RCGD423 是一种gp130调节剂,能阻断关节软骨的退化,并诱导其修复。
产品描述
RCGD423, a small molecule gp130 modulator, prevents articular cartilage degeneration and promotes repair.
体外活性
The ability of RCGD 423 to inhibit hypertrophy in human cells was confirmed by assessing RUNX2 and COL 10 levels in healthy and osteoarthritic articular chondrocytes following incubation with the compound. RCGD 423 elicited a unique signaling profile, driving strong increases in pSTAT3 and MYC levels without activating AKT or NF-κB, resulting in a signaling milieu downstream of gp130 similar to actively proliferating and anabolic fetal chondrocytes.
体内活性
Operated animals would receive an intra-articular injection of 4 μg RCGD 423 loaded onto microspheres at the time of surgery and another 3weeks later. In RCGD 423-treated animals, there was little to no cartilage degradation, structural damage or generation of osteophytes. Control animals showed increased levels of cartilage-degrading proteins and markers of hypertrophy, while these were mostly absent in RCGD 423-treated rats.
Cas No.
108237-91-8
分子式
C15H11BrN2S
分子量
331.23
储存和溶解度
H2O:Insoluble
DMSO:150 mg/mL (452.86 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years