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Tepoxalin

🥰Excellent
Catalog No. T7724Cas No. 103475-41-8
Alias RWJ-20485, RWJ20485, RWJ 20485, ORF-20485, ORF20485, ORF 20485

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).

Tepoxalin

Tepoxalin

🥰Excellent
Purity: 99.03%
Catalog No. T7724Alias RWJ-20485, RWJ20485, RWJ 20485, ORF-20485, ORF20485, ORF 20485Cas No. 103475-41-8
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 SizePriceAvailabilityQuantity
1 mg48 €In Stock
5 mg115 €In Stock
10 mg169 €In Stock
25 mg392 €In Stock
50 mg587 €In Stock
100 mg835 €In Stock
1 mL x 10 mM (in DMSO)162 €In Stock
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Purity:99.03%
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Product Introduction

Bioactivity
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
LOX:1.7 microM(intact RBL-1 cells), LOX:0.15 microM(RBL-1 lysates), 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)
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].
AliasRWJ-20485, RWJ20485, RWJ 20485, ORF-20485, ORF20485, ORF 20485
Chemical Properties
Molecular Weight385.84
FormulaC20H20ClN3O3
Cas No.103475-41-8
SmilesC(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 & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 60 mg/ml (155.5 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5917 mL12.9587 mL25.9175 mL129.5874 mL
5 mM0.5183 mL2.5917 mL5.1835 mL25.9175 mL
10 mM0.2592 mL1.2959 mL2.5917 mL12.9587 mL
20 mM0.1296 mL0.6479 mL1.2959 mL6.4794 mL
50 mM0.0518 mL0.2592 mL0.5183 mL2.5917 mL
100 mM0.0259 mL0.1296 mL0.2592 mL1.2959 mL

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