(E)-Cardamonin(Synonyms: 小豆蔻明; (E)-Cardamomin; (E)-Alpinetin chalcone)

天然产物 黄酮类 Flavonoids

(E)-Cardamonin (Synonyms: 小豆蔻明; (E)-Cardamomin; (E)-Alpinetin chalcone) 纯度: 99.77%

(E)-Cardamonin ((E)-Cardamomin) 是新颖的hTRPA1阳离子通道拮抗剂,IC50值为454 nM。

(E)-Cardamonin(Synonyms: 小豆蔻明; (E)-Cardamomin;  (E)-Alpinetin chalcone)

(E)-Cardamonin Chemical Structure

CAS No. : 19309-14-9

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10 mM * 1 mL in DMSO ¥550 In-stock
5 mg ¥500 In-stock
10 mg ¥700 In-stock
25 mg ¥1400 In-stock
50 mg ¥2200 In-stock
100 mg ¥3600 In-stock
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生物活性

(E)-Cardamonin ((E)-Cardamomin) is a novel antagonist of hTRPA1 cation channel with an IC50 of 454 nM.

IC50 & Target

IC50: 454 nM (hTRPA1 cation channel)[1]

体外研究
(In Vitro)

(E)-Cardamonin ((E)-Cardamomin) 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. (E)-Cardamonin ((E)-Cardamomin) does not significantly reduce HEK293 cell viability, nor does it impair cardiomyocyte constriction[1]. (E)-Cardamonin ((E)-Cardamomin) 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

(E)-Cardamonin ((E)-Cardamomin) (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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

270.28

Formula

C16H14O4

CAS 号

19309-14-9

中文名称

小豆蔻明

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 28 mg/mL (103.60 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6999 mL 18.4993 mL 36.9987 mL
5 mM 0.7400 mL 3.6999 mL 7.3997 mL
10 mM 0.3700 mL 1.8499 mL 3.6999 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Wang S, et al. Cardamonin, a Novel Antagonist of hTRPA1 Cation Channel, Reveals Therapeutic Mechanism of Pathological Pain. Molecules. 2016 Aug 29;21(9). pii: E1145.

    [2]. Park MK, et al. Novel anti-nociceptive effects of cardamonin via blocking expression of cyclooxygenase-2 andtransglutaminase-2. Pharmacol Biochem Behav. 2014 Mar;118:10-5.

Cell Assay
[1]

HEK293 cells are treated with (E)-Cardamonin ((E)-Cardamomin) (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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1][2]

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 (E)-Cardamonin ((E)-Cardamomin) (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 (E)-Cardamonin ((E)-Cardamomin). 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Wang S, et al. Cardamonin, a Novel Antagonist of hTRPA1 Cation Channel, Reveals Therapeutic Mechanism of Pathological Pain. Molecules. 2016 Aug 29;21(9). pii: E1145.

    [2]. Park MK, et al. Novel anti-nociceptive effects of cardamonin via blocking expression of cyclooxygenase-2 andtransglutaminase-2. Pharmacol Biochem Behav. 2014 Mar;118:10-5.