Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Leflunomide (HWA486) 是嘧啶合成抑制剂,能够抑制二氢乳清酸脱氢酶,具有抗风湿的活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 187 | 现货 | ||
25 mg | ¥ 314 | 现货 | ||
50 mg | ¥ 527 | 现货 | ||
100 mg | ¥ 798 | 现货 | ||
500 mg | ¥ 2,192 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 581 | 现货 |
产品描述 | Leflunomide (HWA486) is an immunomodulatory agent used in the therapy of rheumatoid arthritis and psoriatic arthritis. |
体外活性 | Leflunomide能够防止和逆转啮齿动物、狗、猴等体内同种异体移植物和异种移植物排斥. |
体内活性 | Leflunomide是一种免疫调节药物,可通过抑制线粒体酶二氢乳清脱氢酶发挥作用。Leflunomide能够抑制抗CD3-和白细胞介素-2(IL-2)刺激的T细胞增殖。Leflunomide也抑制抗CD3单克隆抗体刺激的反应,即人T淋巴细胞中IL-2产生和IL-2受体的表达。Leflunomide也抑制CTLL-4细胞中IL-2刺激的酪氨酸磷酸化。Leflunomide通过干扰由于rUMP产生不足和利用涉及p53的机制而引起的细胞周期进展来阻止活化和自身免疫淋巴细胞的扩增。Leflunomide在体外酪氨酸激酶测定中,能够抑制p59fyn和p56lck活性。 |
激酶实验 | DHODase activity is measured by the DCIP colorimetric assay. This is a coupled assay in which oxidation of DHO and subsequent reduction of ubiquinone are stoichiometrically equivalent to the reduction of DCIP. Reduction of DCIP is accompanied by a loss of absorbance at 610 nm (ε=21500 M/cm). The assay is performed in a 96-well microtiter plate at ambient temperature (ca. 25°C). Stock solutions of 10 mM leflunomide and A771726 are prepared in dimethyl sulfoxide (DMSO) and these are diluted with reaction buffer (100 mM Tris and 0.1 % Triton X-100, pH 8.0) to prepare working stocks of the inhibitors at varying concentrations. For each reaction, the well contained 10 nM DHODase, 68 μM DCIP, 0.16 mg/mL gelatin, the stated concentration of ubiquinone, 10 μL of an inhibitor working stock to give the stated final concentration, and reaction buffer. After a 5-min equilibration period, the reaction is initiated by addition of DHO to the stated final concentrations. The total volume of reaction mixture for each assay is 150 μL, and the final DMSO concentration is ≤ 0.01% (v/v). The reaction progress is followed by recording the loss of absorbance at 610 nm over a 10-min period (during which the velocity remained linear). Velocities are reported as the change in absorbance at 610 nm per minute, and each reported value is the average of three replicates. In experiments where the DHO or ubiquinone concentration is varied, the other substrate is held constant at 200 μM. To determine the inhibitor potency of leflunomide and A771726, the effects of varying concentrations of the two compounds on the initial velocity of the DHODase reaction is measured over a concentration range of 0.01?1.0 μM. In these experiments the DHO and ubiquinone concentrations are held constant at 200 and 100 μM, respectively. |
别名 | SU101, RS-34821, HWA486, 来氟米特 |
分子量 | 270.21 |
分子式 | C12H9F3N2O2 |
CAS No. | 75706-12-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 27 mg/mL (100 mM)
Ethanol: 27 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 3.7008 mL | 18.5041 mL | 37.0083 mL | 92.5206 mL |
5 mM | 0.7402 mL | 3.7008 mL | 7.4017 mL | 18.5041 mL | |
10 mM | 0.3701 mL | 1.8504 mL | 3.7008 mL | 9.2521 mL | |
20 mM | 0.185 mL | 0.9252 mL | 1.8504 mL | 4.626 mL | |
50 mM | 0.074 mL | 0.3701 mL | 0.7402 mL | 1.8504 mL | |
100 mM | 0.037 mL | 0.185 mL | 0.3701 mL | 0.9252 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。
Leflunomide 75706-12-6 Immunology/Inflammation Metabolism Others Dehydrogenase AhR SU101 SU 101 Inhibitor RS34821 Dihydroorotate Dehydrogenase RS 34821 RS-34821 HWA 486 DHODH inhibit SU-101 HWA486 来氟米特 HWA-486 inhibitor