| 中文名称: | CA-074 | ||||
|---|---|---|---|---|---|
| 英文名称: | CA-074 | ||||
| 别名: | (S)-1-((2S,3S)-3-甲基-2-((2S,3S)-3-(丙基氨基甲酰基)环氧乙烷-2-甲酰胺基)戊酰基)吡咯烷-2-羧酸 (2S)-1-[(2S,3S)-3-Methyl-2-{[(2S,3S)-3-(propylcarbamoyl)oxiran-2-yl]formamido}pentanoyl]pyrrolidine-2-carboxylic acid | ||||
| CAS No: | 134448-10-5 | 分子式: | C18H29N3O6 | 分子量: | 383.44 |
| CAS No: | 134448-10-5 | ||||
| 分子式: | C18H29N3O6 | ||||
| 分子量: | 383.44 | ||||
基本信息
|
产品编号： |
C11259 |
||||
|
产品名称： |
CA-074 |
||||
|
CAS: |
134448-10-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
|
|
|
||||
|
分子式： |
溶于液体 |
-80℃ |
六个月 |
||
|
分子量 |
383.44 |
-20℃ |
一个月 |
||
|
化学名： |
(2S)-1-[(2S,3S)-3-Methyl-2-{[(2S,3S)-3-(propylcarbamoyl)oxiran-2-yl]formamido}pentanoyl]pyrrolidine-2-carboxylic acid |
||||
|
Solubility (25°C)： |
|||||
|
体外:
|
DMSO |
125mg/mL(326.00mM;Need ultrasonic) |
|||
|
Ethanol |
|
||||
|
Water |
|
||||
|
体内(现配现用): |
1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.08mg/mL(5.42mM);Clear solution |
||||
|
此⽅案可获得≥2.08mg/mL(5.42mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄清DMSO储备液加到400μL PEG300中，混合均匀；向上述体系中加⼊50μL Tween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。 |
|||||
|
2.请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline) Solubility:≥2.08mg/mL(5.42mM);Clear solution |
|||||
|
此⽅案可获得≥2.08mg/mL(5.42mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄清DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中，混合均匀。 |
|||||
|
3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility:≥2.08mg/mL(5.42mM);Clear solution |
|||||
|
此⽅案可获得≥2.08mg/mL(5.42mM，饱和度未知)的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL20.8mg/mL的澄清DMSO储备液加到900μL⽟⽶油中，混合均匀。 |
|||||
|
＜1mg/ml表示微溶或不溶。 |
|||||
|
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
|||||
|
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
|||||
制备储备液
|
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
|
1mM |
2.6080mL |
13.0399mL |
26.0797mL |
|
5mM |
0.5216mL |
2.6080mL |
5.2159mL |
|
10mM |
0.2608mL |
1.3040mL |
2.6080mL |
生物活性
|
产品描述 |
一种组织蛋白酶B (cathepsin B) 的有效抑制剂。 |
|
靶点 |
Ki: 2 to 5nM (Cathepsin B) |
|
体外研究 |
CA-074 is a synthetic analogue of E-64, a natural peptidyl epoxide that irreversibly inhibits most known lysosomal cysteine proteinases, and is developed by means of rational drug design, exploiting the dipeptidylcarboxypeptidase activity of cathepsin B. CA-074 can be used to selectively inhibit cathepsin B within living cells, as long as the experimental conditions permit significant fluid-phase endocytosis of the drug. CA-074 inhibits cathepsin B with a Ki of 2 to 5nM, whereas the initial Kis for cathepsin H and L are about 40-200μM. CA-074 exhibits 10000-30000 times greater inhibitory effects on purified rat cathepsin B than on cathepsin H and L |
|
体内研究 |
Intraperitoneally injection of compound CA-074 into rats potently and selectively inhibits cathepsin B activity. Intravenously administration of CA-074 immediately after the ischaemic insult saves 67% of CA1 neurons from delayed neuronal death on day 5 in eight monkeys undergoing 20 min brain ischaemia: the extent of inhibition is excellent in three of eight and good in five of eight monkeys |
推荐实验方法(仅供参考)
|
Animal Administration |
Rats: Compound CA-074 or CA-030 or E-64 is injected intraperitoneally as a solution in saline containing DMSO. A dose of 8 mg/100g body weight is injected. The rats are killed by a blow to the head 6 h after the injection, and their liver is perfused with saline, removed, weighed and chilled on ice. Samples of 4 g of liver are minced and homogenized. The homogenate is centrifuged at 800 xg for 15 min and the supernatant is centrifuged at 12000 xg for 30 min. The precipitate is suspended in 2mL of 0.05M acetate buffer, pH 5,0, and freeze-thawed for measurements of cathepsin B, H and L activities |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
