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Denosumab is designed to target RANKL (RANK ligand), a protein that acts as the primary signal to promote bone removal/resorption. Denosumab prevents RANKL from activating its receptor, RANK, on the surface of osteoclasts and their precursors. Prevention of the RANKL/RANK interaction inhibits osteoclast formation, function, and survival, thereby decreasing bone resorption and increasing bone mass and strength in both cortical and trabecular bone.
In vivo, treatment with 60 mg of Denosumab resulted in reduction in the bone resorption marker serum type 1 C-telopeptide (CTX) by approximately 85% by 3 days. Consistent with the physiological coupling of bone formation and resorption in skeletal remodeling, subsequent reductions in bone formation markers (i.e. osteocalcin and procollagen type 1 N-terminal peptide [PlNP]) were observed starting 1 month after the first dose of Denosumab.
| Molecular Weight | 144700 |
| Formula | C6404H9912N1724O2004S50 |
| CAS Number | 615258-40-7 |
| Form | Liquid |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related NF-κB Products |
|---|
| QNZ
QNZ is an inhibitor of NF-κB activation with IC50 of 11 nM. QNZ (EVP4593) shows strong inhibitory effects on NF-κB transcriptional activation and TNF-α production with IC50s of 11 and 7 nM, respectively. QNZ (EVP4593) is a neuroprotective inhibitor of SOC channel. |
| Caffeic Acid Phenethyl Ester
Caffeic acid phenethyl ester is a potent and specific inhibitor of NF-κB activation, and also displays antioxidant, immunomodulatory and antiinflammatory activities. |
| Cepharanthine
Cepharanthine is a biscoclaurine alkaloid inhibiting tumor necrosis factor (TNF)-α-mediated NFκB stimulation, plasma membrane lipid peroxidation and platelet aggregation and suppressing cytokine production. |
| JSH-23
Jsh-23 is a NF-κB inhibitor, inhibited NF-κB transcriptional activity in lipopolysaccharid-stimulated macrophages RAW 264.7 with IC50 of 7.1 μM. Jsh-23 inhibited the nuclear translocation of NF-κB P65 without affecting the degradation of IκBα. |
| Methylthiouracil
Methylthiouracil is an anti-thyroid agent. Methylthiouracil inhibits TNF-α and IL-6 production and NF-κB and ERK1/2 activation. |
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