ELN441958 (ELN-441958) is a novel, potent, and small molecule antagonist of neutral bradykinin B1 receptor which inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM. ELN441958 exhibits high oral bioavailability and potent systemic efficacy in rhesus monkey inflammatory pain. The bradykinin B(1) receptor plays a critical role in chronic pain and inflammation, although efforts to demonstrate efficacy of receptor antagonists have been hampered by species-dependent potency differences, metabolic instability, and low oral exposure of current agents.

纯度：≥98%

CAS：913064-47-8