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組織蛋白酶L抑制劑是組織蛋白酶的強效抑制劑,其IC50為0.85 nM。它對布魯氏菌具有45nM的ED50值的錐蟲殺性,該ED50值遠低于人HL-60細胞21500nM的ED 50值。
編號:147230
CAS號:167498-29-5
單字母:Z-FY-CHO
編號: | 147230 |
中文名稱: | 組織蛋白酶L抑制劑:Cathepsin L Inhibitor |
英文名: | Cathepsin L Inhibitor |
CAS號: | 167498-29-5 |
單字母: | Z-FY-CHO |
三字母: | Cbz N端Cbz保護 -PheL-苯丙氨酸:phenylalanine。系統(tǒng)命名為(2S)-氨基-3-苯基丙酸。是編碼氨基酸。是哺乳動物的必需氨基酸。符號:F,Phe。 -TyrL-酪氨酸:tyrosine。系統(tǒng)命名為(2S)-氨基-3-(4-羥基苯基)丙酸。是編碼氨基酸。符號:Y,Tyr。 -CHOC端醛基化 |
氨基酸個數(shù): | 2 |
分子式: | C26H26O5N2 |
平均分子量: | 446.5 |
精確分子量: | 446.18 |
等電點(PI): | - |
pH=7.0時的凈電荷數(shù): | 1 |
平均親水性: | -2.95 |
疏水性值: | 0.95 |
消光系數(shù): | 1490 |
來源: | 人工化學合成,僅限科學研究使用,不得用于人體。 |
鹽體系: | 可選TFA、HAc、HCl或其它 |
儲存條件: | 負80℃至負20℃ |
標簽: | 醛肽 CBZ修飾肽 二肽(Dipeptide) |
Z-Phe-酪氨酸是一種有效的選擇性組織蛋白酶L抑制劑。在用未分級的大鼠骨細胞進行的凹坑形成測定中,1.5nM的Z-FY-CHO顯著抑制甲狀旁腺激素刺激的破骨細胞性骨吸收。在去卵巢的小鼠中,它以2.5-10 mg/kg/天的ip劑量依賴性地抑制四周的骨重量減輕。
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.
組織蛋白酶L抑制劑是組織蛋白酶的強效抑制劑,其IC50為0.85 nM。它對布魯氏菌具有45nM的ED50值的錐蟲殺性,該ED50值遠低于人HL-60細胞21500nM的ED 50值。在體內(nèi),組織蛋白酶L抑制劑(2.5-10 mg/kg)以劑量依賴性方式抑制骨質疏松小鼠模型中的骨丟失。組織蛋白酶L抑制劑還可以完全抑制從牛皮質骨分離的股骨切片上破骨細胞凹坑的形成。
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 | 名稱 | |
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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 | 下載 |
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 | 下載 |
10.1016/0014-2999(95)00858-6 | Suppressive effect of N-(benzyloxycarbonyl)-L-phenylalanyl-L-tyrosinal on bone resorption in vitro and in vivo | 下載 |
10.1016/s0924-8579(03)00096-7 | Improved trypanocidal activities of cathepsin L inhibitors | 下載 |