CPU0213

CPU0213 is a novel, non-selective **endothelin receptor antagonist** developed by the Center of New Drug Research and Development at China Pharmaceutical University. It blocks both endothelin A (ETA) and endothelin B (ETB) receptors, suppressing vasoconstriction and endothelin-1 (ET-1) binding. CPU0213 has demonstrated greater potency than bosentan in experimental models, is effective in attenuating cardiac hypertrophy and heart failure, and exhibits significant protective effects against renal dysfunction and injury in animal models of diabetic nephropathy and septic acute renal failure. Its mechanism of action includes inhibition of ET-1-mediated vascular and renal pathology and suppression of the endothelin-ROS-NF-κB pathway in sepsis. CPU0213 also exhibits anti-apoptotic effects in renal epithelial cells by inhibiting Nox4-dependent superoxide production and modulating Bcl-2/Bax expression, which may underlie its nephroprotective effects in diabetic nephropathy[1][2][3][5].