Relebactam 是一种二氮杂双环辛烷抑制剂，对广谱 β-内酰胺酶具有活性，包括 A 类（超广谱 β-内酰胺酶和 KPC）和 C 类 (AmpC) 酶。
| Cas No. | 1174018-99-5 |
| 别名 | 瑞来巴坦,MK-7655 |
| Canonical SMILES | O=S(ON1[C@]2([H])CC[C@@H](C(NC3CCNCC3)=O)[N@@](C2)C1=O)(O)=O |
| 分子式 | C12H20N4O6S |
| 分子量 | 348.38 |
| 溶解度 | Water : 72 mg/mL (206.67 mM) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 文献引用 | |
| 产品描述 | Relebactam is a diazabicyclooctane inhibitor with activity against a wide spectrum of β-lactamases, including class A (extended-spectrum β-lactamases [ESBLs] and KPC) and class C (AmpC) enzymes.Target: beta-lactamaseImipenem with Relebactam is active against Escherichia coli, Klebsiella pneumoniae, and Enterobacter spp., including K. pneumoniae carbapenemase (KPC)-producing isolates. The combination of Imipenem with Relebactam demonstrated activity against KPC-producing Enterobacteriaceae and multidrug-resistant P. aeruginosa. The imipenem MIC50 and MIC90 values for the ESBL-producing isolates were 0.25 and 0.5 ug/ml, respectively; with the addition of Relebactam, the corresponding values were 0.25 and 0.25 ug/ml. Five isolates harbored blaKPC. For these 5 isolates, the imipenem MICs ranged from 0.5 to >32 ug/ml. With the addition of Relebactam, the MICs decreased to 0.12 to 0.5 ug/ml.[1] Relebactam inhibits most class A and class C β-lactamases, with selected inhibition of class D enzymes by avibactam. β-Lactamase inhibitors (BLIs) have played an important role in combatting β-lactam resistance in Gram-negative bacteria, but their effectiveness has diminished with the evolution of diverse and deleterious varieties of β-lactamases.[2] References:
[1]. Lapuebla A, et al. Activity of Imipenem with Relebactam against Gram-Negative Pathogens from New York City. Antimicrob Agents Chemother. 2015 Aug;59(8):5029-31.
[2]. Bush K. A resurgence of β-lactamase inhibitor combinations effective against multidrug-resistant Gram-negative pathogens. Int J Antimicrob Agents. 2015 Nov;46(5):483-93. |
