Adavivint Struktur

Adavivint

Bezeichnung:Adavivint

Englisch Name:Adavivint

CBNumberCB23137556

SummenformelC29H24FN7O

Molgewicht505.55

Adavivint physikalisch-chemischer Eigenschaften

Adavivint Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
Adavivint is an intra-articular potential disease-modifying osteoarthritis drug.
Biologische Aktivität
Adavivint (SM04690) is a potent canonical Wnt signaling pathway inhibitor with EC50 of 19.5 nM for TCF/LEF reporter gene. It was more potent than other known Wnt inhibitors in multiple cellular experiments.
in vitro

Treatment of bone marrow-derived human mesenchymal stem cells (CD29+, CD44+ CD166+ CD105+ CD45-) with SM04690 induced a concentration-dependent decrease in Wnt pathway gene expression (ASCL1, LEF1, TCF7L2, TCF7 , C-262 MYC and AXIN2). Selective activation of Wnt signaling pathway with Wnt3a or GSK3β inhibitor CHIR-99021, in IEC6 (intestinal stem cells sensitive to Wnt activation), M04690 can inhibit the expression of AXIN2 and LGR5; in hMSCs, inhibit the expression of AXIN2, TCF7 and LEF1 Express. It has minimal effects on non-canonical Wnt signaling and BMP signaling. In vitro, SM04690 protects chondrocytes from metabolic breakdown.
in vivo

Intra-articular injection of Adavivint promotes cartilage growth and improves joint health in a rat model of knee osteoarthritis. In vivo, it reduces cartilage breakdown.

target

Target	Value
Wnt ()