http://www.ureiko-chem.com/inh....ibitors-agonists/wnt Structure : GLPG-1690
CAS No.: 1628260-79-6
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GLPG-1690(Ziritaxestat;GLPG 1690;GLPG169
Catalog No.:聽URK-V653聽Only Used For Lab.
GLPG-1690 (Ziritaxestat, GLPG169 is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM.
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Biological Activity
GLPG-1690 (Ziritaxestat, GLPG169 is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM; inhibits ATX-induced LPA 18:2 production in mouse, rat, and healthy donor plasma with IC50 of 418 nM, 542 nM, and 242 nM, respectively; shows no CYP3A4 TDI and decreased hERG inhibitory activity (IC50=15 uM), and good pharmacokinetic profile for treatment idiopathic pulmonary fibrosis.
Fibrosis
Phase 2 Clinical
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Physicochemical Properties
M.Wt588.71
FormulaC30H33FN8O2S
CAS No.1628260-79-6
StorageSolide Powder
-20 掳C 3years;
4掳C 2yearsIn Solvent
-80掳C 6 Months
-20掳C 1 Months
Solubility10 mM in DMSO
Chemical Name2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]-piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]-methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile
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References
1. Desroy N, et al. J Med Chem. 2017 May 11;60(9):3580-3590.
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URK-V653_COA
URK-V653_SDS
URK-V653_TDS
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聽Wnt/Notch/Hedgehog Library
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