| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
Bacterial flavoproteins/nitrofuran reductases (activation); ribosomal proteins; bacterial DNA and RNA; multiple intracellular targets; cell-wall synthesis.
|
|---|---|
| ln Vitro |
Nitrofurantoin sodium treatment (0-512 mg/L; 8 hours) suppresses E. coli growth. isolates of E. Coli [3].
Nitrofurantoin sodium is activated by bacterial nitrofuran reductases to reactive intermediates that inhibit inducible enzyme synthesis at concentrations equivalent to its MIC. It inhibits bacterial DNA, RNA, protein and cell-wall synthesis, and it is bactericidal through multiple interconnected metabolic pathways, including aminoacyl-tRNA biosynthesis and purine metabolism. Its activity is largely confined to the urinary tract because systemic levels are low. |
| ln Vivo |
1.19 Nitrofurantoin's pharmacokinetic effects in SD rats [4]. Ten milligrams per kilogramme; 2 milligrams per kilogramme for intravenous injection; 306 AUC0-120 (μg/mL·min); 90.3 AUC0-∞ (μg/mL·min); 344 91.5 Cmax (μg/mL); 1.01 CL/F or CL (ml/min/kg); 31.0 22.7 t1/2 (min) 166 23.6 Bioavailability (%) 60.1
In vivo, nitrofurantoin sodium is orally active and achieves high urinary concentrations, making it effective for uncomplicated cystitis. It is not used for systemic infections because tissue penetration is poor. Typical adult doses are 50–100 mg four times daily, and renal impairment reduces efficacy and increases toxicity. |
| Enzyme Assay |
For antibacterial susceptibility testing, uropathogenic E. coli and other isolates are cultured in Mueller–Hinton broth and exposed to two-fold serial dilutions of nitrofurantoin sodium (0.5–128 μg/mL). The MIC is determined after 16–20 h at 35–37°C, and time–kill assays assess bactericidal kinetics.
|
| Cell Assay |
Cell Viability Assay[3]
Cell Types: E. coli Isolates: DA10708, DA13815, DA13824, DA13957, DA13992, DA10626, DA10627 Tested Concentrations: 0, 32, 64, 128, 256 and 512 mg/L Incubation Duration: 8 hrs (hours) Experimental Results: For DA10708, DA13815 and DA13824, a bactericidal effect was observed at 32 mg/L. The growth of DA13957 and DA13992 was completely inhibited at 128 mg/L, and a bactericidal effect was observed at 256 mg/L. DA10626 and DA10627 demonstrated moderate lethality at >128 mg/L. For mechanism-based assays, bacterial cultures are treated with nitrofurantoin sodium at sub-MIC concentrations, and inducible enzyme synthesis (e.g., β-galactosidase) is measured. Reactive intermediate formation can be assessed by measuring nitrofuran reduction using bacterial lysates and NADPH. |
| Animal Protocol |
For in vivo studies, mice with ascending urinary tract infection receive nitrofurantoin sodium (e.g., 10–50 mg/kg, oral) and bacterial burden in bladder and kidneys is quantified by CFU counting. Urine and plasma drug concentrations are measured by LC-MS/MS to relate urinary exposure to efficacy.
|
| References |
|
| Additional Infomation |
Nitrofurantoin sodium is the sodium salt form of nitrofurantoin, a synthetic derivative of imidazolidinedione (hydantoin), which inhibits the synthesis of bacterial DNA, RNA, and cell wall proteins. See also: Nitrofurantoin (with active moiety).
|
| Molecular Formula |
C8H6N4NAO5
|
|---|---|
| Molecular Weight |
261.1463
|
| Exact Mass |
260.016
|
| CAS # |
54-87-5
|
| Related CAS # |
Nitrofurantoin;67-20-9;Nitrofurantoin-13C3;1217226-46-4
|
| PubChem CID |
9562058
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.81g/cm3
|
| Melting Point |
263ºC
|
| LogP |
0.683
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
18
|
| Complexity |
401
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1C(=NC(=O)N1N=CC2=CC=C(O2)[N+](=O)[O-])[O-].[Na+]
|
| InChi Key |
AFDJQFFKYDCYIG-JSGFVSQVSA-M
|
| InChi Code |
InChI=1S/C8H6N4O5.Na/c13-6-4-11(8(14)10-6)9-3-5-1-2-7(17-5)12(15)16;/h1-3H,4H2,(H,10,13,14);/q;+1/p-1/b9-3+;
|
| Chemical Name |
sodium;3-[(E)-(5-nitrofuran-2-yl)methylideneamino]-2-oxo-4H-imidazol-5-olate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~191.5 mM; with ultrasonication and warming by heating to 60°C)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (19.15 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (50.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (19.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (50.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8292 mL | 19.1461 mL | 38.2922 mL | |
| 5 mM | 0.7658 mL | 3.8292 mL | 7.6584 mL | |
| 10 mM | 0.3829 mL | 1.9146 mL | 3.8292 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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