AcrB-IN-6
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.
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- CAS No.: 3082621-32-4
- 화학식: C28H33BrN2O2
- 분자량:509.48
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
AcrB-IN-6 (Compound 11i) (1-512 μg/mL) does not show any antibacterial activity against wild-type E. coli<.i> BW25113 or the BW25113 ΔAcrB mutant but demonstrates synergistic activity with six distinct antibiotics included 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) and Piperacillin (HY-B1923)[1].
AcrB-IN-6 (50 μM, 0-5 min) inhibits Nile Red activity in wild-type E. coli BW25113[1].
AcrB-IN-6 (128 μg/mL, 0-20 min) does not disrupt the outer membrane permeability and and inner membrane proton motive force of the wild-type E. coli BW25113[1].
AcrB-IN-6 (2-256 μg/mL) does not cause hemolysis of mouse red blood cells and is low cytotoxicity toward mammalian cells[1].
Mcl-1-IN-16 (128 μg/mL, 0-12 h) enhances the post-antibiotic effect of Azithromycin in E. coli BW25113[1].
Mcl-1-IN-16 (16-128 μg/mL, 24 h) combined with Azithromycin and Linezolid exhibits significantly inhibitory effect on biofilm[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Cmax | Tmax | AUC0-t | AUC0-∞ | CL | MRT0-t | MRT0-∞ | F |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 0.5 mg/kg | i.v. | 10.45 h | 361.26 ng/mL | 0.25 h | 1623 ng·h/mL | 4824.16 ng·h/mL | 207.24 mL/h/kg | 2.73 h | 14.90 h | / |
| Mice[1] | 1 mg/kg | i.v. | 12.73 h | 358.20 ng/mL | 0.25 h | 1612.74 ng·h/mL | 5679.26 ng·h/mL | 177.55 mL/h/kg | 2.75 h | 18.23 h | / |
| Mice[1] | 1.5 mg/kg | i.v. | 12.54 h | 360.20 ng/mL | 0.25 h | 1634.08 ng·h/mL | 5689.69 ng·h/mL | 175.92 mL/h/kg | 2.75 h | 17.96 h | / |
| Mice[1] | 2.5 mg/kg | i.p. | 9.89 h | 944.68 ng/mL | 0.50 h | 2866.06 ng·h/mL | 8292.25 ng·h/mL | 608.42 mL/h/kg | 2.74 h | 14.20 h | / |
| Mice[1] | 5 mg/kg | i.p. | 9.12 h | 964.90 ng/mL | 0.50 h | 2947.62 ng·h/mL | 8074.07 ng·h/mL | 627.47 mL/h/kg | 2.72 h | 15.47 h | 35.54 % |
| Mice[1] | 7.5 mg/kg | i.p. | 10.75 h | 918.02 ng/mL | 0.50 h | 2841.59 ng·h/mL | 8826.55 ng·h/mL | 570.45 mL/h/kg | 2.74 h | 13.13 h | / |
AcrB-IN-6 (5-10 mg/kg, i.p., applied to the wound, for 8 days) enhances the efficacy of Azithromycin in eliminating bacteria during skin infections in mice[1].
AcrB-IN-6 (250-1000 mg/kg, injected in the hemocoel, single dose) demonstrated good safety even at extremely high doses in the Galleria mellonella larvae[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:E. coli BW25113 infection model established in male SPF Kunming (KM) mice (20-22 g)[1]
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Dosage:25 mg/kg (monotherapy); 5 and 15 mg/kg with Tetracycline
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Administration:Intraperitoneal injection (i.p.), single dose
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Result:Decreased CFU by approximately 0.5 log10 alone. Proved a more remarkable effect with Tetracycline.
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Animal Model:Skin would bacterial infection model established in male SPF Kunming (KM) mice (20-22 g)[1]
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Dosage:5 and 10 mg/kg with Azithromycin
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Administration:Applied to the wound, once daily for 8 days
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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.
Chemical Information
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CAS No. 3082621-32-4
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분자량 509.48
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화학식 C28H33BrN2O2
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SMILES
O=C(N1CCCCC1)CN2C3=C(C4=C2C=C(OCC5=CC=C(Br)C=C5)C=C4)CC(C)(C)CC3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AcrB-IN-6 Related Classifications
HY-178111 Related Classifications
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