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Cardioxane (ADR-529) 是一种心脏保护剂。
Cardioxane (ADR-529) 是一种心脏保护剂。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 257 | 现货 | |
10 mg | ¥ 413 | 现货 | |
25 mg | ¥ 632 | 现货 | |
50 mg | ¥ 813 | 现货 | |
100 mg | ¥ 1,120 | 现货 | |
200 mg | ¥ 1,660 | 现货 | |
500 mg | ¥ 2,790 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 293 | 现货 |
产品描述 | Cardioxane (ADR-529) is a cardio-protective drug. |
体外活性 | Dexrazoxane(10 mM),临床上已知可限制蒽环类化合物引起的心脏毒性,可以预防多柔比星引发的心肌细胞凋亡,但对于高浓度蒽环类化合物引起的坏死则无效。[1] Dexrazoxane通过结合游离态或松散结合的铁,或与多柔比星形成的铁复合物,从而防止或减少特定位置的氧基团产生,这种氧基团会损害细胞成分,推测其发挥心脏保护作用。[2] Dexrazoxane专门消除多柔比星引起的DNA损伤信号gamma-H2AX,但对坎普地星或过氧化氢则无效,在H9C2心肌细胞中。它还能快速降解Top2beta,与多柔比星引起的DNA损伤的减少相对应。Dexrazoxane通过干扰Top2beta抵消多柔比星引起的DNA损伤,这可能意味着Top2beta在多柔比星引起的心脏毒性中起作用。[3] Dexrazoxane在细胞内被水解为活性形式并结合铁,以防止超氧化物自由基的形成,从而防止线粒体破坏。[4] |
体内活性 | Dexrazoxane 结合 doxorubicin、daunorubicin 或 idarubicin 在 B6D2F1 小鼠中减少了组织损伤(以伤口大小与持续时间曲线下面积表示),分别降低了96%、70%、和87%。此外,Dexrazoxane 的联合使用显著降低了小鼠出现伤口的比例及伤口持续的时间。[5] |
激酶实验 | HTRF assay: Homogeneous time-resolved fluorescence (HTRF) assay measures the signal generated by 2 components when they are in close proximity. The p53–MDM2 binding assay uses a biotinylated peptide derived from the MDM2-binding domain of p53 and a truncated N-terminal portion of recombinant human GST-tagged MDM2 protein containing the p53-binding domain. Proteins for crystal structure studies are expressed in E. coli strain BL21 using the helper plasmid pUBS 520 coding for the lacIq repressor and the rare tRNAArg [AGA/AGG]. For crystallization, the frozen protein is thawed and concentrated to 9.8 mg/mL using a Centricon concentrator (3,000 MW cutoff). The complex is then formed by combining the protein with a slight molar excess of the inhibitor (stock solution is 100 mM in DMSO) and this solution is allowed to sit for 4 hours at 4°C. Cryopreserved crystals are used to collect diffraction data on beamline X8C at the National Synchrotron Light Source at Brookhaven National Laboratory. |
别名 | 右雷佐生盐酸盐, ICRF-187 hydrochloride, ICRF-187, Dexrazoxane HCl, Cardioxane hydrochloride, ADR-529 Hydrochloride, ADR-529 |
分子量 | 304.73 |
分子式 | C11H16N4O4·HCl |
CAS No. | 149003-01-0 |
Smiles | Cl.CC(CN1CC(=O)NC(=O)C1)N1CC(=O)NC(=O)C1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: 55 mg/mL (180.5 mM) DMSO: 50 mg/mL (164.08 mM), Sonication is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
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