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| Targets |
Morniflumate targets cyclooxygenase (COX) enzymes, specifically COX-1 and COX-2, which are involved in the synthesis of prostaglandins from arachidonic acid. As an NSAID, it inhibits prostaglandin synthesis, thereby reducing inflammation, pain, and fever. Morniflumate is a non-steroidal anti-inflammatory drug with antipyretic properties.
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| ln Vitro |
Morniflumate is an NSAID with anti-inflammatory, analgesic, and antipyretic properties. It is the morpholinoethyl ester of niflumic acid. Specific IC50 values for COX-1 and COX-2 inhibition are not extensively detailed in standard reference sources.
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| ln Vivo |
Morniflumate is used in the symptomatic treatment of inflammatory conditions in humans. It is indicated for the treatment of pain associated with ear, nose, throat (ENT) and gastrointestinal inflammatory conditions. In Italy, morniflumate is also indicated for use in children.
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| Enzyme Assay |
Morniflumate's inhibition of COX enzymes can be assessed using in vitro enzyme assays. Recombinant COX-1 or COX-2 enzymes are incubated with arachidonic acid in the presence of varying concentrations of morniflumate. Prostaglandin production is measured using a suitable detection method (e.g., ELISA) to determine the IC50.
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| Cell Assay |
The anti-inflammatory activity of morniflumate is evaluated in vitro using cell-based assays. Macrophages or other inflammatory cells are stimulated with LPS in the presence or absence of morniflumate. Pro-inflammatory cytokine production (e.g., TNF-α, IL-6, IL-1β) and prostaglandin E2 levels are measured by ELISA.
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| Animal Protocol |
Morniflumate is administered orally in clinical use. In preclinical studies, the compound would be evaluated in animal models of inflammation, such as carrageenan-induced paw edema in rats or adjuvant-induced arthritis. Efficacy is assessed by measuring paw swelling, inflammatory markers, and pain behavior.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Mean 0.12 L/kg 45 ml/min Metabolisms/Metabolites This study investigated the pharmacokinetics of nifluric acid administered orally to 12 subjects in two different formulations. Bioavailability and pharmacokinetic studies following oral and intravenous (IV) administration showed that nifluric acid esters are rapidly hydrolyzed in plasma after absorption from the gastrointestinal tract, releasing a free acidic form, which is the source of its anti-inflammatory effect. This ester has a gastric protective effect against the ulcerative effects of nifluric acid. Biological Half-Life 2 hours Morniflumate is a prodrug that is hydrolyzed to its active metabolite, niflumic acid. It has a molecular formula of C19H17F3N2O4 and a molecular weight of 394.35. Specific pharmacokinetic parameters such as half-life, bioavailability, and plasma protein binding are not extensively detailed in standard reference sources. |
| Toxicity/Toxicokinetics |
Protein Binding
It has strong binding affinity to plasma proteins and a bioavailability of approximately 100%. Morniflumate, as an NSAID, can cause common adverse effects including gastrointestinal disturbances, such as dyspepsia, nausea, and ulceration. It may also cause renal and cardiovascular effects. Specific LD50 values and organ-specific toxicity data are not extensively detailed in standard reference sources. |
| Additional Infomation |
Morniflumate belongs to the (trifluoromethyl)benzene family of compounds. Morniflumate is a nonsteroidal anti-inflammatory drug (NSAID) with antipyretic properties. It is a morpholine ethyl ester of niflurane. One study showed that patients with bronchitis experienced improvement in physical examination and clinical symptoms after taking Morniflumate. Indications: Morniflumate is indicated for the treatment of inflammatory diseases of the respiratory, otolaryngological, genitourinary, and skeletal systems in adults. In Italy, it is also indicated for the treatment of pain caused by otolaryngological and gastrointestinal inflammation in children. Morniflumate is a well-established NSAID that has been used for over thirty years in Italy (especially for the treatment of upper respiratory tract infections in children), France, Belgium, Austria, Switzerland, Spain, and Portugal; it is well-tolerated. Mechanism of Action: The main mechanism of action of niflurane and its esters is the inhibition of enzymes involved in the synthesis of inflammatory prostaglandins. This drug inhibits the cyclooxygenase and 5-lipoxygenase pathways, leading to fever and inflammation. Niflurane is a calcium-activated chloride channel blocker, used as an analgesic and anti-inflammatory agent to treat inflammatory diseases. Niflurane does not directly inhibit calcium channels or activate potassium channels. Instead, it selectively reduces the pressor response induced by norepinephrine and serotonin by inhibiting mechanisms that lead to the opening of voltage-gated calcium channels. Niflurane (NFA) exhibits biphasic behavior in human CLC-K channels, indicating the presence of two functionally distinct binding sites: an activating site and a blocking site.
Morniflumate (CAS# 65847-85-0) is a non-steroidal anti-inflammatory drug (NSAID) derived from niflumic acid. It is used in the symptomatic treatment of inflammatory conditions of the airways, ENT, and the urogenital and osteoarticular systems. Morniflumate is a prodrug that is hydrolyzed to its active metabolite, niflumic acid. |
| Molecular Formula |
C19H20F3N3O3
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|---|---|
| Molecular Weight |
395.3822
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| Exact Mass |
395.145
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| CAS # |
65847-85-0
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| Related CAS # |
86827-84-1 (HCl);65847-85-0;
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| PubChem CID |
72106
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
478.2±45.0 °C at 760 mmHg
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| Melting Point |
75-77ºC
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| Flash Point |
243.0±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.555
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| LogP |
4.79
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
501
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC(=C1)NC2=C(C=CC=N2)C(=O)OCCN3CCOCC3)C(F)(F)F
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| InChi Key |
LDXSPUSKBDTEKA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H20F3N3O3/c20-19(21,22)14-3-1-4-15(13-14)24-17-16(5-2-6-23-17)18(26)28-12-9-25-7-10-27-11-8-25/h1-6,13H,7-12H2,(H,23,24)
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| Chemical Name |
2-morpholin-4-ylethyl 2-[3-(trifluoromethyl)anilino]pyridine-3-carboxylate
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| Synonyms |
UP 164; UP-164; Morniflumate
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~125 mg/mL (~316.15 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.26 mM) (saturation unknown) in 10% DMSO + 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 20.8 mg/mL clear DMSO 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: 2.08 mg/mL (5.26 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5292 mL | 12.6461 mL | 25.2921 mL | |
| 5 mM | 0.5058 mL | 2.5292 mL | 5.0584 mL | |
| 10 mM | 0.2529 mL | 1.2646 mL | 2.5292 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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