Description |
Cardamonin is a novel antagonist of hTRPA1 cation channel with an IC50 of 454 nM.
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Target |
IC50: 454 nM (hTRPA1 cation channel)[1]
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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-κB) in a concentration-dependent manner, and restores the expression of IκB in MG63 and Raw264.7 cells[2].
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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].
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Cell Assay |
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].
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Animal Admin |
Rats: The rats are divided into groups of six according to their nociceptive pressure thresholds, after which carrageenan (0.1 mL, 1%) is injected into the plantar surface of the left hind paw. The rats received vehicle or cardamonin (3-30 mg/kg) or indomethacin (3 mg/kg) orally 2 h after carrageenan injection and are evaluated for paw hyperalgesia 0, 1 and 2 h after administration of compounds. Indomethacin is used as a positive control[2]. Mice: Acute pain is induced by an intraperitoneal injection of 0.2 mL of 0.02% PBQ 54 min after oral administration of cardamonin. Six minutes after the PBQ injection, the total number of writhes is counted for 6 min. The control animals received an appropriate volume of dosing vehicle (80% saline, 10% ethanol and 10% Tween 80). Indomethacin is used as a positive control[2].
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Density | 1.3±0.1 g/cm3 |
Boiling Point | 484.5±45.0 °C at 760 mmHg |
Flash Point | 182.7±22.2 °C |
Exact Mass | 270.089203 |
PSA | 66.76000 |
LogP | 3.62 |
Vapour Pressure | 0.0±1.3 mmHg at 25°C |
Storage condition | Store at +4°C |