| Description | Deferitazole (FBS 0701) is a novel and orally active, selective and high affinity iron chelator. |
| In vitro | Deferitazole (FBS0701) 对铁(III)具有高亲和力和选择性,其表现为 logβ2 = 33.39 ± 0.03 及 pFe(3+) 值为 22.3。在生物条件下,铁(III)复合物存在两种平衡的异构体形式。Deferitazole 也能高亲和地结合三价金属Al(III)和La(III),其 logβ2 值分别为 26.68 和 21.55。与二价阳离子相比,Deferitazole 的亲和力略低,但对Cu(II)的例外,其 logβ2 值为 25.5;Deferitazole 能够从柠檬酸和白蛋白等动态来源中清除铁,其效率与其他治疗性铁螯合剂,包括 deferasirox、deferiprone 和 desferrioxamine 相当。Fe(III)(Deferitazole)2 在生理条件下稳定且不进行氧化还原循环。Deferitazole 对铁(III)的高亲和力使其不大可能导致铁的重新分布,因此显示出作为治疗性铁(III)螯合剂的巨大潜力。 |
| Synonyms | SPD602, FBS 0701, SPD-602, FBS0701, FBS-0701, SPD 602 |
| molecular weight | 399.46 |
| Molecular formula | C18H25NO7S |
| CAS | 945635-15-4 |
| Storage | store at low temperature|Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (125.17 mM) |
| References | 1. Hider RC, et al. Deferitazole, a new orally active iron chelator. Dalton Trans. 2015 Mar 21;44(11):5197-204. 2. Ferrer P, et al. Antimalarial iron chelator FBS0701 blocks transmission by Plasmodium falciparum gametocyte activation inhibition. Antimicrob Agents Chemother. 2015 Mar;59(3):1418-26. 3. Gumienna-Kontecka E, et al. Iron chelating strategies in systemic metal overload, neurodegeneration and cancer. Curr Med Chem. 2014;21(33):3741-67. 4. Ferrer P, et al. Antimalarial iron chelator, FBS0701, shows asexual and gametocyte Plasmodium falciparum activity and single oral dose cure in a murine malaria model. PLoS One. 2012;7(5):e37171. |