1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESinapine thiocyanateCat. No.: HY-N0450CAS No.: 7431-77-8分式: CHNOS分量: 368.45作靶點(diǎn): P-glycoprotein; Reactive Oxygen Species作通路: Membrane Transporter/Ion Channel;Immunology/Inflammation; Metabolic Enzyme/Protease; NF-B儲(chǔ)存式: 4C, protec

2、t from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 125 mg/mL (339.26 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.7141 mL 13.5704 mL 27.1407 mL5 mM 0.5428 mL 2.7141 mL 5.4281 mL10 mM 0.2714 mL 1.3570 mL 2.71

3、41 mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)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(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 12.5 mg/mL (33.93 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMS

4、O 90% (20% SBE-CD in saline)Solubility: 12.5 mg/mL (33.93 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 12.5 mg/mL (33.93 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Sinapine thiocyanate來字花科物種的物堿，具有抗氧化劑和放射性保護(hù)等活性。IC50 & Target P-glyco

5、protein 1體外研究 Sinapine thiocyanate increases the sensitivity of Caco-2 cells to doxorubicin in a dose-dependent manner,whereas no or less effect is observed in the cells treated with doxorubicin alone. The combination of Sinapineand doxorubicin has a synergistic effect and increased the cytotoxicity

6、 of doxorubicin against Caco-2 cells.Results indicate that Sinapine plays an important role in the down-regulation of P-glycoprotein expressionthrough suppression of FGFR4-FRS2a-ERK1/2 signaling pathway 1.Sinapine thiocyanate can effectively protect against OH-induced damages to DNA and MSCs, thereb

7、y it mayhave a therapeutic potential in MSCs transplantation 2.體內(nèi)研究 During the first 8 days, the dry matter intake and live weight gain of the rats are significantly reduced by theintake of Sinapine thiocyanate and other phenolic compounds. However, after this adaptation period theirperformances are

8、 similar to those of the control group 3.PROTOCOLCell Assay 1 The Caco-2 cells are seeded into a 96-well plate with 8000 cells/well for 24 h. After incubation with differentdoses of Sinapine (0-200 M), doxorubicin, or both for 24 h, the medium is discarded. Cell survival afterexposure to Sinapine al

9、one or a combination of Sinapine and the anti-tumor agent doxorubicin is examinedby MTT colorimetric assay 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats 3Administration 3 Sixty male Sprague-Dawley rats (95 g) are randomly allotted to 6 g

10、roups of 10 rats each and reared inindividual cages. Six groups of 10 growing rats each are fed ad libitum for 15 days one of six diets: diet A,rapeseed (3.80 g of sinapine/kg DM); diet B, ethanol/water-extracted rapeseed (0.48 g of sinapine); diet C,control diet; diet G, control diet+3.74 g of extr

11、acted sinapine; diet H, control diet + 3.72 g of sinapine+otherphenolic compounds; or diet I, control diet+the hydrolysis products of sinapine and other phenoliccompounds. The rats are weighed at 8 a.m. on days 1, 4, 8, 11 and 15 of the trial. After sacrifice the gutcontents are eliminated to permit

12、 determination of empty body weight gain (EBWG). The distribution, refusaland intake of each rat are recorded every day 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Guo Y, et al. Sinapine as an active compound for inhibiting the prolif

13、eration of Caco-2 cells via downregulation of P-glycoprotein. FoodChem Toxicol. 2014 May;67:187-92.2. Li X, et al. Protective Effect of Sinapine against Hydroxyl Radical-Induced Damage to Mesenchymal Stem Cells and Possible2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMechanisms. Chem Pharm Bull (Tokyo). 2016;64(4):319-25.3. Vermorel M, et al. Valorization of rapeseed meal. 5. Effects of sinapine and other phenolic compounds on food intake and nutrientutilization in growing rats. Reprod Nutr Dev. 1987;27(4):781