Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tepoxalin (RWJ 20485) 是有效的5-脂氧合酶和环氧合酶抑制剂,表现出强大的抗炎活性和较小的胃肠道刺激性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 495 | 现货 | ||
5 mg | ¥ 1,230 | 现货 | ||
10 mg | ¥ 1,830 | 现货 | ||
25 mg | ¥ 3,130 | 现货 | ||
50 mg | ¥ 4,590 | 现货 | ||
100 mg | ¥ 6,550 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,260 | 现货 |
产品描述 | 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). |
靶点活性 | 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) |
体外活性 | 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]. |
体内活性 | 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]. |
别名 | RWJ-20485, RWJ20485, ORF20485, 替泊沙林, 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)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5917 mL | 12.9587 mL | 25.9175 mL | 64.7937 mL |
5 mM | 0.5183 mL | 2.5917 mL | 5.1835 mL | 12.9587 mL | |
10 mM | 0.2592 mL | 1.2959 mL | 2.5917 mL | 6.4794 mL | |
20 mM | 0.1296 mL | 0.6479 mL | 1.2959 mL | 3.2397 mL | |
50 mM | 0.0518 mL | 0.2592 mL | 0.5183 mL | 1.2959 mL | |
100 mM | 0.0259 mL | 0.1296 mL | 0.2592 mL | 0.6479 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Tepoxalin 103475-41-8 Immunology/Inflammation Metabolism Neuroscience Lipoxygenase COX inhibit RWJ-20485 LOX RWJ20485 Inhibitor ORF20485 替泊沙林 ORF-20485 Cyclooxygenase RWJ 20485 ORF 20485 inhibitor