| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Cyclooxygenase (COX). Ampyrone, like other pyrazolone derivatives, is believed to exert its analgesic and antipyretic effects through inhibition of cyclooxygenase enzymes, reducing prostaglandin synthesis. The compound may also have effects on other inflammatory mediators.
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|---|---|
| ln Vitro |
Ampyrone demonstrates analgesic and anti-inflammatory activity in vitro through inhibition of prostaglandin synthesis. The compound has been characterized in various in vitro assays for its ability to inhibit COX enzyme activity. It is also used as a chromogenic reagent in biochemical assays for the detection of phenols and peroxides.
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| ln Vivo |
In vivo, Ampyrone has been used as an analgesic and antipyretic agent. Its effects are mediated through inhibition of prostaglandin synthesis. The compound has been studied in various animal models of pain and fever. Its use as a therapeutic agent has been largely superseded by newer drugs with better safety profiles.
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| Enzyme Assay |
In vitro enzyme assays for Ampyrone involve measuring COX-1 and COX-2 activity in the presence of varying concentrations of the compound. The enzymes are incubated with arachidonic acid substrate, and prostaglandin production is measured using ELISA or other detection methods. IC50 values are determined from dose-response curves.
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| Cell Assay |
Cellular assays for Ampyrone involve culturing cells such as macrophages or fibroblasts and stimulating them with LPS or other inflammatory stimuli. Cells are treated with Ampyrone, and prostaglandin E2 production is measured by ELISA. The compound's effects on inflammatory cytokine production can also be assessed.
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| Animal Protocol |
In vivo animal studies for Ampyrone have been conducted in rodent models of pain and fever. The compound is typically administered orally or intraperitoneally. Analgesic activity is assessed using the acetic acid-induced writhing test or hot plate test. Antipyretic activity is assessed by measuring body temperature in febrile animals.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Ampyrone are limited. The compound has a molecular weight of 203.24 and a molecular formula of C11H13N3O. It is soluble in water and organic solvents. The compound is metabolized in the liver and excreted via the renal route. Detailed pharmacokinetic parameters are not extensively documented.
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| Toxicity/Toxicokinetics |
Ampyrone is generally well-tolerated but can cause side effects including gastrointestinal irritation and allergic reactions. It is contraindicated in patients with a history of hypersensitivity to pyrazolone derivatives. The compound has been associated with agranulocytosis in rare cases. Its use as a therapeutic agent has been largely discontinued due to safety concerns.
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| References | |
| Additional Infomation |
4-Aminoantipyrine is a pyrazolone compound belonging to the pyrazolone class. It is a derivative of antipyrine with an amino group substituted at the C-4 position. It is a metabolite of aminopyrine and methylaminopyrine. It has various pharmacological effects, including nonsteroidal anti-inflammatory drug, non-narcotic analgesic, antirheumatic drug, peripheral nervous system drug, EC 1.14.99.1 (prostaglandin intraperoxidase synthase) inhibitor, antipyretic, drug metabolite, and marine xenobiotic metabolite. It is a primary amino compound belonging to the pyrazolone class. Its function is related to that of antipyrine. A metabolite of aminopyrine, it has analgesic and anti-inflammatory properties. It can be used as a reagent in biochemical reactions to generate peroxides or phenolic compounds. Aminopyrine can stimulate liver microsomes and can also be used to measure extracellular fluid. See also: Aminopyrine (note moved to).
Ampyrone (4-aminoantipyrine) is a pyrazolone derivative with analgesic, antipyretic, and anti-inflammatory properties. It is a metabolite of aminopyrine and has been used as a reagent in biochemical assays. The compound is also used as a chromogenic reagent for the detection of phenols and peroxides. Its use as a therapeutic agent has been largely superseded by newer drugs. It is available for research purposes. |
| Molecular Formula |
C11H13N3O
|
|---|---|
| Molecular Weight |
203.2404
|
| Exact Mass |
203.105
|
| CAS # |
83-07-8
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| Related CAS # |
Ampyrone-d3;1329792-51-9
|
| PubChem CID |
2151
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.2±0.1 g/cm3
|
| Boiling Point |
309.0±45.0 °C at 760 mmHg
|
| Melting Point |
105-110 °C(lit.)
|
| Flash Point |
140.7±28.7 °C
|
| Vapour Pressure |
0.0±0.7 mmHg at 25°C
|
| Index of Refraction |
1.607
|
| LogP |
-0.4
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
15
|
| Complexity |
305
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
RLFWWDJHLFCNIJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C11H13N3O/c1-8-10(12)11(15)14(13(8)2)9-6-4-3-5-7-9/h3-7H,12H2,1-2H3
|
| Chemical Name |
4-amino-1,5-dimethyl-2-phenylpyrazol-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)
|
| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~246.01 mM)
H2O : ~50 mg/mL (~246.01 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 150 mg/mL (738.04 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.9203 mL | 24.6015 mL | 49.2029 mL | |
| 5 mM | 0.9841 mL | 4.9203 mL | 9.8406 mL | |
| 10 mM | 0.4920 mL | 2.4601 mL | 4.9203 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04621253 | Completed | Drug: Novalgin | Drug-drug Interaction | University Hospital, Basel, Switzerland | 2020-04-29 | Phase 1 |
| NCT05612516 | Completed | Procedure: Assessment of hydrogen peroxide levels in saliva using trays with reservoir. Procedure: Assessment of hydrogen peroxide levels in saliva using trays without reservoir. |
Consumption | Cairo University | 2024-01-10 | Not Applicable |
| NCT06248437 | Completed | Other: innovative nutraceutical-type food product that we designed called HIC1® from coffee mucilage |
Respiratory Function Loss Sarcopenia |
Fundación Cardiovascular de Colombia | 2019-03-30 |
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