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CA-074 methyl ester
CA-074 methyl ester
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货号：A917874
同义名：
CA-074Me;Cathepsin B Inhibitor IV
CA-074 methyl ester是一种特异性的半胱氨酸蛋白 酶B抑制剂，具有神经保护、抗癌和抗炎 等强效生物活性。
CA-074 methyl ester 化学结构
CA-074 methyl ester 3D分子结构
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CA-074 methyl ester 质控信息
Z-FA-FMK
✔
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Leupeptin hemisulfate
✔
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PMSF
✔
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PD 151746
+
m-calpain, IC50: 5.33 μM
μ-Calpain, IC50: 260 nM
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Odanacatib
++++
Cathepsin K (rabbit), IC50: 1 nM
Cathepsin K (human), IC50: 0.2 nM
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E-64
+++
Cysteine protease, IC50: 9 nM
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E 64c
✔
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E-64d
✔
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MG-101
✔
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Calpeptin
++
Calpain II (porcine kidney), ID50: 40 nM
Calpain I (porcine erythrocytes), ID50: 52 nM
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Cathepsin inhibitor 1
+++
Cathepsin L2, pIC50: 5.5
Cathepsin L, pIC50: 7.9
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
CA-074 methyl ester 生物活性
描述
CA-074 is a selective cathepsin B inhibitor with Ki value about 2-5nM for purified rat cathepsin B, 10000~30000 times greater than the Ki values for cathepsin H and L. Intraperitoneal injection of 8mg CA-074 into rats potently inhibited cathepsin B in vivo [3] [4]
CA-074 methyl ester 动物研究
Dose
Mice: 10 mg/kg[3]
Administration
i.v.
CA-074 methyl ester 参考文献
[1] Towatari T, Nikawa T, et al. Novel epoxysuccinyl peptides. A selective inhibitor of cathepsin B, in vivo. FEBS Lett. 1991 Mar 25;280(2):311-5.
[2] Withana NP, Blum G, et al. Cathepsin B inhibition limits bone metastasis in breast cancer. Cancer Res. 2012 Mar 1;72(5):1199-209.
[3] Towatari T, Nikawa T, Murata M, Yokoo C, Tamai M, Hanada K, Katunuma N. Novel epoxysuccinyl peptides. A selective inhibitor of cathepsin B, in vivo. FEBS Lett. 1991 Mar 25;280(2):311-5. doi: 10.1016/0014-5793(91)80319-x. PMID: 2013329.
[4] Withana NP, Blum G, Sameni M, Slaney C, Anbalagan A, Olive MB, Bidwell BN, Edgington L, Wang L, Moin K, Sloane BF, Anderson RL, Bogyo MS, Parker BS. Cathepsin B inhibition limits bone metastasis in breast cancer. Cancer Res. 2012 Mar 1;72(5):1199-209. doi: 10.1158/0008-5472.CAN-11-2759. Epub 2012 Jan 19. PMID: 22266111; PMCID: PMC3538126.
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CA-074 methyl ester 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.52mL
0.50mL
0.25mL
12.58mL
2.52mL
1.26mL
25.16mL
5.03mL
2.52mL
CA-074 methyl ester 技术信息
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