货号:A602643 同义名: Loxistatin acid;NSC 694279
Loxistatin acid, a derivative of E-64, is an irreversible and membrane-permeant cysteine protease inhibitor.
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产品名称 | Cysteine Protease ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Z-FA-FMK | ✔ | 99%+ | |||||||||||||||||
Leupeptin hemisulfate | ✔ | 97% | |||||||||||||||||
PMSF | ✔ | 95% | |||||||||||||||||
PD 151746 |
+
μ-Calpain, IC50: 260 nM m-calpain, IC50: 5.33 μM |
98% | |||||||||||||||||
Odanacatib |
++++
Cathepsin K (rabbit), IC50: 1 nM Cathepsin K (human), IC50: 0.2 nM |
99%+ | |||||||||||||||||
E-64 |
+++
Cysteine protease, IC50: 9 nM |
99%+ | |||||||||||||||||
E 64c | ✔ | 95% | |||||||||||||||||
E-64d | ✔ | 99%+ | |||||||||||||||||
MG-101 | ✔ | 98%+ | |||||||||||||||||
Calpeptin |
++
Calpain II (porcine kidney), ID50: 40 nM Calpain I (porcine erythrocytes), ID50: 52 nM |
98%+ | |||||||||||||||||
Cathepsin inhibitor 1 |
+++
Cathepsin L2, pIC50: 5.5 Cathepsin L, pIC50: 7.9 |
98% | |||||||||||||||||
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。 |
靶点 |
|
描述 | E-64c is a derivative of a naturally occurring epoxide that inhibits cysteine proteases, particularly effective against papain. This inhibition is characterized by the hydrogen bonding and hydrophobic interactions between the ligands and the conserved residues within the catalytic binding site[1]. E-64c has been identified as a primary structure for the creation of irreversible inhibitors targeting cathepsin C[2]. |
Animal study | The half-life (t-1/2) of E-64c in plasma is 0.48 hours. At this dosage, E-64c does not exhibit hemodynamic effects. Statistical analysis using two-way ANOVA reveals that both reperfusion and E-64c independently have significant effects on infarct size. The reduction in creatine phosphokinase (CPK) is marginally lower in the E-64c treated groups compared to the vehicle-injected groups. The limited efficacy of E-64c might be due to its early administration and the relatively short half-life. Given the established effectiveness of NCO-700, the results suggest that E-64c may have a modest yet positive impact on reducing infarct size and CPK levels[3]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.18mL 0.64mL 0.32mL |
15.90mL 3.18mL 1.59mL |
31.81mL 6.36mL 3.18mL |
CAS号 | 76684-89-4 |
分子式 | C15H26N2O5 |
分子量 | 314.377 |
别名 | Loxistatin acid;NSC 694279;EP 475 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 250 mg/mL(795.22 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |