Cardamonin 是一种新型hTRPA1阳离子通道拮抗剂,IC50值为454 nM。
产品描述
Cardamomin (also known as cardamonin) is a chalconoid that has been isolated from several plants including Alpinia katsumadai and Alpinia conchigera. It is a novel antagonist of hTRPA1 cation channel with an IC50 of 454 nM. It has received growing attention from the scientific community due to the expectations toward its benefits to human health.
体外活性
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-κB) in a concentration-dependent manner, and restores the expression of IκB in MG63 and Raw264.7 cells[2].
体内活性
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].
细胞实验
HEK293 cells are treated with cardamonin (0-90 μM). The cells treated in the absence of the test compound are the negative control. After incubated for 24 h, Cell Titer-Glo reagent is added to the cells and Luminescence is acquired on the plate reader[1].
Cas No.
19309-14-9
分子式
C16H14O4
分子量
270.284
别名
Cardamomin;Cardamonin;Alpinetin chalcone;豆蔻明;(E)-Cardamoni;小豆蔻明
储存和溶解度
DMSO:27 mg/mL(100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years