Size | Price | |
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50mg | ||
100mg | ||
250mg |
Purity: ≥98%
Nigericin, a natural antibiotic extracted from Streptomyces hygroscopicus, is a novel and potent cationic ionophore that inhibits Golgi function and suppresses growth of gram positive bacteria. It also prevents viral activation and triggers activation of the NALP3 inflammasome. Nigericin sodium works by acting as an H+, K+, and Pb2+ ionophore.
ln Vitro |
Through caspase 1/GSDMD, nigericin (0–4 μg/ml; 24 hours) effectively causes pyroptosis in TNBC cells [6]. With its focused action, nigericin (0-0.25 μg/ml; 24 hours) suppresses the upregulation of Wnt/β-catenin in H460 cells and exhibits anti-cancer properties [7]. Gram-positive bacteria are resistant to antibiotics[4].
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ln Vivo |
Mice with Staphylococcus aureus USA300 infection can be lessened by administering 1 mg/kg of nigericin intraperitoneally every 12 hours for three days [4]. Nigericin (subcutaneous injection, once every two days; 0.025 mg/kg)
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Cell Assay |
Cell viability assay [4]
Cell Types: Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis, Enterococcus faecium, Streptococcus pneumoniae) and Streptococcus agalactiae Tested Concentrations: 0 μg/ml, 0.05 μg/ml, 0.125 μg/ ml, 0.25 μg/ml Incubation Duration: 24 hrs (hours) Experimental Results: demonstrated potent activity against these clinical MDR strains with MIC values ranging from 0.004-0.25 mg/ml. Western Blot Analysis[6] Cell Types: MDA-MB-231 and 4T1 Cell Tested Concentrations: 0 μg/ml, 2 μg/ml, 4 μg/ml Incubation Duration: 24 hrs (hours) Experimental Results: Shows increased caspase 1 protein levels and N-GSDMD . Cell viability assay [7] Cell Types: H460 Cell Tested Concentrations: 0.5 μM, 1 μM, 2.5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Down-regulation of expression of classic Wnt proteins (LRP6, Wnt5a/b and β-catenin) signaling pathway. |
Animal Protocol |
Animal/Disease Models: balb/c (Bagg ALBino) mouse orthotopically injected with 4T1 cells [6]
Doses: 0.025 mg/kg Route of Administration: subcutaneous injection Experimental Results: Shown almost complete inhibition of tumor growth with anti-PD-1 antibody. Animal/Disease Models: Staphylococcus aureus-infected mice USA300[4] Doses: 1 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Major The bacterial load in the organs is diminished to 1,000-10,000 times. |
References |
[1]. Zotova L, et al. Novel components of an active mitochondrial K(+)/H(+) exchange. J Biol Chem. 2010 May 7;285(19):14399-414.
[2]. Mariathasan S, et al.Cryopyrin activates the inflammasome in response to toxins and ATP.Nature. 2006 Mar 9;440(7081):228-32. [3]. Bissinger R, et al. Triggering of Suicidal Erythrocyte Death by the Antibiotic Ionophore Nigericin. Basic Clin Pharmacol Toxicol. 2016 May;118(5):381-9. [4]. Xiaoli Zhu, et al. Nigericin is effective against multidrug resistant gram-positive bacteria, persisters, and biofilms. Front Cell Infect Microbiol. 2022 Dec 20:12:1055929. [5]. Guanzhuang Gao, et al. Evidence of nigericin as a potential therapeutic candidate for cancers: A review. Biomed Pharmacother. 2021 May:137:111262. [6]. Lisha Wu, et al. Nigericin Boosts Anti-Tumor Immune Response via Inducing Pyroptosis in Triple-Negative Breast Cancer. Cancers (Basel). 2023 Jun 16;15(12):3221. [7]. Juan Sebastian Yakisich, et al. Nigericin decreases the viability of multidrug-resistant cancer cells and lung tumorspheres and potentiates the effects of cardiac glycosides. Tumour Biol.2017 Mar;39(3):1010428317694310. |
Molecular Formula |
C40H68O11
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Molecular Weight |
746.94318
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CAS # |
28380-24-7
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Related CAS # |
Nigericin sodium salt;28643-80-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C[C@H]([C@H]1[C@@H](C)CC[C@H](C[C@H](C[C@@H](OC)[C@H]2C)O[C@]32[C@H](C)C[C@@](C)([C@@H]4O[C@](C)([C@@H]5O[C@@H]([C@@H]6[C@@H](C)C[C@@H](C)[C@@](CO)(O)O6)C[C@@H]5C)CC4)O3)O1)C(O[Na])=O
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InChi Key |
MOYOTUKECQMGHE-PDEFJWSRSA-M
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InChi Code |
InChI=1S/C40H68O11.Na/c1-21-11-12-28(46-33(21)26(6)36(42)43)17-29-18-30(45-10)27(7)40(48-29)25(5)19-38(9,51-40)32-13-14-37(8,49-32)35-23(3)16-31(47-35)34-22(2)15-24(4)39(44,20-41)50-34/h21-35,41,44H,11-20H2,1-10H3,(H,42,43)/q+1/p-1/t21-,22-,23-,24+,25+,26+,27+,28+,29+,30+,31+,32+,33+,34-,35+,37-,38-,39-,40+/m0./s1
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Chemical Name |
sodium
(R)-2-((2R,3S,6R)-6-(((2S,4R,5R,7R,9R,10R)-2-((2S,2'R,3'S,5R,5'R)-5'-((2S,3S,5R,6R)-6-hydroxy-6-(hydroxymethyl)-3,5-dimethyltetrahydro-2H-pyran-2-yl)-2,3'-dimethyloctahydro-[2,2'-bifuran]-5-yl)-9-methoxy-2,4,10-trimethyl-1,6-dioxaspiro[4.5]decan-7-yl)methyl)-3-methyltetrahydro-2H-pyran-2-yl)propanoate
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Synonyms |
Azalomycin M,Antibiotic K178, Helexin C,Antibiotic X464, Polyetherin A
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.3388 mL | 6.6940 mL | 13.3880 mL | |
5 mM | 0.2678 mL | 1.3388 mL | 2.6776 mL | |
10 mM | 0.1339 mL | 0.6694 mL | 1.3388 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.