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SPR741 acetate
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
SPR741 acetate图片
包装与价格：
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
SPR741 acetate (NAB741 acetate) 是衍生自多粘菌素 B 的阳离子肽，是一种增效剂分子。SPR741 acetate 可提高革兰氏阴性细菌外膜的通透性，用于治疗严重的革兰氏阴性细菌感染。SPR741 acetate 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 acetate 具有扩展抗生素活性谱的能力。
别名NAB741 acetate
Canonical SMILESCC(N[C@@H]([C@H](O)C)C(N[C@H](CO)C(N[C@@H](CCNC([C@](N1)([H])[C@H](O)C)=O)C(N[C@@H](CCN)C(N[C@@H](C(N[C@H](C(N[C@H](C(N[C@@H](CCN)C1=O)=O)CCN)=O)CC(C)C)=O)CC2=CC=CC=C2)=O)=O)=O)=O)=O.CC(O)=O
分子式C46H77N13O15
分子量1052.18
溶解度DMSO: 130 mg/mL (123.55 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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

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].

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].

[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.