J-104132 NLT 98%

J-104132 is a potent, orally active ET_A/ET_B receptor antagonist, with K_is of 0.034 nM and 0.104 nM for cloned human ET_A and ET_B receptors expressed in CHO cells. IC50 & Target: Ki: 0.034 nM (human ET_A receptor, CHO cell), 0.104 nM (human ET_B receptor, CHO cell)^[1] In Vitro: J-104132 is a potent, orally active mixed ET_A/ET_B receptor antagonist, with K_is of 0.034 nM and 0.104 nM for cloned human ET_A and ET_B receptors expressed in CHO cells. J-104132 also shows K_i of 0.350 ± 0.158 nM for ET_A receptor in human uterus and 0.343 ± 0.146 nM for ET_B receptor in human hippocampus^[1].