辣椒素 T1321

Product Introduction
Bioactivity


英文名: Nonivamide

描述: Nonivamide (Nonanoic acid vanillylamide) 具有激动活性，在静态毒性检测中，4d-EC50为 5.1 mg/L。

细胞实验: Nonivamide is dissolved in ethanol to 1,000× stock solutions freshly each time and final ethanol concentration during the assays never exceeded 0.2% (v/v)[3]. In the MTT assay, the reduction of yellow tetrazolium salt MTT to a purple formazan by mitochondrial and ER enzymes is used as a measure for cell viability. Cells are seeded in 96‐well plates and treated with 1?nM-10?μM CAP or Nonivamide with or without addition of 25-100?μM BCH or the corresponding ethanol concentration (0.1-0.2% (v/v), solvent control) for 12 days after initiation of differentiation. Cell culture media is exchanged every second day. On Day 12, 100?μL of the MTT working reagent (0.83?mg/mL MTT diluted in PBS/serum-free media (1:5)), is added to each well, and cells are incubated at 37°C for approximately 15?min. The MTT working solution is removed and the purple formazan formed during incubation is dissolved in 150?μL DMSO per well. Absorbance is measured at 550?nm with 690?nm as reference wavelength using multiwell plate reader. The number of metabolically active cells is calculated relative to untreated control cells or the corresponding solvent control (100%)[3].

体外活性: Nonivamide（一种合成的天然Capsaicin 衍生物）具有有效的抗污染活性。在针对假单胞菌、伊利湖细菌、弧菌和副溶血弧菌的静态毒性测试中，Capsaicin 的4d-EC50值分别为5.5±0.5mg/L、23±2mg/L、6.9±0.2mg/L和15.6±0.4mg/L。非尼伐胺经1mg/L处理4天的实验组观察到显著的生长抑制效应（p<0.01），其4d-EC50值为5.1 mg/L[1]。非尼伐胺处理能引起内质网释放钙离子，并影响生长停滞与DNA损伤诱导的转录物3（GADD153）、GADD45α、GRP78/BiP、ATF3、CCND1和CCNG2的转录，其方式与典型内质网应激诱导剂相似。通过先以2.5微摩尔的丝蓟素处理细胞5分钟，再加入2.5微摩尔的非尼伐胺来评估内质网钙通量。用2.5微摩尔非尼伐胺处理TRPV1高表达细胞会显著增加胞质钙水平，由于来自内质网储藏的钙释放。用1微摩尔非尼伐胺处理TRPV1高表达细胞造成约50%的细胞活力在24小时后丧失。用100和200微摩尔非尼伐胺处理的BEAS-2B细胞同样显示出EIF2α-P的相对量改变，并且GADD153 mRNA和蛋白表达增加[2]。与Capsaicin 处理相比，非尼伐胺减少脂肪堆积的效果相似，且在所有测试浓度下其效果并无差异。相较于未经处理的对照细胞，非尼伐胺处理降低了脂肪堆积5.34±1.03%（P<0.05）至0.01微摩尔，最高可达10.4±2.47%（P<0.001）至1µM[3]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (170.42 mM)


关键字: TRP Channel | Inhibitor | inhibit | Transient receptor potential channels | Nonivamide

相关产品: (Z)-Capsaicin | TC-I 2014 | AM-0902 | TRPV4 agonist-1 free base | Oleoyl Serotonin | Methyl syringate | SB-705498 | TRPA1-IN-2 | ML329 | Fingolimod hydrochloride

相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Food Additive Library | Bioactive Compounds Library Max | Chinese Pharmacopoeia Natural Product Library | Anti-Cancer Clinical Compound Library | Human Endogenous Metabolite Compound Library Plus | Traditional Chinese Medicine Monomer Library | RO5 Drug-like Natural Product Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途