Atrasentan (ABT-627, A-147627) is a potent, selective and orally active nonpeptide endothelin A receptor (ETA) with IC50 of 0.055 nM.
Atrasentan (ABT-627, A-147627) significantly inhibits LNCaP and C4-2b prostate cancer cell growth.
Atrasentan (ABT-627, A-147627) inhibits ET-1 radioligand binding with IC50 of 0.36 nM, 1000-fold selectivity for the ET(A) vs the ET(B) receptor.
Atrasentan (ABT-627, A-147627) also is a potent inhibitor (IC50=0.16 nM) of phosphoinositol hydrolysis stimulated by ET-1, and it antagonizes the ET-1-induced contraction of the rabbit aorta with a pA(2)=9.20.
