Teplinovivint 是 wnt/β-CATenin 信号通路抑制剂。它具有抗炎作用,对用于肌腱病具有潜在的研究价值。
产品描述
Teplinovivint is a potent wnt/β-catenin signaling pathway inhibitor. It has anti-inflammatory activity and has the potential for tendinopathy research.
体外活性
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. 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).
体内活性
Teplinovivint (1 mg/ml with 1% BA) has a Tmax of 1 hours in plasma. ?Teplinovivint (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.
Cas No.
1428064-91-8
分子式
C25H26N6O2
分子量
442.523
储存和溶解度
DMSO:83.33 mg/mL (188.31 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years