PF-0463481 is safe and well-tolerated and has the potential for the study of diabetic nephropathy. PF-0463481 is an effective and orally active dual CCR2/CCR5 antagonist. It also has comparable human and rodent CCR2 potency (rat IC50=20.8 nM). PF-0463481
Thiocillin I is a thiopeptide antibiotic and has in vitro antibacterial activity against Gram-positive bacterial strains(MIC of Thiocillin I against S. aureus 1974149, E. faecalis 1674621, B. subtilis ATCC 6633 and S. pyogenes 1744264 are 2 μg/mL, 0.5 μg/mL, 4 μg/mL and 0.5 μg/mL, respectively).
DNA ligase-IN-2 (compound 2) 是 LigA 的高效抑制剂,能够抑制全长 LigA 及截短酶 LigA:AD 的 DNA 非依赖性自发腺苷酸化活性,其 IC50 为 29 nM。此化合物显著抑制金黄色葡萄球菌的体外生长,对于金黄色葡萄球菌 (S. aureus) ATCC 29213、金黄色葡萄球菌 (S. aureus) ATCC 700699 的 MIC 值为 1 μg/mL,而对大肠杆菌 (E. coli) ATCC 25922 的 MIC 值大于 64 μg/mL。