组织蛋白酶L抑制剂是组织蛋白酶的强效抑制剂,其IC50为0.85 nM。它对布鲁氏菌具有45nM的ED50值的锥虫杀性,该ED50值远低于人HL-60细胞21500nM的ED 50值。
编号:147230
CAS号:167498-29-5
单字母:Z-FY-CHO
编号: | 147230 |
中文名称: | 组织蛋白酶L抑制剂:Cathepsin L Inhibitor |
英文名: | Cathepsin L Inhibitor |
CAS号: | 167498-29-5 |
单字母: | Z-FY-CHO |
三字母: | Cbz N端Cbz保护 -Phe苯丙氨酸 -Tyr酪氨酸 -CHOC端醛基化 |
氨基酸个数: | 2 |
分子式: | C26H26O5N2 |
平均分子量: | 446.5 |
精确分子量: | 446.18 |
等电点(PI): | - |
pH=7.0时的净电荷数: | 1 |
平均亲水性: | -2.95 |
疏水性值: | 0.95 |
消光系数: | 1490 |
来源: | 人工化学合成,仅限科学研究使用,不得用于人体。 |
盐体系: | 可选TFA、HAc、HCl或其它 |
储存条件: | 负80℃至负20℃ |
标签: | 醛肽 CBZ修饰肽 二肽(Dipeptide) |
Z-Phe-酪氨酸是一种有效的选择性组织蛋白酶L抑制剂。在用未分级的大鼠骨细胞进行的凹坑形成测定中,1.5nM的Z-FY-CHO显著抑制甲状旁腺激素刺激的破骨细胞性骨吸收。在去卵巢的小鼠中,它以2.5-10 mg/kg/天的ip剂量依赖性地抑制四周的骨重量减轻。
Z-Phe-Tyrosinal is a potent and selective cathepsin L inhibitor. In the pit formation assay with unfractionated rat bone cells, 1.5 nM of Z-FY-CHO markedly inhibited parathyroid hormone-stimulated osteoclastic bone resorption. In ovariectomized mice, it suppressed at 2.5-10 mg/kg/day ip for four weeks bone weight loss dose-dependently.
组织蛋白酶L抑制剂是组织蛋白酶的强效抑制剂,其IC50为0.85 nM。它对布鲁氏菌具有45nM的ED50值的锥虫杀性,该ED50值远低于人HL-60细胞21500nM的ED 50值。在体内,组织蛋白酶L抑制剂(2.5-10 mg/kg)以剂量依赖性方式抑制骨质疏松小鼠模型中的骨丢失。组织蛋白酶L抑制剂还可以完全抑制从牛皮质骨分离的股骨切片上破骨细胞凹坑的形成。
Cathepsin L inhibitor is a potent inhibitor of cathepsin L with IC50 of 0.85 nM. 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. In vivo, cathepsin L inhibitor (2.5-10 mg/kg) inhibits bone loss in a mouse model of osteoporosis in a dose-dependent manner. Cathepsin L inhibitor can also completely suppress osteoclastic pit formation on femur slices isolated from bovine cortical bone.
DOI | 名称 | |
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10.1515/BC.2004.082 | Cathepsin L is involved in cathepsin D processing and regulation of apoptosis in A549 human lung epithelial cells | 下载 |
10.1111/j.1460-9568.2005.04279.x | Up-regulation of lysosomal cathepsin L and autophagy during neuronal death induced by reduced serum and potassium | 下载 |
10.1016/0014-2999(95)00858-6 | Suppressive effect of N-(benzyloxycarbonyl)-L-phenylalanyl-L-tyrosinal on bone resorption in vitro and in vivo | 下载 |
10.1016/s0924-8579(03)00096-7 | Improved trypanocidal activities of cathepsin L inhibitors | 下载 |