Teplinovivint is a potent wnt/β-catenin signaling pathway inhibitor. Teplinovivint has anti-inflammatory activity and has the potential for tendinopathy research.In Vitro: Teplinovivint (compound 175; 0.0003-10 μM) inhibits Wnt/p-catenin activity in human colorectal cancecell line (SW480) in a dose-dependent manner (EC50=152.9 nM).
Teplinovivint inhibits SW480 cells (EC50=25 nM) and primary human mesenchymal stem cells (hMSCs; EC50=10.377 μM).
Teplinovivint (5.8, 10.8, 21.7, 41.7, 83.3, 166.6, 333.3, 750 nM) induced the expression of SCXA, TenacinC and Tenomodulin, in a dose-dependent manner with an EC50 between 139-189 nM.
In Vivo: Teplinovivint (compound 175; 10 mg/ml; once daily for 21 days via topical application) causes amelioration of inflammation as well as tendon degeneration. Teplinovivint results in a decrease of aninflammatory plasma biomarker, KC/GRO in the Collagenase-induced Tendon Injury Model.
Teplinovivint (1 mg/ml with 1% BA) has a Tmax of 1 hours in plasma.