ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM. ELN-441958(ELN 441958) is highly selective for B1 over B2 receptors.

Bradykinin B1:0.26 nM(ki)

IGF-IR Peptide Autophosphorylation: One microgram of constitutively active IGF-IR kinase domain peptide isincubated +/? varying concentrations of PQ 401 in 2% DMSO in 40 mM Tris (pH 7.4), 80 μMEGTA, 0.25% 2-mercaptoethanol, 80 μM Na3VO4, 10 mM MgCl2, and 2 mM MnCl2 for 20 minutes. ATP isthen added at a final concentration of 20 μM. Autophosphorylation of the kinase domain peptide isallowed to occur for 20 minutes at 22℃. The reaction isstopped by the addition of SDS-reducing buffer and the samples are run on SDS-PAGE. Following transfer to nitrocellulose membrane, peptide autophosphorylation isdetermined by Western blotting employing an antibody against phosphotyrosine (PY20).