| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| Other Sizes |
| Targets |
Famprofazone acts as a nonsteroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic, and anti-inflammatory properties. Like other pyrazolone derivatives, it is believed to inhibit cyclooxygenase (COX) enzymes, thereby reducing prostaglandin synthesis. However, its precise molecular targets are not fully characterized in publicly available literature.
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|---|---|
| ln Vitro |
In vitro, Famprofazone exhibits anti-inflammatory activity by inhibiting prostaglandin synthesis through COX enzyme inhibition. It demonstrates analgesic effects in various in vitro pain models. The compound's pyrazolone ring structure is characteristic of its class and contributes to its pharmacological activity. Specific in vitro potency data are not extensively documented.
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| ln Vivo |
In vivo, Famprofazone is used for its analgesic and antipyretic effects, effectively alleviating pain and reducing fever. It has been studied for the treatment of arthritis and muscle pain. Following administration, Famprofazone is metabolized to methamphetamine and amphetamine, which may contribute to its pharmacological effects.
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| Enzyme Assay |
The in vitro enzyme assay for Famprofazone typically involves measuring its inhibitory effect on cyclooxygenase (COX-1 and COX-2) enzymes. Recombinant COX enzymes are incubated with varying concentrations of Famprofazone and arachidonic acid substrate. Prostaglandin production is measured using ELISA or radiometric methods. The IC50 for COX inhibition is determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for Famprofazone involve treating cultured inflammatory cells (e.g., macrophages) with varying concentrations of the compound. Pro-inflammatory cytokine production (e.g., TNF-α, IL-6, PGE2) is measured by ELISA. Cell viability is assessed using MTT assays to determine cytotoxicity. NF-κB activation may also be evaluated using reporter gene assays.
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| Animal Protocol |
In vivo animal experiments for Famprofazone typically use rodent models of pain and inflammation, such as the carrageenan-induced paw edema model or the acetic acid-induced writhing test. Famprofazone is administered via oral or intraperitoneal routes at various doses. Pain responses and edema are measured at specific time points. The compound's analgesic and anti-inflammatory effects are compared to reference NSAIDs.
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| ADME/Pharmacokinetics |
Famprofazone is known to be metabolized to methamphetamine and amphetamine following administration, which has implications for its pharmacokinetic and safety profile. The compound has a molecular weight of 377.52. As an NSAID, it is expected to be well-absorbed orally, extensively protein-bound, and metabolized in the liver. Specific PK parameters are not well documented in public literature.
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| Toxicity/Toxicokinetics |
Famprofazone, as an NSAID, may cause gastrointestinal ulceration, bleeding, and renal impairment with chronic use. The metabolism of Famprofazone to methamphetamine and amphetamine raises concerns about central nervous system stimulant effects and potential for abuse. The compound is contraindicated in patients with peptic ulcer disease, severe renal impairment, or hypersensitivity to pyrazolone derivatives.
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| Additional Infomation |
1-Methyl-5-[[methyl(1-phenylprop-2-yl)amino]methyl]-2-phenyl-4-prop-2-yl-3-pyrazolone belongs to the pyrazole class of compounds and is a cyclic compound. Faprodone is a nonsteroidal anti-inflammatory drug (NSAID) found in combination formulations, such as "Gevodin" sold in Taiwan. It is important to note that this drug is metabolized in the body to methamphetamine and amphetamine, which may lead to a positive drug test result. Faprodone has been added to the World Anti-Doping Agency's (WADA) list of prohibited substances.
Famprofazone (CAS#: 22881-35-2) is a pyrazolone derivative NSAID used for its analgesic, antipyretic, and anti-inflammatory properties. It is also known as Geodowin. A unique feature of Famprofazone is its metabolism to methamphetamine and amphetamine following administration. The compound is not approved for clinical use in major markets and remains a research compound. No active clinical trials are registered for Famprofazone. |
| Molecular Formula |
C24H31N3O
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|---|---|
| Molecular Weight |
377.532
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| Exact Mass |
377.247
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| Elemental Analysis |
C, 76.35; H, 8.28; N, 11.13; O, 4.24
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| CAS # |
22881-35-2
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| PubChem CID |
3326
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| Appearance |
White to off-white solid powder
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| Density |
1.083g/cm3
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| Boiling Point |
485.1ºC at 760mmHg
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| Flash Point |
184.8ºC
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| Vapour Pressure |
1.45E-09mmHg at 25°C
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| Index of Refraction |
1.574
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| LogP |
4.362
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
558
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)C1=C(CN(C)C(C)CC2=CC=CC=C2)N(C)N(C3=CC=CC=C3)C1=O
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| InChi Key |
GNUXVOXXWGNPIV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H31N3O/c1-18(2)23-22(17-25(4)19(3)16-20-12-8-6-9-13-20)26(5)27(24(23)28)21-14-10-7-11-15-21/h6-15,18-19H,16-17H2,1-5H3
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| Chemical Name |
1-methyl-5-[[methyl(1-phenylpropan-2-yl)amino]methyl]-2-phenyl-4-propan-2-ylpyrazol-3-one
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| Synonyms |
BRN 5768367; Geodowin; BRN 5768,367; BRN-5768367; BRN5768367; Famprofazone
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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) |
Ethanol : ~25 mg/mL (~66.22 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.62 mM) (saturation unknown) in 10% EtOH + 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 25.0 mg/mL clear EtOH 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: ≥ 2.5 mg/mL (6.62 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear EtOH stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6488 mL | 13.2440 mL | 26.4880 mL | |
| 5 mM | 0.5298 mL | 2.6488 mL | 5.2976 mL | |
| 10 mM | 0.2649 mL | 1.3244 mL | 2.6488 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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