Cardamonin

19309-14-9

C16H14O4

DMSO : >= 28 mg/mL (103.60 mM); H2O : < 0.1 mg/mL (insoluble)

Membrane Transporter/Ion Channel; Neuronal Signaling

Cardamonin is a novel antagonist of hTRPA1 cation channel with an IC₅₀ of 454 nM. IC50 & Target: IC50: 454 nM (hTRPA1 cation channel)^[1] In Vitro: Cardamonin selectively blocksTRPA1 activation (IC₅₀=454 nM) while does not interact with TRPV1 nor TRPV4 channel. Docking analysis of cardamonin demonstrates a compatible interaction with A-967079-binding site of TRPA1. Cardamonin does not significantly reduce HEK293 cell viability, nor does it impair cardiomyocyte constriction^[1]. Cardamonin suppresses the expression of Tgase-2, cyclooxygenase-2 (COX-2), and p65 (nuclear factor-kappaB) in a concentration-dependent manner, and restores the expression of IkappaB in MG63 and Raw264.7 cells^[2]. In Vivo: Cardamonin (3-30 mg/kg, orally administered) significantly inhibits PBQ-induced writhing. CDN also produces a significant, dose-dependent increase in the withdrawal response latencies in carrageenan-induced hyperalgesia^[2].