Zamaporvint (RXC004) is a selective, orally active and potent inhibitor of the Wnt pathway that acts on the membrane-bound fatty acyltransferase porcupine to block Wnt ligand palmitoylation, secretion, and pathway activation.

High affinity angiotensin-converting enzyme (ACE) ligand (Kd = 2.79 nM). Exhibits no significant effect on ACE enzymatic activity up to 500 nM concentration. Potentiates NMDA + D-serine-induced dopamine release from striatal slices in vitro and the striatum in vivo.

Methylswertianin is an active constituent in Swertia punicea Hemsl, with anti-diabetic effect. Methylswertianincan abates type-2 diabetes, likely via the improvement of insulin resistance (IR).