Balicatib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Balicatib 是组织蛋白酶 K 的抑制剂，IC50 值为 1.4nM。

Balicatib is an inhibitor of cathepsin K with IC50 value of 1.4nM.Balicatib is highly selective against cathepsin K over cathepsin B, L and S in the in vitro enzyme assay. However, the selectivity is not so high in cell-based enzyme assay. The lysosomotropic character of balicatib results in its accumulation in lysosomes and the subsequent nonselective off-target effects. The off-target effects also cause the skin adverse events of balicatib. As a cathepsin K inhibitor, balicatib is developed for osteoporosis. It has been reported to reduce the biochemical markers of bone resorption and increase bone mineral density in ovariectomized monkeys.(In Vitro):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.(In Vivo):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.

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.

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.

AAE581

Proteasome/Ubiquitin

Cysteine Protease

Cathepsin K

Metabolic Disease

——

354813-19-7

411.54

C23H33N5O2

>98% (HPLC)

Soluble in DMSO

O=C(NC1(C(NCC#N)=O)CCCCC1)C2=CC=C(N3CCN(CCC)CC3)C=C2

N-(1-((cyanomethyl)carbamoyl)cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide

(-20℃)

With Ice Pack

≥ 2 years