Adavivint (SM04690) 是选择性的典型的Wnt信号通路抑制剂,在 SW480 细胞中,用高通量 TCF/LEF 报告基因实验,测得EC50=19.5 nM。
半岛bd体育手机客户端 描述
Adavivint (SM04690) is a Wnt pathway inhibitor.
体内活性
Adavivint (SM04690) is a?novel Wnt pathway inhibitor, for the treatment of moderate to severe osteoarthritis of the knee.
动物实验
A high-throughput screen was performed using a cell-based reporter assay for Wnt pathway activity to develop a small molecule designated SM04690. Its properties were evaluated in bone-marrow-derived human mesenchymal stem cells (hMSCs) to assess chondrocyte differentiation and effects on cartilage catabolism by immunocytochemistry and gene expression, and glycosaminoglycan breakdown. In vivo effects of SM04690 on Wnt signaling, cartilage regeneration and protection were measured using biochemical and histopathological techniques in a rodent acute cruciate ligament tear and partial medial meniscectomy (ACLT + pMMx) OA model.
Cas No.
1467093-03-3
分子式
C29H24FN7O
分子量
505.557
别名
Adavivint (SM04690)
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years