Vixticibart

Vixticibart specifically binds to human and monkey natriuretic peptide receptor 1 extracellular domain proteins, with no cross-reactivity to mouse natriuretic peptide receptor 1, natriuretic peptide receptor 2, or natriuretic peptide receptor 3, and does not interfere with atrial natriuretic peptide binding to human natriuretic peptide receptor 1^[1].
Vixticibart (10^-12 to 10^-6 M; under conditions supporting binding) dose-dependently binds to human and monkey natriuretic peptide receptor 1-expressing HEK293 cells, with enhanced binding in the presence of atrial natriuretic peptide or brain natriuretic peptide, and EC₅₀ values ranging from 2.27 to 5.69 nM^[1].
Vixticibart (10^-15 to 10^-5 M) dose-dependently agonizes human and monkey natriuretic peptide receptor 1 in a calcium flux bioassay, with EC₅₀ values ranging from 42.5 to 82.2 nM, and achieves maximum activation comparable to natriuretic peptide ligands at high concentrations^[1].
Vixticibart (10^-14 to 10^-5 M) dose-dependently activates human natriuretic peptide receptor 1 to induce cGMP accumulation in HEK293 cells, acts as a partial agonist relative to natriuretic peptide ligands, and shows enhanced activation in the presence of low concentrations of atrial natriuretic peptide or brain natriuretic peptide^[1].
Vixticibart (molar excess; overnight at 4°C) binds to the N-terminal domain of human NPR1 dimers, stabilizing an active conformation in the presence of atrial natriuretic peptide and an active-like conformation in the absence of atrial natriuretic peptide, which drives downstream signaling^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.