Y1693 is an orally active RANKL inhibitor with a K d of 5.03 μM for hRANKL . Y1693 inhibits the activation of the downstream c-fos/NFATc1 signaling pathway by blocking its interaction with RANK. Y1693 significantly inhibits RANKL-induced osteoclast differentiation, F-actin ring formation and bone resorptive activity, while downregulating the mRNA and protein expressions of TRAP , cathepsin K , c-fos and NFATc1 . Y1693 shows no obvious cytotoxicity to bone marrow-derived macrophages and osteoclast precursor cells, and exhibits favorable ADME properties. Y1693 improves ovariectomy-induced osteoporosis in mice and reverses ligation-induced periodontal alveolar bone loss. Y1693 is applicable to research related to osteoporosis and periodontal diseases.
Products | Products > Disease Areas > Digestive System Disease | Products > Disease Areas > Digestive System Inflammation | Products > Disease Areas > Mineral Metabolism | Products > Disease Areas > Periodontal Disease | Products > Disease Areas > Osteoporosis | Products > Disease Areas > Inflammation or Immune System Disease | Products > Disease Areas > Metabolic or Endocrine Disease | Products > Signaling Pathways > NF-κB | Products > Signaling Pathways > Immunology/Inflammation | Products > Signaling Pathways > Metabolic Enzyme/Protease | Products > Research Areas > Metabolic Disease | Products > Research Areas > Inflammation/Immunology | Products > Signaling Pathways > RANKL/RANK | Products > Signaling Pathways > Nuclear Factor of activated T Cells (NFAT) | Products > Signaling Pathways > Cathepsin
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