr 28;59(8):3793-807. DOI:10.1021/acs.jmedchem.5b02000
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    4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide Spectrum
    817194-38-0, 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamideRelated Search:
    • API
    • 抑制剂
    • 药靶配体
    • 细胞生物学试剂
    • 化合物GSK180736A,10 MM DMSO 溶液
    • 4-(4-氟苯基)-N-(1H-吲唑-5-基)-6-甲基-2-氧代-1,2,3,4-四氢嘧啶-5-甲酰胺
    • 化合物GSK180736A
    • GRK2抑制剂(GSK180736A)
    • 817194-38-0
    • GSK180736A, 10 mM in DMSO
    • inhibit,ROCK,Inhibitor,ROK,Rho-kinase,Rho-associated kinase,Rho-associated protein kinase,GSK180736A,GSK-180736A
    • GSK180736A
    • GSK180736A >=98% (HPLC)
    • 5-Pyrimidinecarboxamide, 4-(4-fluorophenyl)-1,2,3,4-tetrahydro-N-1H-indazol-5-yl-6-methyl-2-oxo-
    • GSK180736A (GSK180736)
    • GSK180736
    • GRK2 inhibitor GS180736A
    • CS-2541
    • 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide

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    TargetValue
    ROCK
    (Cell-free assay)    		 100 nM
    GRK2
    (Cell-free assay)    		 6.6(pIC50)