右雷佐生盐酸盐 T6467

Product Introduction
Bioactivity


英文名: Cardioxane

描述: Cardioxane (ADR-529) 是一种心脏保护剂。

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.

体外活性: Dexrazoxane (10 mM), known clinically to limit anthracycline cardiac toxicity, prevents daunorubicin-induced myocyte apoptosis, but not necrosis induced by higher anthracycline concentrations in rat cardiac myocytes. [1] Dexrazoxane presumably exerts its cardioprotective effects by either binding free or loosely bound iron, or iron complexed to doxorubicin, thus preventing or reducing site-specific oxygen radical production that damages cellular components. [2] Dexrazoxane specifically abolishes the DNA damage signal gamma-H2AX induced by doxorubicin, but not camptothecin or hydrogen peroxide, in H9C2 cardiomyocytes. Dexrazoxane also induces rapid degradation of Top2beta, which paralleles the reduction of doxorubicin-induced DNA damage. Dexrazoxane antagonizes doxorubicin-induced DNA damage through its interference with Top2beta, which could implicate Top2beta in doxorubicin cardiotoxicity. [3] Dexrazoxane is hydrolyzed to its active form intracellularly and binds iron to prevent the formation of superhydroxide radicals, thus preventing mitochondrial destruction. [4]

体内活性: Dexrazoxane combined with doxorubicin, daunorubicin, or idarubicin reduces the tissue lesions in B6D2F1 mice (expressed as area under the curve of wound size times duration) by 96%, 70%, and 87%, respectively. Dexrazoxane combined with doxorubicin, daunorubicin, or idarubicin results in a statistically significant reduction in the fraction of mice with wounds as well as the duration of wounds. [5]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 55 mg/mL (180.5 mM)
DMSO : 56 mg/mL (183.8 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: Dexrazoxane | ICRF 187 | inhibit | Cardioxane Hydrochloride | Inhibitor | NSC-169780 | Dexrazoxane hydrochloride | ADR 529 | ICRF187 | ADR 529 Hydrochloride | NSC 169780 | ICRF 187 Hydrochloride | NSC169780 | ADR529 Hydrochloride | Cardioxane | ADR529 | ICRF187 Hydrochloride | ICRF-187 Hydrochloride

相关产品: Topixantrone 2HCl | Lupalbigenin | Amsacrine hydrochloride | (4-NH2)-Exatecan | Doxorubicin hydrochloride | (±)-10-Hydroxycamptothecin | Belotecan hydrochloride | Ellagic acid | α-Lapachone | Bisantrene

相关库: Drug Repurposing Compound Library | Approved Drug Library | Clinical Compound Library | Ferroptosis Compound Library | Pediatric Drug Library | DNA Damage & Repair Compound Library | EMA Approved Drug Library | Preclinical Compound Library | NO PAINS Compound Library | Bioactive Compound Library

右雷佐生盐酸盐 T6467信息由TargetMol中国为您提供，如您想了解更多关于右雷佐生盐酸盐 T6467报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途