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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETheobromineCat. No.: HY-N0138CAS No.: 83-67-0Synonyms: 3,7-Dimethylxanthine分式: CHNO分量: 180.16作靶点: Adenosine Receptor; Endogenous Metabolite作通路: GPCR/G Protein; Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solven
2、t -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 6 mg/mL (33.30 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 5.5506 mL 27.7531 mL 55.5062 mL5 mM 1.1101 mL 5.5506 mL 11.1012 mL10 mM 0.5551 mL 2.7753 mL 5.5506 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,并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Th
3、eobromine在可可中发现的甲基黄嘌呤,可以抑制腺苷受体 A1 (AR1) 信号传导。IC50 & Target Human Endogenous Metabolite体外研究Theobromine, at concentrations above 25 M, decreases lipid accumulation in these cells. Cell viability is notaffected by Theobromine. Theobromine, at concentrations above 25 M, suppresses protein expression of1
4、/2 Master of Small Molecules 您边的抑制剂师www.MedChemEPPAR, C/EBP and adipogenic genes. The mRNA levels of these genes are also decreased byTheobromine 1.体内研究 Body weights are lower in the Theobromine group than in the vehicle group. In addition, Theobrominesuppresses gains in weight of epididymal and per
5、irenal adipose tissues. The mean adipocyte area is smallerin the Theobromine group than in the vehicle group 1. Theobromine group shows lower counts than theother groups when considering the number of bacteria per fecal weight (p=0.021 and p=0.055 compare to thereference (RF) and the cocoa (CC) grou
6、ps, respectively). The Theobromine diet leads to higher pH valuesthan those found after the RF and CC diets. Fecal concentrations of lactic acid are not signicantly affectedby the experimental diets (4.261.54 mM in RF group; 1.960.41 mM in CC group; 2.690.73 mM inTheobromine group) 2.PROTOCOLKinase
7、Assay 1 3T3-L1 preadipocytes are pre-incubated with MG132 (10 M) for 30 min, followed by incubation with IBMX inthe presence or absence of Theobromine (25 M) for 8 h. The cells are lysed in denaturing cell extractionbuffer (50 mM Tris-HCl, pH 7.5, containing 70 mM -mercaptoethanol and 2% SDS) at 95C
8、 for 10 min. Thecell lysates are diluted 20 fold with dilution buffer (20 mM Tris-HCl, pH 7.5, containing 150 mM NaCl, 1 mMEDTA, 1mM EGTA, 1% TritonX-100, 2.5 mM sodium pyrophosphate and protease inhibitor cocktail) andcentrifuged at 20,000 g for 30 s. The supernatant is incubated with rabbit polycl
9、onal anti-C/EBP IgG, anti-FLAG IgG or control IgG at 4C overnight, followed by incubation with 30 L protein G-Sepharose resin at4C for 1 h. The resin is washed with lysis buffer three times and proteins bound to the resin are separatedby SDSand analyzed by western blotting 1.MCE has not independentl
10、y confirmed the accuracy of these methods. They are for reference only.Animal Lewis rats (3 week old) are used in this study. The rats are randomly distributed into three dietary groupsAdministration 2 (n=7 per group): the reference (RF) group ingested standard diet AIN-93M, the cocoa (CC) group ing
11、ested astandard diet with 10% of natural Forastero cocoa containing 0.25% Theobromine, and the Theobromine(TB) group ingested a standard diet including 0.25% of Theobromine, i.e. the content of Theobrominepresents in the CC diet 2.MCE has not independently confirmed the accuracy of these methods. Th
12、ey are for reference only.REFERENCES1. Mitani T, et al. Theobromine suppresses adipogenesis through enhancement of CCAAT-enhancer-binding protein degradation byadenosine receptor A1.2. Martn-Pelez S, et al. Effect of cocoas theobromine on intestinal microbiota of rats. Mol Nutr Food Res. 2017 Oct;61(10).McePdfHeightCaution: P
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