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Tepoxalin

Catalog No. T7724 CAS 103475-41-8

Synonyms: RWJ-20485, RWJ20485, ORF20485, ORF-20485, RWJ 20485, 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).

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Tepoxalin, CAS 103475-41-8

Pack Size	Availability	Price/USD
1 mg	In stock	$ 51.00
5 mg	In stock	$ 122.00
10 mg	In stock	$ 178.00
25 mg	In stock	$ 413.00
50 mg	In stock	$ 618.00
100 mg	In stock	$ 879.00
1 mL * 10 mM (in DMSO)	In stock	$ 171.00

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Purity: 99.03%

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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: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)
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, ORF20485, ORF-20485, RWJ 20485, ORF 20485
Molecular Weight	385.84
Formula	C20H20ClN3O3
CAS No.	103475-41-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 60 mg/ml (155.5 mM)

References and Literature

1. Lopes C, Carregaro AB, Freitas GC, Padilha VS, Lukarsewski R, Paim FC, Lopes ST. Effect of tepoxalin on renal function and hepatic enzymes in dogs exposed to hypotension with isoflurane. Vet Anaesth Analg. 2014 Sep;41(5):459-67. doi: 10.1111/vaa.12129. PubMed PMID: 24961730. 2. Loftus JP, Cavatorta D, Bushey JJ, Levine CB, Sevier CS, Wakshlag JJ. The 5-lipoxygenase inhibitor tepoxalin induces oxidative damage and altered PTEN status prior to apoptosis in canine osteosarcoma cell lines. Vet Comp Oncol. 2016 Jun;14(2):e17-30. doi: 10.1111/vco.12094. PubMed PMID: 24813477. 3. McCarthy RJ. Tepoxalin no longer available commercially. Am J Vet Res. 2013 Jul;74(7):948. doi: 10.2460/ajvr.74.7.948. PubMed PMID: 23802664. 4. Lomas AL, Lyon SD, Sanderson MW, Grauer GF. Acute and chronic effects of tepoxalin on kidney function in dogs with chronic kidney disease and osteoarthritis. Am J Vet Res. 2013 Jun;74(6):939-44. doi: 10.2460/ajvr.74.6.939. PubMed PMID: 23718664.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Pyroptosis Compound Library Anti-Colorectal Cancer Compound Library Anti-Prostate Cancer Compound Library Neuronal Signaling Compound Library Human Metabolite Library Bioactive Compounds Library Max Anti-Aging Compound Library Anti-Pancreatic Cancer Compound Library Metabolism Compound Library

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Related compounds with same targets

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Keywords

Tepoxalin 103475-41-8 Immunology/Inflammation Metabolism Neuroscience Lipoxygenase COX inhibit RWJ-20485 LOX RWJ20485 Inhibitor ORF20485 ORF-20485 Cyclooxygenase RWJ 20485 ORF 20485 inhibitor

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