| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
| Targets |
Nifenazone targets cyclooxygenase (COX) enzymes, which are involved in the production of prostaglandins that mediate inflammation and pain. By inhibiting COX activity, Nifenazone reduces the synthesis of prostaglandins, thereby alleviating inflammation and pain. As an NSAID, it belongs to the pyrazolone class of anti-inflammatory drugs. The compound's analgesic and anti-inflammatory effects are mediated through this mechanism.
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| ln Vitro |
In vitro, Nifenazone exhibits a diverse range of bioactivities across multiple assays. It shows potency in inhibiting various targets. The compound's COX inhibitory activity has been characterized in biochemical assays. It also demonstrates anti-inflammatory effects in cell-based models. Detailed in vitro data are available in the pharmacological literature. Nifenazone is used as a reference NSAID in some studies.
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| ln Vivo |
In vivo, Nifenazone has been used as an analgesic for a number of rheumatic conditions. It is administered orally for the treatment of rheumatism and other inflammatory disorders. The compound's efficacy and safety have been evaluated in clinical studies. It is available as a drug in some countries. Detailed in vivo data are available in pharmacological and clinical literature.
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| Enzyme Assay |
In vitro COX inhibition assays for Nifenazone typically use purified COX-1 and COX-2 enzymes. The compound is dissolved in DMSO and diluted in assay buffer (100 mM Tris-HCl, pH 8.0, 5 mM EDTA, 2 μM heme). Enzyme and inhibitor are pre-incubated for 10-15 minutes, followed by addition of arachidonic acid substrate. Prostaglandin production is measured by ELISA or immunoassay. IC₅₀ values are calculated from dose-response curves. Controls include DMSO vehicle and reference COX inhibitors (e.g., indomethacin).
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| Cell Assay |
For cell-based assays, relevant cell lines (e.g., macrophages or synovial fibroblasts) are cultured in DMEM with 10% FBS. Cells are seeded in 96-well plates and treated with Nifenazone at various concentrations for 1-24 hours. Cells are stimulated with LPS or other inflammatory stimuli to induce COX-2 expression. Prostaglandin E₂ (PGE₂) levels in the culture medium are measured by ELISA. Cell viability is assessed by MTT. All treatments include vehicle controls and are performed in triplicate.
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| Animal Protocol |
In vivo, Nifenazone is typically administered orally to patients at doses specified in clinical guidelines. For animal studies, rodents are dosed orally or intraperitoneally. Pain models (e.g., carrageenan-induced paw edema, formalin test) are used to assess analgesic activity. Inflammation is assessed by paw swelling measurement or histological analysis. Blood samples are collected for pharmacokinetic analysis. All procedures follow institutional guidelines.
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| ADME/Pharmacokinetics |
Nifenazone is a pyrazolone NSAID with established pharmacokinetic properties. It is orally absorbed and distributed to tissues. The compound is metabolized in the liver and excreted in urine. Half-life and clearance parameters are available from pharmacological literature. The compound is available as a drug in some countries.
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| Toxicity/Toxicokinetics |
Nifenazone has been used clinically as an NSAID and has an established safety profile. Like other NSAIDs, it may cause gastrointestinal side effects. The compound is contraindicated in patients with NSAID hypersensitivity. Standard precautions for NSAID use apply. The compound is available as a pharmaceutical product in some countries.
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| References |
: The solvatochromic, spectral, and geometrical properties of nifenazone: a DFT/TD-DFT and experimental study. Phys Chem Chem Phys. 2014 Aug 7;16(29):15519-26.
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| Additional Infomation |
Nifenazon is a cyclic compound belonging to the pyrazole class of compounds.
Nifenazone is an NSAID used for the treatment of rheumatic conditions. It inhibits COX enzymes and reduces prostaglandin production. The compound is available as a drug in some countries. It is also available from chemical suppliers for research purposes. Its mechanism involves anti-inflammatory and analgesic activities. |
| Molecular Formula |
C17H16N4O2
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|---|---|
| Molecular Weight |
308.33454
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| Exact Mass |
308.127
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| CAS # |
2139-47-1
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| PubChem CID |
4487
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.33g/cm3
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| Melting Point |
252-253° (also reported as mp 256-258°)
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| Index of Refraction |
1.671
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| LogP |
2.204
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
511
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1=CC=CN=C1)NC2=C(C)N(C)N(C3=CC=CC=C3)C2=O
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| InChi Key |
BRZANEXCSZCZCI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H16N4O2/c1-12-15(19-16(22)13-7-6-10-18-11-13)17(23)21(20(12)2)14-8-4-3-5-9-14/h3-11H,1-2H3,(H,19,22)
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| Chemical Name |
N-(1,5-dimethyl-3-oxo-2-phenylpyrazol-4-yl)pyridine-3-carboxamide
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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) |
DMSO : ~16.67 mg/mL (~54.07 mM)
H2O : ~2 mg/mL (~6.49 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 1.67 mg/mL (5.42 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 16.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 1.67 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2 mg/mL (6.49 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2433 mL | 16.2164 mL | 32.4328 mL | |
| 5 mM | 0.6487 mL | 3.2433 mL | 6.4866 mL | |
| 10 mM | 0.3243 mL | 1.6216 mL | 3.2433 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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