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.

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.

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

Autotaxin modulator 1 is a new modulator of Autotaxin.

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].

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].

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.

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

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

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.

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).

BI-2545 is an autotaxin (ATX) inhibitor that significantly reduces LPA. For human ATX and rat ATX, the IC50s values are 2.2 nM and 3.4 nM , respectively.

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.

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 inhibitor

HA130 is a selective ATX (autotaxin) inhibitor.

PAT-078 is an inhibitor of type II autotaxin.

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.

PAT-494 is an inhibitor of type II Autotaxin.

BMP-22 is an inhibitor of autotaxin (IC50 = 170 nM). It is selective for autotaxin over the phosphodiesterases NPP6 and NPP7 at 10 μM. BMP-22 (0.1-1,000 nM) inhibits autotaxin-mediated production of lysophosphatidic acid (LPA) from lysophosphatidylcholine in vitro in a concentration-dependent manner. It inhibits LPC-dependent MM1 cell invasion of a human umbilical vein endothelial cell (HUVEC) monolayer. BMP-22 (0.5 mg/kg per day) decreases the number of lung metastatic foci in a B16/F10 syngeneic mouse melanoma model of lung metastasis.