NDMC101 是有效的破骨细胞形成抑制剂,通过下调 NFATc1 调控基因表达抑制破骨细胞分化。它与DPP4底物相似,通过抑制DPP4抑制早期 T 细胞激活。它能够用于骨疾病的研究,如类风湿关节炎、滑膜炎等。
产品描述
NDMC101 is an inhibitor of dipeptidyl peptidase-IV activity in human T cells and exhibits immunomodulatory effects. It also acts as a novel inhibitor of NFATc1 and NF-κB activity.
体外活性
NDMC101 markedly inhibited RANKL-induced formation of TRAP+ multinucleated cells in RAW264.7 and bone marrow macrophage cells (BMMs).?Moreover, pit formation assay showed that NDMC101 significantly reduced the bone-resorbing activity of mature osteoclasts[1].
体内活性
In CIA mice, oral administration of NDMC101 reduced arthritic index and mitigated bone erosion.?Serum TNF-α and IL-1β concentrations in these mice were decreased significantly at the higher dose of 62.5 mg/kg[1].
细胞实验
Differentiation into osteoclast-like cells was examined by tartrate-resistant acid phosphatase (TRAP) staining and expression of osteoclast differentiation markers[1].
动物实验
Collagen-induced arthritis (CIA) mice were administered test articles by gavages to assess its efficacy.?Then clinical, histological, and biochemical parameters were assessed to determine the effects of N-(4-chloro-2-fluorophenyl)-2-hydroxybenzamide (NDMC101) on synovial inflammation and bone erosion by hematoxlin and eosin staining and Enzyme-linked immunosorbent assay (ELISA)[1].
Cas No.
1308631-40-4
分子式
C13H9ClFNO2
分子量
265.66
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years