尼日利亚菌素钠盐作用机制 - Medchemexpress - MCE中国

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

2、th溶解性数据体外实验 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制备储备液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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。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。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可

4、以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 6.25 mg/mL (8.37 mM); Clear solution此案可获得 6.25 mg/mL (8.37 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 62.5 mg/mL 的澄 EtOH 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% EtOH 90% (20

5、% SBE-CD in saline)Page 1 of 2 www.MedChemESolubility: 6.25 mg/mL (8.37 mM); Clear solution此案可获得 6.25 mg/mL (8.37 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 62.5 mg/mL 的澄均匀。EtOH 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合3. 请依序添加每种溶剂： 10% EtOH 90% corn oilSolubility: 6.25 mg/mL (8.37 mM); Clear solution此案可获得 6.25 mg

6、/mL (8.37 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 62.5 mg/mL 的澄 EtOH 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Nigericin sodium salt。从吸链霉 中得到的种抗素，作为 H+，K+ 和 Pb2+ 离载体起作，NLRP3 的激动剂体外研究 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.体内研究 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.户使本产品发表的科研献 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