Adavivint

Product NameAdavivint
CAS1467093-03-3
MFC29H24FN7O
MW505.55
EINECS
MOL File1467093-03-3.mol

Chemical Properties

Density	1.365±0.06 g/cm3(Predicted)
storage temp.	2-8°C
solubility	DMSO:27.5(Max Conc. mg/mL);54.4(Max Conc. mM)
pka	7.75±0.40(Predicted)

Usage And Synthesis

Uses

Adavivint is an intra-articular potential disease-modifying osteoarthritis drug.

Biological Activity

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

Preparation Products And Raw materials

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Target	Value
Wnt ()