RS504393 is a potent, selective CCR2 antagonist with IC50 of 89 nM, shows no activity against CCR1. RS504393 reduced renal interstitial fibrosis relative to wild-type mice. RS504393 attenuates hyperglycaemia and inflammation in a mouse model of hepatic steatosis and lipoatrophy. RS504393 significantly inhibited the expression of CCR1, CCR2 and interleukin (IL)-8 after either LPS or tumor necrosis factor-alpha stimulation in A549 cells,. RS504393 improves insulin resistance, lipid metabolism, and diabetic nephropathy in type 2 diabetic mice.
