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1076088-50-0

中文名称 化合物 WRR-483
英文名称 WRR483
CAS 1076088-50-0
分子式 C29H41N7O4S
分子量 583.75
MOL 文件 1076088-50-0.mol
1076088-50-0 结构式 1076088-50-0 结构式

基本信息

中文别名
化合物 WRR-483
英文别名
WRR483
1-Piperazinecarboxamide, N-[(1S)-4-[(aminoiminomethyl)amino]-1-[[[(1S)-1-(2-phenylethyl)-3-(phenylsulfonyl)-2-propen-1-yl]amino]carbonyl]butyl]-4-methyl-

应用领域

用途一
WRR-483, an analogue of K-11777, is a potent and selective cysteine protease inhibitor with trypanocidal activity in cell culture and animal model with comparable efficacy to K11777. WRR-483 demonstrates good potency against cruzain with sensitivity to pH conditions and high efficacy in the cell culture assay. Furthermore, WRR-483 also eradicates parasite infection in a mouse model of acute Chagas' disease. WRR-483 binds covalently to the active site cysteine of the protease in a similar manner as other vinyl sulfone-based inhibitors. WRR-483 has potential to be developed as a treatment for Chagas' disease.

常见问题列表

概述
WRR-483 是 K11777 的类似物,是克鲁兹蛋白酶(cruzain)的抑制剂,用于细胞培养中对克氏锥虫的增殖抑制。WRR-483 在急性恰加斯病小鼠模型中能根除寄生虫感染。WRR-483 是不可逆的半胱氨酸蛋白酶抑制剂,对克鲁兹蛋白酶和 T. cruzi 感染显示出 pH 依赖的高亲和力和有效的杀锥虫活性,有望抑制恰加斯病。
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