2. Anti-infection
  3. Bacterial
  4. AcrB-IN-6

AcrB-IN-6 是一种有效的 AcrB 抑制剂。AcrB-IN-6 能够抑制细菌多药外排泵的功能，从而显著增强多种抗生素的抗菌活性。AcrB-IN-6 在野生型大肠杆菌 BW25113 中可使最低抑菌浓度 (MIC) 降低 32 倍。AcrB-IN-6 表现出优异的协同抗菌作用、低细胞毒性和溶血性。AcrB-IN-6 可用于研究细菌耐药性。

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AcrB-IN-6

AcrB-IN-6 Chemical Structure

CAS No. : 3082621-32-4

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AcrB-IN-6 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AcrB-IN-6 is an effective AcrB inhibitor. AcrB-IN-6 The compound inhibits the function of bacterial multidrug efflux pumps, thereby significantly enhancing the antibacterial activity of various antibiotics. AcrB-IN-6 achieves 32-fold MIC reductions in wild-type E. coli BW25113. AcrB-IN-6 exhibits excellent synergistic antibacterial effects, low cytotoxicity and hemolytic properties. AcrB-IN-6 can be used for researching anti-resistant bacteria[1].

体外研究
(In Vitro)

AcrB-IN-6 (Compound 11i) (1-512 μg/mL) 对野生型 E. coli BW25113 或 BW25113 ΔAcrB 突变株均未显示出任何抗菌活性，但与包括 Linezolid (HY-10394), Oxacillin (HY-B0925A), Azithromycin (HY-17506), Erythromycin (HY-B0220), Tetracycline (HY-A0107), Fusidic acid (HY-B1350), Minocycline (HY-17412A), Ampicillin (HY-B0522) 和 Piperacillin (HY-B1923) 在内的六种不同抗生素表现出协同活性[1]。
AcrB-IN-6 (50 μM, 0-5 分钟) 可抑制野生型 E. coli BW25113 中的 Nile Red 外排活性[1]。
AcrB-IN-6 (128 μg/mL, 0-20 分钟) 不会破坏野生型 E. coli BW25113 的外膜通透性和内膜质子动力[1]。
AcrB-IN-6 (2-256 μg/mL) 不会引起小鼠红细胞溶血，并且对哺乳动物细胞的细胞毒性较低[1]。
Mcl-1-IN-16 (128 μg/mL, 0-12 小时) 可增强 Azithromycin 在 E. coli BW25113 中的抗生素后效应[1]。
Mcl-1-IN-16 (16-128 μg/mL, 24 小时) 与 Azithromycin 和 Linezolid 联用，对生物膜表现出显著的抑制效果[1]。

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

AcrB-IN-6 相关抗体:
体内研究
(In Vivo)

AcrB-IN-6 (Compound 11i) (5-25 mg/kg, 腹腔注射, 单次给药) 能显著增强 Tetracycline 在小鼠体内的抗菌活性，呈现出剂量依赖性的协同效应[1]。
AcrB-IN-6 (5-10 mg/kg, 腹腔注射, 应用于伤口, 持续 8 天) 能增强 Azithromycin 在清除小鼠皮肤感染细菌方面的功效[1]。
AcrB-IN-6 (250-1000 mg/kg, 血腔注射, 单次给药) 在 Galleria mellonella 幼虫模型中，即使在极高剂量下也表现出良好的安全性[1]。

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

Animal Model: E. coli BW25113 infection model established in male SPF Kunming (KM) mice (20-22 g)[1]
Dosage: 25 mg/kg (monotherapy); 5 and 15 mg/kg with Tetracycline
Administration: Intraperitoneal injection (i.p.), single dose
Result: Decreased CFU by approximately 0.5 log10 alone.
Proved a more remarkable effect with Tetracycline.
Animal Model: Skin would bacterial infection model established in male SPF Kunming (KM) mice (20-22 g)[1]
Dosage: 5 and 10 mg/kg with Azithromycin
Administration: Applied to the wound, once daily for 8 days
Result: Significantly reduced the bacterial load in the heart, liver, spleen, lungs and kidneys, and completely eliminate the bacteria in some organs.
Showed the same epidermal layer thickness and keratinization condition as normal skin, with no significant pathological changes.
Reduced the level of IL-6.
分子量

509.48

Formula

C28H33BrN2O2
CAS 号
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.
纯度 & 产品资料
参考文献

AcrB-IN-6 相关分类

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Keywords:

AcrB-IN-63082621-32-4Bacterial3,3-dimethyl-2,3,4,9-tetrahydro-1H-carbazolederivativesEfflux pump inhibitorAcrBAntibacterial sensitizing activityInhibitorinhibitorinhibit

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