A-216546 free base 3-Pyrrolidinecarboxylic acid, 1-(2-(dibutylamino)-2-oxoethyl)-2-(2,2-dimethylpentyl)-4-(7-methoxy-1,3-benzodioxol-5-yl)-, (2S,3R,4S)-
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ABT-546 is a potent, highly selective and active antagonist of ETA receptor with a Ki of 0.46 nM for [125I]endothelin-1 binding to cloned human ETA. It is >25,000-fold more selectivity for ETA receptor than ETB receptor. It blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50s of 0.59 and 3 nM, respectively.
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