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GLPG-1690

Chemical Structure : GLPG-1690

CAS No.: 1628260-79-6

GLPG-1690 (Ziritaxestat;GLPG 1690;GLPG1690)

Catalog No.: PC-60402Not For Human Use, Lab Use Only.

GLPG-1690 (Ziritaxestat, GLPG1690) is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GLPG-1690 (Ziritaxestat, GLPG1690) is a first-in-class, potent, competitive autotaxin inhibitor with Ki/IC50 of 15 nM/131 nM.
GLPG-1690 (Ziritaxestat) 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.
GLPG-1690 (Ziritaxestat shows no CYP3A4 TDI and decreased hERG inhibitory activity (IC50=15 uM), and good pharmacokinetic profile for treatment idiopathic pulmonary fibrosis.
GLPG-1690 also is an inhibitor of the ectonucleotide pyrophosphatase/ phosphodiesterase family (ENPP2).

Physicochemical Properties

M.Wt 588.71
Formula C30H33FN8O2S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

10 mM in DMSO

Chemical Name/SMILES

2-[[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

References

1. Desroy N, et al. J Med Chem. 2017 May 11;60(9):3580-3590.

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