atx (autotaxin)

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.

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

BIO-32546 (S-isomer) is a highly potent regulator of autotaxin (ATX) with an IC50 value of 1 nM.

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

HA 155 (Autotaxin Inhibitor IV) is a boronic acid-based compound, inhibiting ATX with IC50 of 5.7 nM by selectively binding to its catalytic threonine.

HA130 is a selective ATX (autotaxin) inhibitor.

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

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

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.

Autotaxin modulator 1 (compound 12b) is an autotaxin (ATX) enzyme inhibitor applicable for studying demyelination and tumours.

BI-2545 is a potent and selective autotaxin (ATX) inhibitor with IC50 values of 2.2 nM and 3.4 nM for human and rat ATX, respectively, and reduces plasma LPA levels in rats.

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.

ATX inhibitor 25 (Compound 29) is an orally active Autotaxin inhibitor with an IC50 of 1.08 nM. It exhibits excellent in vitro metabolic stability, with a half-life (t1/2) of over 170 minutes. In a bleomycin-induced pulmonary fibrosis mouse model, ATX inhibitor 25 (administered orally) shows antifibrotic effects.

Autotaxin-IN-7 (45) is a pyridine-2-carboxylic acid derivative exhibiting sub-nanomolar inhibition of ATX (IC50 = 0.086 nM) and features excellent cardiac safety (hERG > 30 μM) with minimal toxicity to fibroblasts. It inhibits the TGF-β/Smad signaling pathway, reducing α-smooth muscle actin (α-SMA) and extracellular matrix components (ECM). Autotaxin-IN-7 (45) can be used in pulmonary fibrosis research.

ATX inhibitor 26 is an Autotaxin (ATX) inhibitor with an IC50 of 57 nM in human plasma. It effectively inhibits cell migration and collagen gel contraction. Additionally, ATX inhibitor 26 demonstrates significant antifibrotic activity, reducing collagen deposition in a Bleomycin (BLM)-induced pulmonary fibrosis model.

ATX inhibitor 27 (Compound 31) is an ATX inhibitor. It demonstrates IC50 values of 13 nM against human autotaxin (hATX) and 23 nM against lysophosphatidylcholine (LPC). By inhibiting the ATX enzyme, ATX inhibitor 27 reduces LPA levels in the body. This compound is applicable in research related to ATX-LPA-associated conditions such as inflammation, neurodegenerative disorders, and cancer.

18:2 Lyso PA sodium is an unsaturated lysophosphatidic acid (LysoPA) primarily found in plasma lipid mediators and is thought to be involved in the pathogenesis of acute coronary syndrome (ACS). Its correlation with autotaxin (ATX), a serum autocrine motility factor in peripheral arteries, is significant.

ATX-IN-3 is an orally active autotaxin (ATX) inhibitor with an IC50 of 46 nM. It effectively ameliorates pulmonary fibrosis in mouse models by significantly reducing collagen deposition. ATX-IN-3 demonstrates excellent metabolic stability and drug-like properties, making it suitable for research on idiopathic pulmonary fibrosis (IFP).

2ccPA sodium is an agonist of lysophosphatidic acid (LPA) receptors. It regulates processes such as cell proliferation, migration, and apoptosis by activating LPA receptors and inhibiting autotaxin (ATX) enzyme activity. 2ccPA sodium shows potential for research in cancer, inflammation, and fibrosis.

EL244 is an inhibitor of Autotaxin (ATX) with an IC50 of 50 nM and an agonist of PPARγ with an IC50 of 1.3 μM and a Kd of 1.3 μM. In human HepG2 cells, EL244 exhibits low cytotoxicity with an EC50 of 81.2 μM and minimal inhibition of cardiac hERG potassium channels (12% at 25 μM). In vivo, EL244 significantly reduces pulmonary lysophosphatidic acid levels, alleviates fibrosis, restores respiratory function, and has limited systemic absorption. EL244 is suitable for research on idiopathic pulmonary fibrosis.

PAT-347 is a potent inhibitor of Autotaxin (ATX), a secreted enzyme responsible for the hydrolysis of lysophosphatidylcholine (LPC) to the bioactive lysophosphatidic acid (LPA) and choline.

ATX inhibitor 7 is an autotaxin inhibitor that demonstrates good oral exposure.

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

ATX inhibitor 15 (compound 30) is an indole-based carbamate derivative with a strong inhibitory effect on autotaxin (ATX), demonstrated by an IC50 of 2.17 nM. It effectively inhibits ATX activity in vivo, suppresses the expression of pro-fibrotic genes, and exhibits protective effects in Bleomycin-induced lung fibrosis in mice [1].