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产品名称：Xcess/AAE-581-Xcessbio Biosciences Inc/2mg/M60434-2s

产品编号：M60434-2s

市场价：¥2780.00

场地：美国(厂家直采)

产品分类：蛋白类>聚合物>

联系QQ：1570468124

电话号码：4000-520-616

邮箱： info@ebiomall.com

美元价：$139.00

品牌： Xcess

公司：Xcess Biosciences, Inc

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Details

Product Information

Molecular Weight:	411.54
Formula:	C₂₃H₂₃N₅O₂
Purity:	>98%
CAS#:	354813-19-7
Solubility:	DMSO: ≥ 46 mg/mL
Chemical Name:	N-(1-((cyanomethyl)carbamoyl)cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide
Storage:	Powder -20^oC 3 years 4^oC 2 yearsIn solvent -80^oC 6 months-20^oC 1 month

Biological Activity:

Balicatib(AAE-581) is a potent and selective inhibitor of cathepsin K; 10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S. IC50 value: Target: cathepsin K The cathepsin K inhibitor AAE-581 (balicatib) as the most advanced of them passed Phase II clinical trials in 2005. Eighty adult female Macaca fascicularis underwent bilateral ovariectomies and were dosed twice daily by oral gavage with balicatib at 0, 3, 10, and 50 mg/kg for 18 months (groups O, L, M, H, respectively). Approximately 1 month after treatment initiation, the 50 mg/kg dose was decreased to 30 mg/kg. Twenty animals underwent sham-ovariectomies (group S). Bone mass was measured at 3-6 month intervals. At 18 months, vertebra and femur were collected for histomorphometry.

Reference:

[1]. Falgueyret JP, et al. Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J Med Chem. 2005 Dec 1;48(24):7535-43.

[2]. Vasiljeva O, et al. Emerging roles of cysteine cathepsins in disease and their potential as drug targets. Curr Pharm Des. 2007;13(4):387-403.

[3]. Jerome C, et al. Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys. Osteoporos Int. 2011 Dec;22(12):3001-11.

品牌介绍

Xcess Biosciences，Inc.（XcessBio）由一群来自学术界和制药/生物技术行业的顶尖科学家于2008年成立，他们在药物化学，生物化学，分子和细胞生物学领域拥有丰富的专业知识。结合我们的合作者和顾问网络，我们致力于开发高质量的产品并提供最佳的服务，以满足生物医学研究中未满足的需求。

XcessBio的总部位于加利福尼亚州圣地亚哥，在最先进的研发设施中运营，设有化学合成实验室，分子和细胞生物学实验室以及分析质量控制实验室。

XcessBio一直为美国许多顶级制药，生物技术和试剂公司提供CRO服务和OEM产品，现在，我们将最好的产品和服务直接扩展到整个生命科学界。

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