Fepradinol
Fepradinol is an orally active nonsteroidal anti-inflammatory agent. Fepradinol inhibits the increase in vascular permeability induced by histamine, 5-hydroxytryptamine, and bradykinin, reduces exudate volume, prevents leukocyte migration, and suppresses acute inflammation models. Fepradinol also induces thrombotic vasculopathy with epidermal necrosis, without leukocytoclastic vasculitis; triggers occlusive contact dermatitis presenting as purpuric papulonecrotic lesions, and causes strongly positive patch test reactions. Fepradinol can be used in research related to occlusive contact dermatitis and acute inflammation.
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- CAS. Nr.: 36981-91-6
- Formel: C12H19NO2
- Molecular Weight:209.28
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
In Vivo
Fepradinol (25 mg/kg; oral; single administration; 30 minutes before zymosan injection) inhibited dye exudation by 67.2% in the early phase (30 min) of zymosan-induced rat peritonitis, and reduced exudate volume by 27% and dye exudation by 50% in the late phase (3 h)[2].
Fepradinol (100 mg/kg; oral; single administration; administered immediately after carrageenan injection) reduced exudate volume by 67.2% and leukocyte migration by 76.4% in a carrageenan-induced rat pleurisy model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male, 5-7 weeks old, 150-200 g)[2]
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Dosage:25 mg/kg
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Administration:p.o.; single dose; 30 min prior to mediator injection
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Result:Inhibited histamine-induced vascular permeability by 81.1%.
Inhibited serotonin-induced vascular permeability by 82.0%.
Inhibited bradykinin-induced vascular permeability by 64.1%.
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Animal Model:Wistar (male, 150-200 g)[2]
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Dosage:100 mg/kg
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Administration:p.o.; single dose; immediately after carrageenin injection
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Result:Reduced pleural exudate volume by 67.2%.
Inhibited leucocyte mobilization by 76.4%.
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Animal Model:Wistar (male, 150-200 g)[2]
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Dosage:25 mg/kg
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Administration:p.o.; single dose; 30 min prior to zymosan injection
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Result:Inhibited dye extravasation by 67.2% at 30 min after zymosan challenge with no effect on exudate volume.
Reduced exudate volume by 27% at 3 h after zymosan challenge.
Inhibited dye extravasation by 50% at 3 h after zymosan challenge.
Chemical Information
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CAS. Nr. 36981-91-6
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Molecular Weight 209.28
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Formel C12H19NO2
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SMILES
OC(CNC(C)(C)CO)C1=CC=CC=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell migration
Cell migration is a method that plays an important role in wound healing, cell differentiation, embryonic development, etc.
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Carrageenan-Induced Paw Edema
Carrageenan-induced paw edema is an acute inflammation model in which intraplantar injection of carrageenan induces localized inflammatory swelling characterized by vascular permeability, leukocyte infiltration, and production of inflammatory mediators such as prostaglandins and cytokines, making it widely used to evaluate anti-inflammatory agents in vivo. The resulting paw volume or thickness increase is quantified over time as a direct readout of inflammatory intensity and drug efficacy, typically reflecting cyclooxygenase-mediated prostaglandin-driven edema formation and immune cell recruitment in peripheral tissue[20].
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TPA/Croton Oil Ear Edema and Dermatitis
The TPA (12-O-tetradecanoylphorbol-13-acetate) and croton oil-induced mouse ear edema model is a well-established acute cutaneous inflammation system used to evaluate topical anti-inflammatory activity by measuring edema formation, neutrophil infiltration, vascular permeability, and cytokine-mediated skin responses in vivo. The inflammatory response is triggered by topical application of phorbol esters (TPA) or croton oil constituents, leading to rapid activation of protein kinase C signaling, leukocyte recruitment, and increased vascular permeability, which can be quantified by ear thickness, weight, dye extravasation, and biochemical markers such as myeloperoxidase (MPO) activity and pro-inflammatory mediators in ear tissue homogenates. This model is widely used for screening anti-inflammatory agents, where reductions in edema and inflammatory biomarkers reflect suppression of acute dermal inflammation and immune cell infiltration. Histological evaluation typically confirms epidermal
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Zymosan-Induced Peritonitis
Zymosan-induced peritonitis is a sterile acute-inflammation model produced by intraperitoneal injection of zymosan, a yeast cell-wall particle preparation, followed by quantification of leukocyte recruitment and soluble inflammatory mediators in peritoneal lavage fluid. Low-dose zymosan peritonitis is commonly used as a self-resolving acute inflammation model in which neutrophil recruitment occurs early and monocyte/macrophage accumulation follows later. The assay readouts include total peritoneal leukocyte number, differential neutrophil and monocyte/macrophage counts, peritoneal cytokines and chemokines, plasma or peritoneal exudation, and optional lipidomic or metabolomic changes during inflammation and resolution. Early neutrophil recruitment after zymosan depends strongly on complement and mast-cell C5a receptor signaling, whereas later monocyte recruitment is linked to MCP-1/CCL2 production.
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
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Contact Hypersensitivity Dermatitis
Contact hypersensitivity (CHS) dermatitis is a T cell-mediated delayed-type (Type IV) immune reaction in which low-molecular-weight haptens applied to the skin bind host proteins to form complete antigens, triggering sensitization followed by a secondary inflammatory response upon re-exposure (elicitation phase), which is commonly quantified by ear swelling as a readout of skin inflammation in murine models. This model is widely used to study allergic contact dermatitis because it is antigen-specific, reproducible, and reflects key immunological events including dendritic cell activation, T cell priming in draining lymph nodes, and effector T cell-driven tissue inflammation. DNFB- and oxazolone-induced CHS models are standard systems for evaluating both acute and chronic T cell-dependent skin inflammation and for testing immunomodulatory interventions.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Calculators
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