| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Fenoprofen Calcium targets multiple molecular pathways. Its primary mechanism of action is the inhibition of cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2. By inhibiting COX, the compound reduces the production of prostaglandins, which are mediators of inflammation, pain, and fever. Fenoprofen Calcium is also a melanocortin receptors (MCRs) positive allosteric modulator (PAM). The compound increases ERK1/2 activation in HEK293T cells, suggesting involvement in the MAPK/ERK signaling pathway. The S-enantiomer of fenoprofen is more potent than the R-enantiomer in terms of COX inhibition. The compound's anti-inflammatory, analgesic, and antipyretic effects are primarily mediated through COX inhibition and the subsequent reduction of prostaglandin synthesis.
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| ln Vitro |
In vitro, Fenoprofen Calcium has been shown to inhibit COX-1 and COX-2 enzyme activity. It reduces the production of prostaglandins in various cell systems. The compound also acts as a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen Calcium increases ERK1/2 activation in HEK293T cells. The compound's anti-inflammatory effects can be assessed in cell culture models by measuring the production of pro-inflammatory mediators such as prostaglandins, cytokines, and nitric oxide. The compound's analgesic effects can be studied in cell-based assays of pain signaling.
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| ln Vivo |
In vivo, Fenoprofen Calcium has analgesic, anti-inflammatory, and antipyretic effects. It is used clinically for the treatment of rheumatoid arthritis, osteoarthritis, and mild to moderate pain. In animal models, the compound has been shown to reduce paw volume and reduce disease incidence in models of inflammation. The compound is administered orally, with typical doses of 10 mg/kg administered intraperitoneally twice per day. The compound's efficacy depends on the dose, route of administration, and the specific disease model.
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| Enzyme Assay |
For non-cellular enzyme assays, Fenoprofen Calcium can be tested for inhibition of COX-1 and COX-2 using standard enzyme activity assays. The enzymes are incubated with varying concentrations of the compound, and the production of prostaglandins is measured using spectrophotometric or radioimmunoassay methods. The IC₅₀ values for COX-1 and COX-2 inhibition can be determined. The compound's activity as a melanocortin receptor PAM can be assessed using radioligand binding assays or functional assays measuring cAMP accumulation.
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| Cell Assay |
For in vitro cell-based assays, cells are cultured and treated with Fenoprofen Calcium. Prostaglandin production is measured to assess COX inhibition. For melanocortin receptor studies, cells expressing melanocortin receptors are treated with the compound, and receptor activation is measured by cAMP accumulation or other downstream signaling events. ERK1/2 activation can be assessed by Western blotting using phospho-specific antibodies. Cell viability, proliferation, and inflammatory marker expression can be assessed using standard assays.
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| Animal Protocol |
For in vivo animal studies, Fenoprofen Calcium can be administered to animal models of inflammation and pain. The compound is typically administered orally or intraperitoneally. In models of arthritis, the compound's effects on paw volume, disease incidence, and inflammatory markers are assessed. In models of pain, the compound's analgesic effects are evaluated using behavioral assays. Pharmacokinetic and pharmacodynamic studies can be performed to characterize the compound's absorption, distribution, metabolism, and excretion.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Fenoprofen Calcium include a molecular weight of 262.31. The compound is the calcium salt of fenoprofen. It is administered orally and is well absorbed from the gastrointestinal tract. It is highly protein-bound and is metabolized in the liver. The compound is excreted in the urine. The pharmacokinetic profile of fenoprofen is characterized by a half-life of approximately 2-3 hours. The compound should be stored under appropriate conditions.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Some reviewers consider fenprofen acceptable during lactation. Due to limited published experience regarding fenprofen use during lactation, alternative medications may be preferred, especially when breastfeeding newborns or premature infants. ◉ Effects on Breastfed Infants No published information found as of the revision date. ◉ Effects on Lactation and Breast Milk No published information found as of the revision date. The side effect profile of Fenoprofen Calcium includes gastrointestinal disturbances (such as nausea, vomiting, and gastrointestinal bleeding), cardiovascular effects (such as increased risk of heart attack and stroke), and renal effects (such as decreased renal function). The compound may also cause hypersensitivity reactions in some patients. The compound should not be used in patients with a history of allergy to NSAIDs. The compound is intended for research use only and is not for human use in research settings. |
| Additional Infomation |
Anhydrous Fenoprofen calcium is the anhydrous form of Fenoprofen calcium salt. Fenoprofen calcium dihydrate is used as a nonsteroidal anti-inflammatory drug (NSAID) to treat mild to moderate pain and relieve pain and inflammation caused by conditions such as arthritis. It is a cyclooxygenase-2 inhibitor and a cyclooxygenase-1 inhibitor. It contains the Fenoprofen (1-) molecule. Fenoprofen calcium is the calcium salt form of Fenoprofen, a propionic acid derivative with analgesic, NSAID, and antirheumatic effects. Fenoprofen inhibits two isoenzymes of cyclooxygenase, thereby inhibiting prostaglandin synthesis and blocking the conversion of arachidonic acid to prostaglandins. Furthermore, Fenoprofen can activate peroxisome proliferator-activated receptor (PPAR)-α and -γ, thereby downregulating the production of leukotriene B4. Fenoprofen is a propionic acid derivative used as a nonsteroidal anti-inflammatory drug. See also: Fenoprofen (containing the active ingredient); Fenoprofen sodium (its salt form).
Fenoprofen Calcium is a nonsteroidal anti-inflammatory drug (NSAID) belonging to the propionic acid class. It inhibits cyclooxygenase (COX) enzymes and reduces prostaglandin production. The compound is also a melanocortin receptors (MCRs) positive allosteric modulator (PAM) and increases ERK1/2 activation. Fenoprofen Calcium is used for the relief of mild to moderate pain and for the treatment of rheumatoid arthritis and osteoarthritis. The compound is also known as LILLY-53858 Calcium. It is not currently approved for clinical use in research settings and is available only for research purposes. |
| Molecular Formula |
C30H26CAO6
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|---|---|
| Molecular Weight |
522.6018
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| Exact Mass |
522.135
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| CAS # |
34597-40-5
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| Related CAS # |
Fenoprofen Calcium hydrate;71720-56-4;Fenoprofen;29679-58-1
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| PubChem CID |
64746
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.183g/cm3
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| Boiling Point |
381.3ºC at 760mmHg
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| Flash Point |
141.7ºC
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| LogP |
7.179
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
37
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| Complexity |
265
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[Ca+2].O(C1C([H])=C([H])C([H])=C([H])C=1[H])C1=C([H])C([H])=C([H])C(=C1[H])C([H])(C(=O)[O-])C([H])([H])[H].O(C1C([H])=C([H])C([H])=C([H])C=1[H])C1=C([H])C([H])=C([H])C(=C1[H])C([H])(C(=O)[O-])C([H])([H])[H]
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| InChi Key |
VHUXSAWXWSTUOD-UHFFFAOYSA-L
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| InChi Code |
InChI=1S/2C15H14O3.Ca/c2*1-11(15(16)17)12-6-5-9-14(10-12)18-13-7-3-2-4-8-13;/h2*2-11H,1H3,(H,16,17);/q;;+2/p-2
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| Chemical Name |
calcium;2-(3-phenoxyphenyl)propanoate
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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) |
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 | 1.9135 mL | 9.5675 mL | 19.1351 mL | |
| 5 mM | 0.3827 mL | 1.9135 mL | 3.8270 mL | |
| 10 mM | 0.1914 mL | 0.9568 mL | 1.9135 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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