| Name | Tepoxalin |
| Description | Tepoxalin (RWJ 20485) is a 5-lipoxygenase inhibitor potentially for the treatment of asthma, osteoarthritis. Tepoxalin inhibits COX-1, COX-2, and 5-LOX. Tepoxalin is a potent inhibitor of sheep seminal vesicle cyclooxygenase (COX) (IC50 = 4.6 microM), rat basophilic leukemia cell (RBL-1) lysate COX (IC50 = 2.85 microM) and COX from intact RBL-1 cells (IC50 = 4.2 microM). |
| In vitro | Tepoxalin inhibits the production of thromboxane B2 (TxB2) in Ca++ ionophore A-23187-stimulated human peripheral blood leukocytes (HPBL; IC50 = 0.01 microM) and human whole blood (IC50 = 0.08 microM) and is a potent inhibitor of epinephrine-induced human platelet aggregation (IC50 = 0.045 microM). Tepoxalin inhibits lipoxygenase (LOX) in RBL-1 lysates (IC50 = 0.15 microM) and intact RBL-1 cells (IC50 = 1.7 microM) and inhibits the generation of leukotriene B4 (LTB4) in calcium ionophore A-23187-stimulated HPBL (IC50 = 0.07 microM) and human whole blood (IC50 = 1.57 microM). Human platelet 12-LOX (IC50 = 3.0 microM) is inhibited, but 15-LOX is only weakly so (IC50 = 157 microM)[3]. |
| In vivo | Tepoxalin inhibits inflammation and microvascular dysfunction induced by abdominal irradiation in rats.[1]In vivo, tepoxalin, administered orally, demonstrated potent anti-inflammatory activity in the established adjuvant arthritic rat (ED50 = 3.5 mg/kg) and potent analgesic activity in the acetic acid abdominal construction assay in mice (ED50 = 0.45 mg/kg). In an ex vivo whole blood eicosanoid production assay, tepoxalin produces a dose-related inhibition of prostaglandin (PG) and LT production in dogs (PGF2 alpha - ED50 = 0.015 mg/kg; LTB4 - ED50 = 2.37 mg/kg) and adjuvant arthritic rats following oral administration. In adjuvant arthritic rats, tepoxalin is devoid of ulcerogenic activity within its anti-inflammatory therapeutic range (1-33 mg/kg p.o.) and does not exhibit ulcerogenic activity in normal rats at doses lower than 100 mg/kg (UD50 = 173 mg/kg p.o.)[3]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.18 mM), Sonication is recommended.
DMSO : 60 mg/mL (155.5 mM), Sonication is recommended.
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| Keywords | Tepoxalin | LOX | Lipoxygenase | Inhibitor | inhibit | Cyclooxygenase | COX-2 | COX-1 | COX | 5-LOX |
| Inhibitors Related | Acetaminophen | Phenidone | Deferiprone | 4-Aminosalicylic acid | Gallic Acid Monohydrate | Diclofenac Potassium | Paradol | Trometamol | 5-Methylfurfural | Phenylbutazone | Rebamipide | Magnesium sulfate |
| Related Compound Libraries | Anti-Colorectal Cancer Compound Library | Pain-Related Compound Library | Bioactive Compound Library | ReFRAME Related Library | HIF-1 Signaling Pathway Compound Library | EMA Approved Drug Library | Inhibitor Library | Lipid Metabolism Compound Library | Metabolism Compound Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
