SPR741(Synonyms: NAB741)

SPR741;(Synonyms: NAB741)

SPR741 (NAB741) 是衍生自多粘菌素 B 的阳离子肽,是一种增效剂分子。SPR741 可提高革兰氏阴性细菌外膜的通透性,用于严重的革兰氏阴性细菌感染的研究。SPR741 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 具有扩展抗生素活性谱的能力。

SPR741amp;;(Synonyms: NAB741)

SPR741 Chemical Structure

CAS No. : 1179330-52-9

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SPR741 的其他形式现货产品:

SPR741 acetate

生物活性

SPR741 (NAB741) is a cationic peptide derived from polymyxin B and is a potentiator molecule. SPR741 increases the permeability of the outer membrane of Gram-negative bacteria and is used to treat severe Gram-negative bacteria infections. SPR741 inhibits multidrug-resistant Gram-negative bacteria. The spectrum of activity of the antibiotic can be widened when used in combination with SPR741[1][2].

体外研究
(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[1].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

992.13

Formula

C44H73N13O13

CAS 号

1179330-52-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Corbett D, et al. Potentiation of Antibiotic Activity by a Novel Cationic Peptide: Potency and Spectrum of Activity of SPR741. Antimicrob Agents Chemother. 2017 Jul 25;61(8). pii: e00200-17.

    [2]. Eckburg PB, et al. Safety, Tolerability, Pharmacokinetics, and Drug Interaction Potential of SPR741, an Intravenous Potentiator, after Single and Multiple Ascending Doses and When Combined with β-Lactam Antibiotics in Healthy Subjects. Antimicrob Agents Chemother. 2019 Aug 23;63(9). pii: e00892-19.