A potent autotaxin inhibitor
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Product Categories

Product Type

Biochemicals

Research Area

Immunology & Inflammation
Pulmonary Diseases

GLPG1690

Item No. 25498

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[2-ethyl-6-[4-[2-(3-hydroxy-1-azetidinyl)-2-oxoethyl]-1-piperazinyl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)-5-thiazolecarbonitrile
CAS Number
1628260-79-6
Synonyms
  • Ziritaxestat
Molecular Formula
C30H33FN8O2S
Formula Weight
588.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 80 mg/ml
λmax
252 nm
SMILES
O=C(N1CC(O)C1)CN2CCN(C3=CN4C(C(C)=C3)=NC(CC)=C4N(C5=NC(C6=CC=C(F)C=C6)=C(C#N)S5)C)CC2
InChi Code
InChI=1S/C30H33FN8O2S/c1-4-24-29(35(3)30-34-27(25(14-32)42-30)20-5-7-21(31)8-6-20)39-15-22(13-19(2)28(39)33-24)37-11-9-36(10-12-37)18-26(41)38-16-23(40)17-38/h5-8,13,15,23,40H,4,9-12,16-18H2,1-3H3
InChi Key
REQQVBGILUTQNN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $103

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    10 mg

    $183

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    25 mg

    $378

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    50 mg

    $653

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    Product Description

    GLP1690 is a potent inhibitor of autotaxin (Ki = 15 nM).1 It inhibits the production of lysophosphatidic acid (LPA) in mouse, rat, and human plasma (IC50s = 418, 542, and 242 nM, respectively). GLPG1690 (30 mg/kg) reduces extracellular matrix deposition in the lung as well as LPA 18:2 levels in bronchoalveolar lavage fluid in a mouse model of pulmonary fibrosis induced by bleomycin (Item No. 13877).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Desroy, N., Housseman, C., Bock, X., et al. Discovery of 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 (GLPG1690), a first-in-class autotaxin inhibitor undergoing clinical evaluation for the treatment of idiopathic pulmonary fibrosis. J. Med. Chem. 60(9), 3580-3590 (2017).