产品
编 号:F333816
分子式:C23H33N5O2
分子量:411.54
产品类型
结构图
CAS No: 354813-19-7
联系客服
产品详情
生物活性:
Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC50 values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis.
体内研究:
Balicatib (0, 3, 10, 50 mg/kg; Oral gavage; twice daily for 18 months) partially prevented ovariectomyinduced changes in bone mass, inhibited bone turnover at most sites, and had an stimulatory effect on periosteal bone formation in cynomolgus monkeys.Animal Model:11-13 years, female cynomolgus monkeys (Macaca fascicularis)
Dosage:0, 3, 10, 50 mg/kg
Administration:Oral gavage; twice daily for 18 months
Result:Completely prevented ovariectomy-induced increases in BFR/BS in cancellous bone of vertebra and femur and in osteonal and endocortical bone of vertebra, significantly decreased bone formation rates.
体外研究:
Balicatib (0-10 μM) shows less than 1.5-fold accumulation of Type I collagen at concentrations up to 10 μM in human dermal fibroblasts.