Tepoxalin

SKU: orb1299561

Description

Tepoxalin

Research Area

Immunology & Inflammation, Metabolism Research, Neuroscience

Key Properties

• CAS Number: 103475-41-8
• MW: 385.84
• Purity: 99.94% (May vary between batches)
• Formula: C₂₀H₂₀ClN₃O₃
• SMILES: C(CC(N(C)O)=O)C1=NN(C(=C1)C2=CC=C(Cl)C=C2)C3=CC=C(OC)C=C3
• Target: Lipoxygenase,COX
• Solubility: DMSO:60 mg/mL (155.5 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.18 mM)

Bioactivity

• Target IC50:
  LOX:0.15 microM(RBL-1 lysates)|LOX:1.7 microM(intact RBL-1 cells)|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)
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• In Vivo:
  Tepoxalin inhibits inflammation and microvascular dysfunction induced by abdominal irradiation in rats.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.).
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• 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).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tepoxalin, RWJ20485, RWJ-20485, RWJ 20485, Inhibitor, ORF 20485, ORF20485, ORF-20485, inhibit, LOX, Lipoxygenase, Cyclooxygenase, COX, COX-1, COX-2, 5-LOX

Compound Identifiers

PubChem CID

59757