Tepoxalin is a dual inhibitor of COX and 5-lipoxygenase (5-LO) with potent anti-inflammatory activity and a favorable gastrointestinal profile.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 1 mg | In stock | $ 164 | |
| 2 mg | In stock | $ 278 | |
| 4 mg | In stock | $ 497 | |
| 10 mg | In stock | $ 844 | |
| 20 mg | In stock | $ 1291 |
| Description | Tepoxalin is a dual inhibitor of COX and 5-lipoxygenase (5-LO) with potent anti-inflammatory activity and a favorable gastrointestinal profile. |
| 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 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.). |
| Synonyms | RWJ-20485, ORF-20485, ORF20485, RWJ20485, RWJ 20485, ORF 20485 |
| CAS No. | 103475-41-8 |
| Chemical Formula | C20H20ClN3O3 |
| Molecular Weight | 385.85 |
| Solubility | DMSO: 60 mg/ml (155.5 mM) |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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