J-104132, formerly known as L-753037, is a potetn and selective endothelin A/B receptor antagonist potentially for the treatment of heart failure. J-104132 cloned human ETA = 0.034 nM; cloned human ETB = 0.104 nM. In vitro, J-104132 is a potent antagonist of ET-1-induced accumulation of [3H]inositol phosphates in Chinese hamster ovary cells stably expressing cloned human ETA receptors (IC50 = 0.059 nM). Pretreatment with J-104132 prevents the lethal response to ET-1 when administered i.v. (ED50 = 0.045 mg/kg) or p.o. in fed animals (ED50 = 0.35 mg/kg). J-104132 is an excellent pharmacological tool to explore the therapeutic use of a mixed ETA/ETB receptor antagonist. References: Kitada K, Yui N, Mori T, Ohkita M, Matsumura Y. Vasoprotective effects of an endothelin receptor antagonist in ovariectomized female rats. Life Sci. 2014 Nov 24;118(2):379-85. doi: 10.1016/j.lfs.2014.01.009. PubMed PMID: 24468711.

纯度：≥98%

CAS：198279-45-7