CHIR-29498

CHIR-29498 is an antibacterial peptoid. CHIR-29498 is active against both Gram-positive and Gram-negative bacteria. CHIR-29498 can be used for the study of fatal Staphylococcus aureus^[1]. In Vitro:CHIR-29498 (0.6-40 μM, 18-24 h) is active against both Gram-positive and Gram-negative bacteria^[1].
CHIR-29498 (20-40 μM) can continuously increase the extracellular β-galactosidase activity of Escherichia coli ML-35 (ATCC 43827), indicating cell membrane leakage^[1].
CHIR-29498 (20-40 μM, 0.5-2 h) causes 54.4% (1× MIC) and 74.2% (2× MIC) of Staphylococcus aureus ATCC 25923 to be stained with PI after incubation for 30 minutes; after 2 hours, the staining percentages increased to 78.1% and 94.1%, respectively, indicating increased membrane permeability. The effect of DHAA is relatively weak^[1].
CHIR-29498 (1 h) induces hemolysis in mice (BALB/c) or human erythrocytes (RBCs) at concentrations above the MIC, but the hemolytic activity is mild^[1].
In Vivo:CHIR-29498 (5-30 mg/kg, i.p., once) shows complete protection at doses of 10 mg/kg and 30 mg/kg in CD-1 mice, and also shows activity in delayed dosing scenarios where infection has been established^[1].