Y1693 is an orally active RANKL inhibitor with a Kd 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[1][2].
Molecular Weight:
419.52
Purity:
99.91
CAS Number:
[2812381-74-9]
Formula:
C28H25N3O
Target:
Cathepsin,Nuclear Factor of activated T Cells (NFAT),RANKL/RANK
Application Notes:
MCE Product type: Reference compound
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