1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENonivamideCat. No.: HY-17568CAS No.: 2444-46-4Synonyms: Pseudocapsaicin; Pelargonic acid vanillylamide; Nonanoic acidvanillylamide分式: CHNO分量: 293.4作靶點: TRP Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式: Pow

2、der -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (340.83 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.4083 mL 17.0416 mL 34.0832 mL5 mM 0.6817 mL 3.4083 mL 6.8166 mL10 mM 0.3408 mL 1.7042 mL 3.4083 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注

3、意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟海僖来翁砑又軇?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.52 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubilit

4、y: 2.5 mg/mL (8.52 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.52 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Nonivamide種 激動劑，在靜態(tài)毒性檢測中，4d-EC50 為 5.1 mg/L。IC50 & Target TRPV1 1體外研究 Nonivamide, a synthetic derivate of na

5、tural capsaicin, has an effective antifouling activity. Capsaicin exhibits4d-EC50 values of 5.50.5mg/L, 232mg/L, 6.90.2mg/L, and 15.60.4mg/L in static toxicity testsconducted using Pseudomonas putida, Lake Erie bacteria, Vibrio natriegens, and Vibrio parahaemolyticus,respectively. A significant grow

6、th inhibitory effect (p50 value (4 d-EC50) is 5.1mg/L 1. Nonivamidetreatment causes calcium release from the ER and altered the transcription of growth arrest- and DNAdamage-inducible transcript 3 (GADD153), GADD45, GRP78/BiP, ATF3, CCND1, and CCNG2) in a mannercomparable with prototypical ER stress

7、-inducing agents. ER calcium flux is evaluated by pretreating cellswith 2.5 M thapsigargin for 5 min followed by addition of 2.5 M Nonivamide. Treatment of TRPV1-overexpressing cells with 2.5 M Nonivamide produces marked increases in cytosolic calcium due to releaseof calcium from ER stores. Treatme

8、nt of TRPV1-overexpressing cells with 1 M Nonivamide causes anapproximate 50% loss in cell viability after a 24-h period. BEAS-2B cells treated with 100 and 200 MNonivamide also exhibits a shift in the relative amount of EIF2-P and an increase in the expression ofGADD153 mRNA and protein 2. Treatmen

9、t with Nonivamide reduces lipid accumulation to a similar extentas CAP; the effects are not different from the effects after CAP treatment at any of the tested concentrations.Compared to untreated control cells, treatment with Nonivamide decreases lipid accumulation by 5.341.03%(P 3.PROTOCOLCell Ass

10、ay 3 In the MTT assay, the reduction of yellow tetrazolium salt MTT to a purple formazan by mitochondrial and ERenzymes is used as a measure for cell viability. Cells are seeded in 96well plates and treated with 1nM-10MCAP or Nonivam ide with or without addition of 25-100M BCH or the corresponding e

11、thanol concentration (0.1-0.2%(v/v), solvent control) for 12 days after initiation of differentiation. Cell culture m edia is exchanged every second day.On Day 12, 100L of the MTT working reagent (0.83m g/m L MTT diluted in PBS/serum -free m edia (1:5), is added toeach well, and cells are incubated

12、at 37C for approxim ately 15m in. The MTT working solution is rem oved and thepurple form azan form ed during incubation is dissolved in 150L DMSO per well. Absorbance is m easured at 550nmwith 690nm as reference wavelength using m ultiwell plate reader. The num ber of m etabolically active cells is

13、 calculated relative to untreated control cells or the corresponding solvent control (100%) 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Zhou J, et al. Toxic effects of environment-friendly antifoulant Nonivamide on Phaeodactylum trico

14、rnutum. Environ Toxicol Chem. 20132/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEApr;32(4):802-9.2. Thomas KC, et al. Transient receptor potential vanilloid 1 agonists cause endoplasmic reticulum stress and cell death in human lungcells. J Pharmacol Exp Ther. 2007 Jun;321(3):830-8.3. Rohm B, et al. Nonivamide enhances miRNA let-7d expression and decreases adipogenesis PPAR expression in 3T3-L1 cells. J CellBiochem. 2015 Jun;