A radioprotective agent
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DMA is a bisbenzimidazole radioprotective agent.1,2 In vivo, DMA (300 mg/kg) decreases radiation-induced lethality without affecting radiation-induced tumor regression in an Ehrlich murine spontaneous adenocarcinoma model.1 It prevents radiation-induced damage of intestinal, hepatic, and splenic tissues, increases in splenic malondialdehyde (MDA) production, and decreases in splenic superoxide dismutase (SOD) activity in a B16/F10 murine melanoma model when administered at a dose of 50 mg/kg.2
1.Nimesh, H., Tiwari, V., Yang, C., et al.Preclinical evaluation of DMA, a bisbenzimidazole, as radioprotector: Toxicity, pharmacokinetics, and biodistribution studies in Balb/c miceMol. Pharmacol.88(4)768-778(2015) 2.Tiwari, V., Kamran, M.Z., Ranan, A., et al.Akt1/NFκB signaling pathway activation by a small molecule DMA confers radioprotection to intestinal epithelium in xenograft modelFree Rad. Biol. Med.108564-574(2017)
Cell experiment: | Various human tumor cells (U87, HeLa and MCF7) are maintained as monolayer at 37°C in 5% CO2 using DMEM medium. Approximately 3000-8000 cells/well are seeded in 96-well plates containing 200 μL of medium and incubated for 24 h. The culture medium is replaced by fresh medium containing 1, 10, 50, 100 μM of DMA (6c) and incubated for 24, 48 and 72 h. The cell viability is determined by the MTT assay. The light absorbance is measured using a microplate reader[1]. |
参考文献: [1]. Singh M, et al. Synthesis and biological activity of novel inhibitors of topoisomerase I: 2-aryl-substituted 2-bis-1H-benzimidazoles. Eur J Med Chem. 2011 Feb;46(2):659-69. |
DMNPE-caged ATP diammonium salt
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