| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| Other Sizes |
| Targets |
Propyphenazone primarily targets cyclooxygenase (COX) enzymes. As a weak nonselective COX inhibitor, it reduces the production of prostaglandins involved in pain and fever. Propyphenazone-based analogues selectively inhibit COX-2. The compound acts as a non-narcotic analgesic and peripheral nervous system drug. Its mechanism involves inhibition of prostaglandin synthesis, similar to other NSAIDs. Propyphenazone is a nonsteroidal anti-inflammatory drug with analgesic and antipyretic properties.
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| ln Vitro |
In vitro, Propyphenazone demonstrates weak nonselective COX inhibition. The compound shows anti-inflammatory, analgesic, and antipyretic activities in cell-based and enzyme-based assays. Propyphenazone-based analogues act as prodrugs and selectively inhibit COX-2. The compound’s effects on prostaglandin production are measured in various in vitro systems. Its minimal anti-inflammatory activity distinguishes it from other NSAIDs. Propyphenazone has been studied for its analgesic and antipyretic effects in preclinical models.
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| ln Vivo |
In vivo, Propyphenazone is orally active and has demonstrated analgesic, antipyretic, and anti-inflammatory effects. It has been used for the treatment of rheumatic disorders. The compound has the effect of reducing pain and antipyretic activity with minimal anti-inflammatory activity. Propyphenazone-based analogues act as prodrugs and selectively inhibit COX-2. Further in vivo studies have evaluated its efficacy in various animal models of pain and inflammation. The compound is typically administered orally.
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| Enzyme Assay |
In vitro enzyme assays for Propyphenazone involve measuring COX-1 and COX-2 enzyme inhibition. Enzyme activity is assessed by monitoring prostaglandin production from arachidonic acid substrate. Propyphenazone is added at varying concentrations, and IC50 values are calculated from dose-response curves. The compound’s weak nonselective COX inhibition is confirmed through these assays. For prodrug analogues, additional assays may be performed to assess conversion to active forms. Assays are performed in appropriate buffer systems with positive controls (e.g., ibuprofen or celecoxib).
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| Cell Assay |
In vitro cell-based assays for Propyphenazone are conducted in inflammatory cell models. Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with Propyphenazone at varying concentrations. Prostaglandin E2 levels in culture supernatants are measured by ELISA. Cytokine production may also be assessed. Cell viability is evaluated by MTT assay to ensure compound concentrations are not cytotoxic. Experiments are performed in triplicate with appropriate positive (e.g., other NSAIDs) and negative (vehicle) controls. IC50 values are calculated from dose-response curves.
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| Animal Protocol |
In vivo animal studies for Propyphenazone are conducted in rodent models of pain and inflammation. For analgesic evaluation, the hot plate test, tail flick test, or writhing test in mice may be used. For antipyretic evaluation, yeast-induced fever models in rats are employed. For anti-inflammatory evaluation, the carrageenan-induced paw edema model may be used. Propyphenazone is administered orally at various doses. Animals are monitored for clinical signs, and blood samples may be collected for pharmacokinetic analysis. Studies are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Propyphenazone (MW 230.31 g/mol) is an orally active NSAID with favorable drug-like properties. The compound is a non-acidic pyrazole derivative. It is soluble in DMSO. Propyphenazone is metabolized by hepatic enzymes. Following administration, the compound is distributed to tissues. Pharmacokinetic parameters including oral bioavailability, half-life, and tissue distribution have been characterized in preclinical studies. The compound shows stability under recommended storage conditions. Its prodrug analogues have been developed to improve pharmacokinetic properties.
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| Toxicity/Toxicokinetics |
Propyphenazone has a favorable safety profile as a clinically used NSAID. The compound has been used for the treatment of rheumatic disorders. Its weak nonselective COX inhibition suggests a lower risk of gastrointestinal side effects compared to more potent NSAIDs. No significant adverse effects have been reported at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation is available from clinical use data.
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| Additional Infomation |
Propipiridine is a pyrazolone derivative, a compound in which antipyrine is substituted with an isopropyl group at the C-4 position. It is a nonsteroidal anti-inflammatory drug, a non-narcotic analgesic, and a peripheral nervous system drug. Its function is similar to that of antipyrine.
Propyphenazone is a pyrazolone derivative with anti-inflammatory, analgesic, and antipyretic activity. It is an orally active non-acidic pyrazole NSAID that is a weak nonselective COX inhibitor. Propyphenazone has the effect of reducing pain and antipyretic activity with minimal anti-inflammatory activity. Propyphenazone-based analogues are widely used as prodrugs and selectively inhibit COX-2. The compound is used for the treatment of rheumatic disorders. All research applications are limited to non-human use. |
| Molecular Formula |
C14H18N2O
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|---|---|
| Molecular Weight |
230.3055
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| Exact Mass |
230.141
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| CAS # |
479-92-5
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| Related CAS # |
Propyphenazone-d3;162935-29-7
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| PubChem CID |
3778
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
319.0±25.0 °C at 760 mmHg
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| Melting Point |
102-105°C
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| Flash Point |
123.8±15.5 °C
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| Vapour Pressure |
0.0±0.7 mmHg at 25°C
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| Index of Refraction |
1.556
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| LogP |
1.74
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
17
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| Complexity |
340
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1C(=C(C([H])([H])[H])N(C([H])([H])[H])N1C1C([H])=C([H])C([H])=C([H])C=1[H])C([H])(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
PXWLVJLKJGVOKE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H18N2O/c1-10(2)13-11(3)15(4)16(14(13)17)12-8-6-5-7-9-12/h5-10H,1-4H3
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| Chemical Name |
1,5-dimethyl-2-phenyl-4-propan-2-ylpyrazol-3-one
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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 : ≥ 2.6 mg/mL (~11.29 mM)
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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 | 4.3420 mL | 21.7099 mL | 43.4197 mL | |
| 5 mM | 0.8684 mL | 4.3420 mL | 8.6839 mL | |
| 10 mM | 0.4342 mL | 2.1710 mL | 4.3420 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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