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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).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $51 | In Stock | In Stock | |
| 5 mg | $122 | In Stock | In Stock | |
| 10 mg | $178 | In Stock | In Stock | |
| 25 mg | $413 | In Stock | In Stock | |
| 50 mg | $618 | In Stock | In Stock | |
| 100 mg | $879 | In Stock | In Stock | |
| 200 mg | $1,190 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $135 | In Stock | In Stock |
| 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). |
| Targets&IC50 | COX:2.85 microM(rat basophilic leukemia cell (RBL-1) lysate), COX:4.2 microM(intact RBL-1 cells), COX:4.6 microM(sheep seminal vesicle), LOX:0.15 microM(RBL-1 lysates), LOX:1.7 microM(intact RBL-1 cells) |
| 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]. |
| Synonyms | RWJ-20485, RWJ20485, RWJ 20485, ORF-20485, ORF20485, ORF 20485 |
| Molecular Weight | 385.84 |
| Formula | C20H20ClN3O3 |
| Cas No. | 103475-41-8 |
| Smiles | C(CC(N(C)O)=O)C1=NN(C(=C1)C2=CC=C(Cl)C=C2)C3=CC=C(OC)C=C3 |
| Relative Density. | 1.26 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 60 mg/mL (155.5 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.18 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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