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| 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide Basic information |
Product Name: | 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide | Synonyms: | 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide;CS-2541;GRK2 inhibitor GS180736A;GSK180736;GSK180736A (GSK180736);5-Pyrimidinecarboxamide, 4-(4-fluorophenyl)-1,2,3,4-tetrahydro-N-1H-indazol-5-yl-6-methyl-2-oxo-;GSK180736A >=98% (HPLC);GSK180736A | CAS: | 817194-38-0 | MF: | C19H16FN5O2 | MW: | 365.36 | EINECS: | | Product Categories: | API | 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 Chemical Properties |
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 |
| 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide Usage And Synthesis |
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 | Target | Value | ROCK (Cell-free assay) | 100 nM | GRK2 (Cell-free assay) | 6.6(pIC50) | table>
| 4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide Preparation Products And Raw materials |
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Tag:4-(4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide(817194-38-0)
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