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SPR741 TFA

CAS No. :

MCE 站：SPR741 TFA

产品活性：SPR741 TFA (NAB741 TFA) 是衍生自多粘菌素 B 的阳离子肽，是一种增效剂分子。SPR741 TFA 可提高革兰氏阴性细菌外膜的通透性，用于抑制严重的革兰氏阴性细菌感染。SPR741 TFA 抑制具有多重耐药性的革兰氏阴性细菌。当与抗生素结合使用时，SPR741 TFA 具有扩展抗生素活性谱的能力。

研究领域：Anti-infection

作用靶点：Bacterial  |  Antibiotic

In Vitro: SPR741 potentiates antibiotics that are substrates of the AcrAB-TolC efflux pump in E. coli, effectively circumventing the contribution of this pump to intrinsic antibiotic resistance. The intrinsic resistance of E. coli to certain antibiotics that is mediated by both the outer membrane ａnd the AcrAB-TolC efflux system can be overcome, or circumvented, by combining the antibiotic with SPR741 but that potentiation of intrinsic resistance due primarily to efflux may be limited.
SPR741 lacks significant antibacterial activity as a stand-alone agent but interacts with the outer membrane of Gram-negative bacteria to increase permeability ａnd thereby improve the accumulation of coadministered antibiotics inside the pathogen.

In Vivo: SPR741 has the ability to permeabilize the outer membrane of Gram-negative bacteria, thus sensitizing them to hydrophobic antibiotics. SPR741 has a significantly safety profile of compared to that of polymyxin B, which suffers severe, dose-limiting nephrotoxicity in humans. In multiday rodent ａnd nonhuman primate studies, polymyxin B exhibited nephrotoxicity at a far-lower exposure-normalized dose than SPR741.

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