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SPR741 acetate Sale

(Synonyms: NAB741 acetate) 目录号 : GC38947

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。

SPR741 acetate Chemical Structure

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5mg
¥4,950.00
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10mg
¥6,750.00
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50mg
¥20,250.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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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.

Chemical Properties

Cas No. SDF
别名 NAB741 acetate
Canonical SMILES CC(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 tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 0.9504 mL 4.752 mL 9.5041 mL
5 mM 0.1901 mL 0.9504 mL 1.9008 mL
10 mM 0.095 mL 0.4752 mL 0.9504 mL
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