| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Neamine tetrahydrochloride primarily targets the bacterial 30S ribosomal subunit by binding to the decoding region of 16S rRNA. It interacts with the A-site of 16S rRNA, specifically with the Hoogsteen face of guanine residues and the phosphodiester backbone. This binding interferes with translational fidelity and inhibits protein synthesis, leading to bacterial growth inhibition. Neamine also targets angiogenin, a protein involved in angiogenesis, and inhibits its ribonucleolytic activity.
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|---|---|
| ln Vitro |
Neamine treatment (0.625-25 μM; 48 hours; AsPC-1 cells) dose-dependently suppresses the proliferation of ANG-mediated AsPC-1 cells in the range of 0.625-25 μM[1]. Neamine (100 μM) also successfully prevents ANG from translocating nuclear[1].
In vitro, neamine tetrahydrochloride exhibits broad-spectrum antibacterial activity against Gram-negative and Gram-positive bacteria. It binds to the A-site of 16S rRNA and perturbs ribosomal subunit rotation by interacting with helices h44 and H69. As an anti-angiogenic agent, neamine inhibits angiogenin-induced angiogenesis and endothelial cell proliferation. It is a key pharmacophore for aminoglycoside-RNA interactions, though its potency is lower than that of full-length neomycin. |
| ln Vivo |
In AsPC-1 xenograft models, neamine (30–60 mg/kg; subcutaneous injection; daily; for 14 days; male Balb/c nude mice) has anti-tumor properties. In tumor xenografts, neamine lowers the expression levels of ANG, Ki-67, and CD31[1].
In vivo, neamine tetrahydrochloride demonstrates antibacterial efficacy in animal infection models. Its anti-angiogenic activity has been evaluated in tumor xenograft models, where it inhibits angiogenesis and tumor growth by targeting angiogenin. The compound is used as a research tool for studying aminoglycoside-RNA interactions and angiogenesis. No approved therapeutic use exists for neamine alone, and clinical data are limited. |
| Enzyme Assay |
For non-cell enzyme/receptor binding assays, the bacterial 30S ribosomal subunit or a model A-site RNA oligonucleotide is incubated with neamine tetrahydrochloride in binding buffer. Binding affinity is measured by fluorescence quenching, surface plasmon resonance (SPR), or isothermal titration calorimetry (ITC). Competition assays with radiolabeled aminoglycosides such as paromomycin can determine relative binding affinities.
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: AsPC-1 cells Tested Concentrations: 0.625 µM, 1.25 µM, 2.5 µM, 5 µM, 10 µM, 25 µM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibited angiogenin (ANG)-induced AsPC-1 cells proliferation. In cell-based assays, bacterial cultures are grown in Mueller-Hinton broth, and neamine tetrahydrochloride is serially diluted in 96-well plates. After incubation at 35-37°C for 16-20 hours, MIC values are determined by visual or spectrophotometric growth inhibition. For anti-angiogenic studies, endothelial cells are treated with neamine, and cell proliferation is measured by MTT or BrdU incorporation. |
| Animal Protocol |
Animal/Disease Models: Male Balb/c nude mice (4 weeks old) injected with AsPC-1 cells[1]
Doses: 30 mg/kg, 60 mg/kg Route of Administration: subcutaneous (sc)injection; daily; for 14 days Experimental Results: Had anti-tumor effects on AsPC-1 xenograft models. For in vivo animal studies, mice with systemic bacterial infection are treated with neamine tetrahydrochloride administered intraperitoneally or intravenously. Survival, bacterial burden in blood and tissues, and histopathology are assessed. For anti-angiogenic studies, tumor xenograft models in mice are used, and neamine is administered to evaluate tumor growth inhibition, microvessel density, and angiogenin target engagement. Pharmacokinetic parameters are determined by LC-MS. |
| References |
| Molecular Formula |
C12H30CL4N4O6
|
|---|---|
| Molecular Weight |
468.20
|
| Exact Mass |
466.092
|
| CAS # |
15446-43-2
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| Related CAS # |
Neamine;3947-65-7
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| PubChem CID |
11784617
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| Appearance |
White to off-white solid powder
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| LogP |
0.893
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| Hydrogen Bond Donor Count |
12
|
| Hydrogen Bond Acceptor Count |
10
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
26
|
| Complexity |
378
|
| Defined Atom Stereocenter Count |
10
|
| SMILES |
NCC1O[C@H](O[C@@H]2C(N)C[C@@H](N)C(O)[C@H]2O)C(N)[C@@H](O)[C@@H]1O
|
| InChi Key |
YHGAXELMYJIVJN-OXGCEHIISA-N
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| InChi Code |
InChI=1S/C12H26N4O6.4ClH/c13-2-5-8(18)9(19)6(16)12(21-5)22-11-4(15)1-3(14)7(17)10(11)20;;;;/h3-12,17-20H,1-2,13-16H2;4*1H/t3-,4+,5-,6-,7+,8-,9-,10-,11-,12-;;;;/m1..../s1
|
| Chemical Name |
(2R,3S,4R,5R,6R)-5-amino-2-(aminomethyl)-6-[(1R,2R,3S,4R,6S)-4,6-diamino-2,3-dihydroxycyclohexyl]oxyoxane-3,4-diol;tetrahydrochloride
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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 | 2.1358 mL | 10.6792 mL | 21.3584 mL | |
| 5 mM | 0.4272 mL | 2.1358 mL | 4.2717 mL | |
| 10 mM | 0.2136 mL | 1.0679 mL | 2.1358 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.
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