GLPG-1690 ( Ziritaxestat;GLPG 1690;GLPG1690 )

Catalog No. M12426 CAS No. 1628260-79-6

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

GLPG-1690
Note

Research use only, not for human use.
Brief Description

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

GLPG-1690 (Ziritaxestat, GLPG1690) 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
Synonyms

Ziritaxestat;GLPG 1690;GLPG1690
Pathway

Wnt/Notch/Hedgehog
Target

Autotaxin
Recptor

autotaxin
Research Area

Other Indications
Indication

Fibrosis

CAS Number

1628260-79-6
Formula Weight

588.71
Molecular Formula

C30H33FN8O2S
Purity

>98% (HPLC)
Solubility

DMSO: Soluble （ < 1 mg/ml refers to the product slightly soluble or insoluble )
SMILES

CCC(N=C1N2C=C(C=C1C)N3CCN(CC3)CC(N4CC(C4)O)=O)=C2N(C)C5=NC(C6=CC=C(C=C6)F)=C(S5)C#N
Chemical Name

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

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

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