ABT-546 (A-216546) is an orally active ET A receptor antagonist, with K i values of 0.46 nM and 13000 nM for human ET A and ET B receptors, respectively, and exhibits >25000-fold selectivity over the ET B receptor. ABT-546 effectively inhibits ET-1 ( HY-P0202 )-induced phosphoinositide hydrolysis ( IC 50 = 0.59 nM) and arachidonic acid release ( IC 50 = 3.03 nM), and antagonizes ET-1-induced contraction in isolated vascular rings. ABT-546 crosses the placental barrier but shows extremely low fetal exposure, with a favorable safety profile. ABT-546 inhibits ET-1-induced pressor response and downregulates the NLRP3 / ROS /GSDMD-mediated pyroptosis pathway. ABT-546 can be used for research on abdominal aortic aneurysm.
Products | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Disease Areas > Cardiovascular Disease | Products > Disease Areas > Aortic Aneurysm | Products > Signaling Pathways > GPCR/G Protein | Products > Signaling Pathways > Immunology/Inflammation | Products > Signaling Pathways > NF-κB | Products > Signaling Pathways > Metabolic Enzyme/Protease | Products > Signaling Pathways > Apoptosis | Products > Research Areas > Cardiovascular Disease | Products > Signaling Pathways > Pyroptosis | Products > Signaling Pathways > Interleukin Related | Products > Signaling Pathways > Endothelin Receptor | Products > Signaling Pathways > NOD-like Receptor (NLR) | Products > Signaling Pathways > Reactive Oxygen Species (ROS)
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