Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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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1 mg | 在庫あり | ¥ 12,000 | |||
5 mg | 在庫あり | ¥ 28,000 | |||
10 mg | 在庫あり | ¥ 41,000 | |||
25 mg | 在庫あり | ¥ 95,000 | |||
50 mg | 在庫あり | ¥ 142,000 | |||
100 mg | 在庫あり | ¥ 202,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 39,500 |
説明 | 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). |
ターゲット&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]. |
別名 | RWJ-20485, RWJ20485, ORF20485, ORF-20485, RWJ 20485, ORF 20485 |
分子量 | 385.84 |
分子式 | C20H20ClN3O3 |
CAS No. | 103475-41-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/ml (155.5 mM)
You can also refer to dose conversion for different animals. 詳細
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Tepoxalin 103475-41-8 Immunology/Inflammation Metabolism Neuroscience COX Lipoxygenase inhibit RWJ-20485 LOX RWJ20485 Inhibitor ORF20485 ORF-20485 Cyclooxygenase RWJ 20485 ORF 20485 inhibitor