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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作靶点: TRP Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式: Pow
2、der -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (340.83 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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,并请注
3、意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案,配制前请先配制澄清的储备液,再依次添加助溶剂(为保证实验结果的可靠性,体内实验的作液,建议您现现配,当天使;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占):1. 请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.52 mM); Clear solution2. 请依序添加每种溶剂: 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 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.52 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Nonivamide种 激动剂,在静态毒性检测中,4d-EC50 为 5.1 mg/L。IC50 & Target TRPV1 1体外研究 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 您边的抑制剂师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;
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