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.

PPARγ:1.3 μM

In a mouse model of Bleomycin-induced pulmonary fibrosis, EL244 (15 mg/kg, inhaled) demonstrated favorable lung-targeted pharmacokinetics, characterized by high pulmonary retention, slow local clearance, and limited systemic absorption. Administered at the same dosage via inhalation once daily for 15 days, EL244 exhibited preventive and mitigating anti-fibrotic effects in the same model. When administered intraperitoneally at 30 mg/kg, EL244 showed excellent pharmacokinetic properties, achieving a plasma concentration of 40 μM within 1 hour, maintaining approximately 35 μM for up to 3 hours, and remaining detectable at about 15 μM at 9 hours post-administration, with peak pharmacodynamic effects at the 3-hour mark.