tcsc0027586 Lanifibranor

Lanifibranor is a pan peroxisome proliferator-activated receptor (PPAR) agonist with EC₅₀s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσ and PPARγ, respectively.

IC50 & Target: EC50: 1.5 μM (hPPARα), 0.87 μM (PPARσ), 0.21 μM (PPARγ)^[1]

In Vivo: Lanifibranor is a pan peroxisome proliferator-activated receptor (PPAR) agonist with EC₅₀s of 1.5, 0.87 and 0.21 μM for human PPARα, PPARσand PPARγ^[1]. Skin fibrosis is attenuated by Lanifibranor (IVA337) (p<0.05, vehicle vs Lanifibranor at 30 mg/kg and p<0.001, vehicle vs Lanifibranor at 100 mg/kg). Both low and high doses of Lanifibranor cause a significant decrease of collagenous matrix deposition. Administration of high (100 mg/kg) doses of Lanifibranor results in reduced body weight compare with vehicle controls (p<0.05; Lanifibranor at 100 mg/kg vs vehicle). Results demonstrate that activation of Peroxisome proliferator-activated receptors (PPARs) with Lanifibranor induces a significant reduction in the infiltration of macrophages, CD45+ leucocytes and lymphocytes in Lanifibranor-treated mice compare with rosiglitazone-treated counterparts^[2].