HL-43 (EP4 antagonist HL-43) is a selective prostaglandin E receptor 4 (EP4) antagonist, promotes chondrocyte differentiation/cartilage regeneration and anabolism with low toxicity;
HL-43 exhibits the highest potency in inducing Col2a1 expression and reducing Mmp3 expression in presence of IL-1β.
HL-43 downregulats Mmp3/13 expression in a dose-dependent manner.
HL-43 induces anabolic factors (ACAN and SOX9), and suppresses catabolic factor (MMP13), and hypertrophic marker (COLX), inhibits the STAT3 catabolic pathway;.
HL-43 promotes chondrocyte differentiation and ECM generation, and inhibits matrix degradation in both human and mouse articular cartilage explants.
HL-43 enhances cartilage repair and regeneration in different artilage defect (CD) animal models.
