J-104132 (L-753037) is a potent, orally active, selective and competitive ETA/ETB receptor antagonist with K i of 0.034 nM for ETA and 0.104 nM for ETB receptors. J-104132 inhibits Endothelin-1 (ET-1) ( HY-P71446 )-induced signaling and vascular contractions in vitro. J-104132 alleviates hypertension, vascular remodeling, and diabetic endothelial dysfunction in vivo by dual ETA/ETB blockade. J-104132 can be used for research on diabetic vascular complications [1][3] .
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