Cathepsin L Inhibitor

A potent and selective cathepsin L inhibitor

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库存: 现货

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5mg

￥1787.00

1430.00

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10mg

￥2862.00

2290.00

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25mg

￥5700.00

4560.00

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50mg

￥9262.00

7410.00

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100mg

￥14687.00

11750.00

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货号: ajci21238
CAS: 167498-29-5
别名: SB 412515; Z-FY-CHO
分子式: C26H26N2O5
分子量: 446.5
纯度: >98%
溶解度: 20 mg/ml in DMSO, 20 mg/ml in DMF, 2 mg/ml in Ethanol
储存: Store at -20°C
库存: 现货

Background

Cathepsin L inhibitor is a potent inhibitor of cathepsin L (IC50 = 0.85 nM). [1]? It is selective for cathepsin L over calpain II and cathepsin B (IC50s = 184, and 85.1 nM, respectively). It is trypanocidal with an ED50 value of 45 nM against T. brucei that is well below the ED50 value of 21,500 nM for human HL-60 cells. [2] Cathepsin L inhibitor completely suppresses osteoclastic pit formation on femur slices isolated from bovine cortical bone at a concentration of 1 μg/ml., [1][3] In vivo, cathepsin L inhibitor (2.5-10 mg/kg) inhibits bone loss in a mouse model of osteoporosis in a dose-dependent manner.

Reference:
[1]. Woo, J.-T., Sigeizumi, S., Yamaguchi, K., et al. Peptidyl aldehyde derivatives as potent and selective inhibitors of cathepsin L. Bioorganic Med. Chem. Lett. 5(14), 1501-1504 (1995).
[2]. Nkemngu, N.J., Grande, R., Hansell, E., et al. Improved trypanocidal activities of cathepsin L inhibitors. Int. J. Antimicrob. Agents 22(2), 155-159 (2003).
[3]. Woo, J.-T., Yamaguchi, K., Hayama, T., et al. Suppressive effect of N-(benzyloxycarbonyl)-L-phenylalanyl-L-tyrosinal on bone resorption in vitro and in vivo. Eur. J. Pharmacol. 300(1-2), 131-135 (1996).