J-104132 is a potent, orally active dual antagonist of the ETA and ETB receptors, exhibiting a Ki of 0.034 nM for ETA and 0.104 nM for ETB receptors. It effectively inhibits Endothelin-1 (ET-1)-induced signaling and vascular contractions in vitro. In vivo studies demonstrate that J-104132 mitigates hypertension, vascular remodeling, and diabetic endothelial dysfunction through dual blockade of ETA and ETB receptors, making it valuable for research into diabetic vascular complications.
J-104132 is a potent, orally active dual antagonist of the ETA and ETB receptors, exhibiting a Ki of 0.034 nM for ETA and 0.104 nM for ETB receptors. It effectively inhibits Endothelin-1 (ET-1)-induced signaling and vascular contractions in vitro. In vivo studies demonstrate that J-104132 mitigates hypertension, vascular remodeling, and diabetic endothelial dysfunction through dual blockade of ETA and ETB receptors, making it valuable for research into diabetic vascular complications.
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