ABT-546 is a potent and highly selective endothelin ETA receptor antagonist, exhibiting a binding affinity (Ki) of 0.46 nM for [125I]endothelin-1 in cloned human ETA receptors. With over 25,000-fold selectivity for the ETA receptor compared to the ETB receptor, ABT-546 effectively inhibits endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis, displaying IC50 values of 0.59 nM and 3 nM, respectively. This compound serves valuable applications in cardiovascular and neurobiological research, particularly in studies investigating endothelin-mediated pathways.
ABT-546 is a potent and highly selective endothelin ETA receptor antagonist, exhibiting a binding affinity (Ki) of 0.46 nM for [125I]endothelin-1 in cloned human ETA receptors. With over 25,000-fold selectivity for the ETA receptor compared to the ETB receptor, ABT-546 effectively inhibits endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis, displaying IC50 values of 0.59 nM and 3 nM, respectively. This compound serves valuable applications in cardiovascular and neurobiological research, particularly in studies investigating endothelin-mediated pathways.
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