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Cat. No. Product Name CAS No. Information

Autotaxin inhibitor compound 1


Autotaxin inhibitor compound 1 (Autotaxin-IN-1) is a potent, selective, orally bioavailable inhibitor of autotaxin with IC50 of 2.2 nM in ex vivo human whole blood assay, does not inhibit related proteins ENPP1 and ENPP7; demonstrates significant anti-inflammatory and analgesic effects in the carrageenan-induced paw inflammation and acetic acid-induced visceral pain tests, respectively; also significantly inhibits disease activity score in the dextran sodium sulfate-induced model of inflammatory bowel disease (IBD) and in autoimmune encephalomyelitis model of multiple sclerosis (MS).




GWJ-A-23 (GWJ-23, GWJ23) is a potent, selective autotaxin inhibitor with Ki of 18 nM, an analog of the known ATX inhibitor S32826 and has improved aqueous solubility compared with the parent compound; reduces lung collagen, bronchoalveolar lavage cell counts, total protein, LPA, and TGF-β levels, attenuates the pathogenesis of pulmonary fibrosis in vivo.




PAT-048 (PAT048) is a potent, selective, noncompetitive autotaxin inhibitor with IC50 of 1.1 nM against the lysoPLD activity of human ATX; exhibits good potency for inhibition of lysoPLD activity with IC50 of 8.9 nM and 22 nM in human blood and mouse plasma, respectively; decreases ATX activity systemically and in the lung, without effect on pulmonary LPA or fibrosis in bleomycin-challenged mice.




PAT-505 (PAT 505, PAT505) is a potent, selective, noncompetitive, and orally active autotaxin inhibitor with IC50 of 2.0 nM against the lysoPLD activity of human ATX; displays high selectivity over other ENPP proteins and no significant agonist or antagonist activity at PPARα and PPARγ; maintains good potency for inhibition of lysoPLD activity with IC50 of 9.7 nM and 62 nM in human blood and mouse plasma, respectively; robustly reduces liver fibrosis with no significant effect on steatosis, hepatocellular ballooning, or inflammation in high-fat diet model of NASH.




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.


Phase 2 Clinical




BI-2545 is a novel potent, selective, orally available Autotaxin inhibitor with IC50 of 2.1 and 3.4 nM for huamn and rat ATX, respectively; displays good potency in the LPA and rat whole blood assay (IC50=29 nM); shows substantial lowering of LPA in vivo, and excellent PK/Target Engagement relationship.




A potent and selective inhibitor of autotaxin with IC50 of 28 nM; shows no effect on chymotryptic, caspase, and tryptic activities of the proteasome, alkaline phosphatase and a broad-spectrum PEDs (IC50>10 uM); inhibits ATX-driven melanoma cell migration and decreases circulating LPA levels in mice.

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