IMD0354,978-62-1

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YZ剂描述：

产品名称：IMD0354

产品别名：N-[3,5-双(三氟甲基)苯基]-5-氯-2-羟基苯甲酰胺

英文别名：IMD 0354;IMD-0354

靶点：IKKβ

CAS：978-62-1

纯度：＞98%

外观：见爱必信官网

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

IMD0354是一种IKKβYZ剂，作用于NF-κβ通路，YZIκBα磷酸化。

溶解性：DMSO : 38.4 mg/mL (100 mM)
Ethanol : 38.4 mg/mL (100 mM)

体外研究：

IMD-0354 (G559 cells and IC-2V814 cells. IMD-0354 (0.5 μM) results in arrest of the cell cycle at the G0/G1 phase in HMC-1 cells. IMD-0354 (1 μM) increases the number of cells with hypodiploid DNA content in HMC-1 cells. IMD-0354 ( IMD-0354 inhibits 98.5% of NF-κB activity at a concentration of 10 μg/ml in HepG2 cells. IMD-0354 (1 μM) ameliorates the TNFα-induced decrease in the adiponectin concentration in the media, when the TNFα (6 nM) and insulin (100 nM) are administered simultaneously in 3T3-L1 adipocytes serum-starved for 12 h. IMD-0354 (1 μM) restores the phosphorylation of Akt down-regulated by the TNFα treatment, when the TNFα (6 nM) and insulin (100 nM) are administered simultaneously in 3T3-L1 adipocytes serum-starved for 12 h. IMD-0354 (1 μM) inhibits phosphorylation of IκBα and nuclear translocation of nuclear factor-kappa B (NF-κB) induced by tumor necrosis factor-α (TNF-α) in cultured cardiomyocytes. IMD-0354 (1 μM) significantly reduces TNF-α-induced production of interleukin-1β and monocyte chemoattractant protein-1 from cultured cardiomyocytes.

体内研究：IMD-0354 at 5 mg/kg also significantly decreases NF-κB, but the magnitude of the decrease is lower than with 20 mg/kg IMD-0354 in lungs of OVA-sensitized mice. IMD-0354 (20 mg/kg) ameliorates airway hyperresponsiveness and reduces the numbers of bronchial eosinophils and mucus-producing cells in OVA-sensitized mice. IMD-0354 (20 mg/kg) also reduces the total numbers of cells and eosinophils in bronchoalveolar lavage fluid in OVA-sensitized mice. IMD-0354 (20 mg/kg) inhibits the production of Th2 cytokines such as interleukin (IL)-5 and IL-13 and eotaxin in the airways and/or lungs of OVA-sensitized mice, but it does not affect the restoration of Th1 cytokines such as IL-12 and interferon-gamma under the same experimental conditions. IMD-0354 (20 mg/kg) results in a partial decrease in serum IgE concentration in OVA-sensitized mice. IMD-0354 significantly decreases the plasma glucose levels in KKAy mice treated with and fed an HF diet in an dose-dependent manner without influence of body weight. IMD-0354 (10 mg/kg) results in a significant dose-dependent reduction of the infarction area/area at risk ratio and the preservation of fractional shortening ratio.

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