尼日利亞菌素鈉鹽作用機制 - Medchemexpress - MCE中國

1、Product Data SheetNigericin sodium saltCat. No.: HY-100381CAS No.: 28643-80-3分式: CHNaO分量: 746.94作靶點: Potassium Channel; NOD-like Receptor (NLR); Bacterial作通路: Membrane Transporter/Ion Channel; Immunology/Inflammation; Anti-infection儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 mon

2、th溶解性數(shù)據(jù)體外實驗 Methanol : 150 mg/mL (200.82 mM)Ethanol : 50 mg/mL (66.94 mM)DMSO : 1 mg/mL (insoluble or slightly soluble)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 1.3388 mL 6.6940 mL 13.3880 mL5 mM 0.2678 mL 1.3388 mL 2.6776 mL10 mM 0.1339 mL 0.6694 mL 1.

3、3388 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；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍浮Ｒ韵氯芙獍付颊埾劝凑?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可

4、以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 6.25 mg/mL (8.37 mM); Clear solution此案可獲得 6.25 mg/mL (8.37 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 62.5 mg/mL 的澄 EtOH 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% EtOH 90% (20

5、% SBE-CD in saline)Page 1 of 2 www.MedChemESolubility: 6.25 mg/mL (8.37 mM); Clear solution此案可獲得 6.25 mg/mL (8.37 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 62.5 mg/mL 的澄均勻。EtOH 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加每種溶劑： 10% EtOH 90% corn oilSolubility: 6.25 mg/mL (8.37 mM); Clear solution此案可獲得 6.25 mg

6、/mL (8.37 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 62.5 mg/mL 的澄 EtOH 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Nigericin sodium salt。從吸鏈霉 中得到的種抗素，作為 H+，K+ 和 Pb2+ 離載體起作，NLRP3 的激動劑體外研究 Nigericin (0.1 M) decreases inhibits proliferation and clonogenicity of H460 lung cancer cells in a d

7、ose dependentmanner. Nigericin inhibits migration and invasion of H460 lung cancer cells1. Nigericin (0.1-10 nM) has apparently adual effect on cell volume, that is a shrinking effect at lower Nigericin concentrations and a swelling effect at higherconcentrations. Nigericin (0.1-1 nM) significantly

8、decreases cytosolic pH (pHi), and slightly increases the pHi at 5 and10 nM2. Nigericin exhibits higher toxicity on S18 cells than S26 cells, with IC50 of 2.030.55 M and 4.772.35 M,respectively. Nigericin can selectively kill cancer stem cells in NPC in vitro. Nigericin dramatically reduces themigrat

9、ion ability of S18 and HONE-1 cells3. Nigericin exhibits gteat toxicity for the HT29 and SW116 cell line with IC50 of 12.920.25 mol and 15.860.18 mol. Nigericin also shows a decreased ability to form colonies underanchorage-independent conditions in a standard soft agar assay4.體內(nèi)研究 Ngericin (4 mg/kg

10、, i.p.) significantly reduces tumor growth and acts synergistically with the chemotherapeutic agentDDP, as shown by the tumor volumes. Nigericin markedly decreases Bmi-1 in vivo. Overexpression of Bmi-1 partiallyrestores CSC content and metastatic ability of NPC cells under Nigericin treatment. The

11、downregulation of Bmi-1 maybe involved in the inhibitory effect of Nigericin on CSCs in NPC3.PROTOCOLCell Assay 1 For RCCs, cells (appr 2000 cells/well) are plated in 96-well cell-culture microplates and incubated over nigericinht incomplete media (CM)-RPMI 1640 supplemented with 5% FBS, 2 mM l-glut

12、amine, 100 U/mL penicillin, and 100mg/mL streptomycin to allow them to adhere. Cells are then exposed to the appropriate concentration of drug orvehicle for 72 h. For PPSS, cells (appr 500 cells/well) are plated in 96-well cell-culture microplates incubated overNigericinht in CM to allow them to adh

13、ere and then maintained in serum-free media for 7-8 days and then treatedwith the appropriate concentration of drug or vehicle for 72 h in SFM. Cell viability for cells growing under RCCs andPPSS are evaluated by the MTT assay. The absorbance of solubilized formazan is read at 570 nm using ELISA(enz

14、yme-linked immunosorbent assay) reader. In all cases, the highest concentration of DMSO is used in the controland this concentration is maintained below 0.001% (v/v). This DMSO concentration does not show any significantantiproliferative effect on the cell line in a short-term assay.MCE has not inde

15、pendently confirmed the accuracy of these methods. They are for reference only.Animal Mice3Administration 3 The S18 cells are injected near the scapula of the nude mice. Nine days after injection, the mice are randomly dividedinto four groups with six animals each (control, DDP, Nigericin and DDP co

16、mbined with Nigericin). DDP (2.5 mg/kg) isPage 2 of 3 www.MedChemEinjected intraperitoneally for five continuous days and nigericin (4 mg/kg) is administrated intraperitoneally every twodays. Tumor length and width are measured with a vernier caliper every other day. Tumor volume is calculated using

17、the formula V=0.5(lengthwidth2). The body weights of the mice are recorded every two days. Mice are humanelyeuthanized when the tumor volume reach 2000 mm3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Cell Metab. 2020 May 5;31(5):892-908.

18、e11. Cell Rep. 2019 May. Cell Death Dis. 2020 Feb 18;11(2):132. Front Microbiol, 30 April 2020 Appl Microbiol Biotechnol. 2017 May;101(10):4201-4213.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Yakisich JS, et al. Nigericin decreases the viability of multidrug-resistant cancer cells and lung tumorspheres and potentiates the effects of cardiacglycosides. Tumour Biol. 2017 Mar;39(3):10104283176943102. Bissinger R, et al. Triggering of Suicidal Erythrocyte Death by the Antibiotic Ionop