SPR741 | 1179330-52-9

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: SPR741
• 英文别名: Spr741 (nab741)；(2S,3R)-2-acetamido-3-hydroxy-N-[(2R)-3-hydroxy-1-oxo-1-[[(3S,6S,9S,12S,15R,18S,21S)-6,9,18-tris(2-aminoethyl)-15-benzyl-3-[(1R)-1-hydroxyethyl]-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]propan-2-yl]butanamide
• CAS: 1179330-52-9
• 化学式: C₄₄H₇₃N₁₃O₁₃
• 分子量: 992.143
• InChiKey: JBFNEVNUGGFPBQ-DDMCRLCFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -4.1
• 重原子数：
  70
• 可旋转键数：
  18
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.64
• 拓扑面积：
  430
• 氢给体数：
  16
• 氢受体数：
  16

安全信息

• 储存条件：
  -20°C，密闭保存，干燥环境中使用

制备方法与用途

SPR741（NAB741）是一种源自多粘菌素B的阳离子肽，作为增效剂分子，能够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。这种化合物还能抑制具有多重耐药性的革兰氏阴性细菌。当与抗生素联合使用时，SPR741能扩展抗生素的作用范围。

文献信息

• POTENTIATION OF ANTIBIOTIC ACTIVITY BY A NOVEL CATIONIC PEPTIDE, SPR741
  申请人：SPERO POTENTIATOR, INC.

  公开号：US20190209645A1

  公开（公告）日：2019-07-11

  This disclosure provides a method of potentiating the efficacy of certain antibiotics by administering a therapeutically effect amount of the antibiotic in combination with SPR741. In certain embodiments the antibiotic is retapamulin, telithromycin, or aztreonam. The disclosure also provides a method of treating a bacterial infection by administering SPR741 in combination with a second antibiotic and pharmaceutical compositions comprising SPR741 and a second antibiotic.
• SPR741 HUMAN PHARMACOKINETICS AND EFFICACIOUS DOSE
  申请人：SPERO POTENTIATOR, INC.

  公开号：US20190192618A1

  公开（公告）日：2019-06-27

  This disclosure provides a method of treating a bacterial infection in a human patient comprising by administering a therapeutically effective dose of SPR741, a polymyxin analog, in combination with a therapeutically effective amount of an antibiotic other than SPR741. The disclosure establishes 100 mg to 500 mg of SPR741, administered 2 to 4 times daily as the effective amount of SPR741 for co-administration with a therapeutically effective amount of a second antibiotic. The disclosure also provides a method of treating a bacterial infection comprising administering 40 mg/kg patient weight/day or less and preferably 5 mg/kg patient weight/day or less of SPR741 in combination with a therapeutically effective amount of a second antibiotic.