| Size | Price | Stock | Qty |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Ramifenazone targets the cyclooxygenase (COX) enzymes (COX-1 and COX-2), which are key enzymes in the biosynthesis of prostaglandins. By inhibiting COX enzymes, it reduces the production of prostaglandins, which are mediators of inflammation, pain, and fever. It has both analgesic and anti-inflammatory effects. The compound belongs to the pyrazolone class of NSAIDs.
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| ln Vitro |
In vitro, ramifenazone inhibits COX-1 and COX-2 enzyme activity, reducing prostaglandin synthesis. It exhibits analgesic and anti-inflammatory activity. Its in vitro potency and selectivity for COX-1 versus COX-2 have been characterized. The compound's in vitro activities are consistent with other pyrazolone NSAIDs. Detailed in vitro data are limited.
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| ln Vivo |
In vivo, ramifenazone is used for the relief of mild to moderate pain and inflammation. It has been used in the treatment of rheumatic disorders, musculoskeletal pain, and other inflammatory conditions. It has analgesic, anti-inflammatory, and antipyretic properties. Its use has declined due to safety concerns, including agranulocytosis and other blood disorders.
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| Enzyme Assay |
General protocols for COX enzyme inhibition assays use recombinant COX-1 and COX-2 enzymes. The enzyme is incubated with arachidonic acid substrate and varying concentrations of ramifenazone (0.1-1000 µM) in assay buffer (100 mM Tris-HCl pH 8.0, 5 mM EDTA, 2 mM phenol, 1 µM hematin) at 37°C for 5-10 minutes. The reaction is stopped by adding HCl. Prostaglandin E2 (PGE2) production is measured by ELISA. IC50 values for COX-1 and COX-2 inhibition are calculated from dose-response curves.
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| Cell Assay |
General protocols for anti-inflammatory activity assays use LPS-stimulated macrophages or whole blood. Cells are seeded in 24-well plates and treated with ramifenazone at various concentrations (1-500 µM) for 1 hour, then stimulated with LPS (1 µg/mL) for 24 hours. PGE2, TNF-α, and IL-6 levels in culture supernatants are measured by ELISA. The percentage inhibition of cytokine production is calculated. Cell viability is assessed by MTT.
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| Animal Protocol |
General protocols for in vivo analgesic activity use the acetic acid-induced writhing test or hot plate test in mice. Ramifenazone is administered orally or intraperitoneally at doses of 10-100 mg/kg. In the writhing test, mice are injected intraperitoneally with 0.6% acetic acid, and the number of writhes is counted for 15-20 minutes. In the hot plate test, the latency to paw licking or jumping is recorded. The percentage reduction in pain response is calculated. Indomethacin or aspirin serves as positive controls.
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| ADME/Pharmacokinetics |
Ramifenazone has a molecular weight of 293.36 g/mol (C18H19N3O). It is a pyrazolone NSAID. It is metabolized in the liver and excreted via the kidneys. Its pharmacokinetic properties include good oral absorption. The elimination half-life is several hours. Its use has declined due to safety concerns.
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| Toxicity/Toxicokinetics |
Ramifenazone has significant toxicity concerns. The most serious adverse effect is agranulocytosis, a potentially fatal blood disorder. Other adverse effects include gastrointestinal bleeding, ulceration, nausea, vomiting, and allergic reactions. It should not be used in patients with a history of blood disorders or NSAID hypersensitivity. Its use requires regular blood count monitoring. It is banned or restricted in many countries.
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| Additional Infomation |
1,5-Dimethyl-2-phenyl-4-(propyl-2-ylamino)-3-pyrazolone is a cyclic compound belonging to the pyrazolium class of compounds.
Ramifenazone (CAS 3615-24-5) is a pyrazolone NSAID with analgesic, anti-inflammatory, and antipyretic properties. It has been used for rheumatic disorders and musculoskeletal pain. Its use has declined significantly due to the risk of agranulocytosis and other blood disorders. It is banned or restricted in many countries and is not recommended for routine use. It is not approved by the FDA. |
| Molecular Formula |
C14H19N3O
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|---|---|
| Molecular Weight |
245.32016
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| Exact Mass |
245.152
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| CAS # |
3615-24-5
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| Related CAS # |
Ramifenazone-d7;1330180-51-2
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| PubChem CID |
5037
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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 |
348.5±45.0 °C at 760 mmHg
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| Flash Point |
164.6±28.7 °C
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| Vapour Pressure |
0.0±0.8 mmHg at 25°C
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| Index of Refraction |
1.595
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| LogP |
0.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
356
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1N(C2=CC=CC=C2)N(C)C(C)=C1NC(C)C
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| InChi Key |
XOZLRRYPUKAKMU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H19N3O/c1-10(2)15-13-11(3)16(4)17(14(13)18)12-8-6-5-7-9-12/h5-10,15H,1-4H3
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| Chemical Name |
1,5-dimethyl-2-phenyl-4-(propan-2-ylamino)pyrazol-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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). This product is not stable in solution, please use freshly prepared working solution for optimal results. |
| 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 | 4.0763 mL | 20.3815 mL | 40.7631 mL | |
| 5 mM | 0.8153 mL | 4.0763 mL | 8.1526 mL | |
| 10 mM | 0.4076 mL | 2.0382 mL | 4.0763 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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