autotaxin

Autotaxin-IN-4 is an Autotaxin inhibitor. It has the potential to treat idiopathic pulmonary fibrosis.

Ziritaxestat (GLPG1690), an autotaxin inhibitor, currently being evaluated in an exploratory phase 2 study in idiopathic pulmonary fibrosis patients.

Autotaxin-IN-3 is an inhibitor of Autotaxin (IC50 = 2.4 nM) which is responsible for the increase in lysophosphatidic acid in ascites and plasma.

Autotaxin-IN-6 (compound 23) is a potent inhibitor of autotaxin (ATX), exhibiting an IC50 of 30 nM, and attenuates cell migration with potential applications in anticancer research [1].

Autotaxin modulator 1 is a new modulator of Autotaxin.

Autotaxin-IN-5 is an Autotaxin inhibitor. It has the potential to treat idiopathic pulmonary fibrosis.

Autotaxin-IN-1 is a potent autotaxin inhibitor used in the treatment of osteoarthritis pain. It exhibits favorable potency (IC50=2.2 nM), pharmacokinetic (PK) properties, and a robust PK pharmacodynamic (PD) relationship[1].

ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor (IC50: 15.3 nM) that reduces CCl4-induced hepatic fibrosis and exhibits anti-hepatic fibrosis effects.

Cudetaxestat (BLD-0409) is a potent, orally active autotaxin inhibitor.

ONO-8430506 is an orally available, potent autotaxin (ATX) ENPP2 inhibitor (IC90: 100 nM) that inhibits ATX activity in mouse plasma.

CRT0273750 regulates plasma LPA levels and is suitable for in vivo studies. CRT0273750 is an autotaxin (ATX) inhibitor with IC50 of 0.014 μM.

HA130 is a selective ATX (autotaxin) inhibitor.

PF-8380 is an effective and orally available autotaxin inhibitor (IC50: 2.8 nM, in isolated enzyme assay; 101 nM, in the human whole blood). It modulates lysophosphatidic acid (LPA) levels in vivo vitro by directly inhibiting autotaxin; reduces LPA levels both in plasma and at the site of inflammation.

Z-HA155 (CS-963) selectively and potently inhibits autotaxin with an IC50 of 5.7 nM.

Sphingomyelins are complex membrane lipids composed of phosphorylcholine, sphingosine, and an acylated group, such as a fatty acid. Lysosphingomyelin is a naturally-occurring lipid which is produced by the removal of the acylated group of sphingomyelin by a deacylase. Lysosphingomyelin may, in turn, serve as a substrate for autotaxin, which removes choline to produce sphingosine-1-phosphate. The receptors and signaling pathways that are activated by lyso-sphingosine are diverse and vary between cell types. Lysosphingomyelin occurs naturally in plasma, is a constituent of lipoproteins, and is increased in some diseases, including dermatitis and Niemann-Pick disease.

KR-40795 is an effective inhibitor of ATX (autotaxin) with an IC50 of 0.13 μM. This compound plays a crucial role in liver diseases.

PAT-048 is an effective and selective autotaxin inhibitor. PAT-048 reduces dermal fibrosis in vivo. PAT-048 also inhibits IL-6 mRNA expression but displays no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in the lung fibrosis model. PAT-048 has an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma.

MEY-003, an Autotaxin (ATX) inhibitor, exhibits EC50 values of 460 nM for hATX-β and 1.09 μM for hATX-ɣ (analysis with LPC18:1), demonstrating its potency against these isoforms. It acts non-competitively with a K i of 432 nM, making it suitable for research into diseases where ATX is implicated [1].

ATX inhibitor 22 is a novel ATX (autotaxin) inhibitor with an IC50 of 218.9 μM, and it lacks inhibitory activity against LPAR1.

PAT-078 is an inhibitor of type II autotaxin.

autotaxin inhibitor

CBT-295, an orally active autotaxin (ATX) inhibitor, effectively decreases inflammatory cytokines including TGF-β, TNF-α, and IL-6, along with the bile duct proliferation marker CK-19, and ameliorates liver fibrosis. The compound's ability to reverse liver fibrosis contributes to lowered ammonia levels in the blood and brain, which in turn reduces ammonia-induced neuroinflammation. CBT-295 shows potential for the study of liver cirrhosis and related encephalopathy.

PAT-505 is an orally available, selective and potent inhibitor of autologous epidermal growth factor (IC50 2 nM in Hep3B cells, 9.7 nM in human blood, 62 nM in mouse plasma).

PAT-347 is a potent Autotaxin Inhibitor. Autotaxin (ATX) is a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline. The ATX-LPA signaling pathway is implicated in cell survival, migration, and proliferation; thus, the inhibition of ATX is a recognized therapeutic target for a number of diseases including fibrotic diseases, cancer, and inflammation, among others.