Potent, orally available inhibitor of cytosolic phospholipase A2α (cPLA2α, a group IVA phospholipase A2, aka IVA-PLA2) with an IC50 value 0.020 µM in vitro and 0.54 - 0.64 µM in whole blood assay (guinea pig and human, respectively)) with anti-inflammatory efficacy in ear edema and asthma models, and potentially useful for the treatment of nonalcoholic fatty liver diseases, including fatty liver and hepatic fibrosis. ASB14780 markedly attenuated expression of smooth muscle a-actin (a-SMA) protein and the mRNA expression of collagen 1a2, a-SMA, and TGFb1 in the liver, and inhibited the expression of monocyte/macrophage markers. Sold as tromethamine (THAM) salt, as it was used in original publication.

KEYWORDS: ASB14780 | supplier | cPLA2α inhibitor | ASB-14780 | CAS [1069046-00-9] | [1069044-40-1] | Phospholipids | cPLA2 | phospholipase | anti-inflammatory | edema | asthma | pulmonary diseases | fatty liver diseases | hepatic fibrosis | actin | collagen | TGFb1