NPR-C activator 1 (Compound 1) is a potent activator of natriuretic peptide receptor C ( NPR-C ). C-type natriuretic peptide (CNP) is involved in the regulation of vascular homeostasis. NPR-C activator 1 is identified as a potent agonist ( EC 50 ∼ 1 μM) with promising in vivo pharmacokinetic properties.