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GLPG1690

Chemical Structure : GLPG1690

CAS No.: 1628260-79-6

GLPG1690 (Ziritaxestat, GLPG 1690)

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

GLPG1690 (Ziritaxestat, GLPG 1690) 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

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