Bioactivity | Efflux pump-IN-4 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-4 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-4 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model[1]. |
Invitro | Efflux pump-IN-4 (compound G11) (8-128 μg/mL) 与至少一种抗生素(ERY、LEV 和 MIN)表现出出色的抗菌协同作用。Efflux pump-IN-4 与 MIN 显示出抗菌协同作用,并在 8 μg/mL 时将 LEV 的 MIC 值降低 4 倍[1]。Efflux pump-IN-4 (50 μM, 100 μM) 在最低浓度 50 μM 下表现出强抑制活性,可抑制尼罗红外排[1]。Efflux pump-IN-4 (4-256 μg/mL) 不引起小鼠红细胞溶血[1]。 |
In Vivo | Efflux pump-IN-4 (compound G11) (128 μg/mL;72 小时) 对秀丽隐杆线虫没有显著的体内毒性[1]。 |
Name | AcrB-IN-4 |
CAS | 2890177-95-2 |
Formula | C29H34N2O4S |
Molar Mass | 506.66 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Guo T, et al. Design and synthesis of benzochromene derivatives as AcrB inhibitors for the reversal of bacterial multidrug resistance. Eur J Med Chem. 2023 Mar 5;249:115148. |