Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Roflumilast (APTA 2217) 是一种口服的长效 4 型磷酸二酯酶抑制剂 (PDE4),具有抗炎和潜在的抗肿瘤活性,作用于PDE4A1,PDEA4,PDEB1和PDEB2,IC50分别为 0.7,0.9,0.7 和 0.2 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 398 | 现货 | ||
10 mg | ¥ 519 | 现货 | ||
50 mg | ¥ 2,422 | 现货 | ||
100 mg | ¥ 3,389 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 398 | 现货 |
产品描述 | Roflumilast (APTA 2217) is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3', 5'-adenosine monophosphate (cAMP) and cAMP-mediated signaling. |
靶点活性 | PDE4B1:0.7 nM, PDE4A4:0.9 nM, PDE4C1:3 nM, PDE4A1:0.7 nM, PDE4B2:0.2 nM |
体外活性 | 在体内实验中,Roflumilast使氧化压力下降.在动物模型中,Roflumilast可一定程度抵抗肺炎(COPD相关).在暴露于烟草7个月的小鼠肺中, Roflumilast(5 mg/kg/day )诱导巨噬细胞,中性粒细胞,B细胞,树突状细胞,CD8+ T细胞,CD4+ T 细胞分别减少82%,78%,100%, 48%,88%和98%.博来霉素气管内给药14天后,Roflumilast(5 mg/kg/day )可适度降低小鼠BAL体液中过氧化氢脂质的增高.在博来霉素处理以后,Roflumilast剂量依赖性降低肺部总羟脯氨酸含量,5 mg/kg/day可抑制47%,并降低肺部纤维化损伤和αI(I)胶原蛋白转录. |
体内活性 | 在体外实验中,Roflumilast起免疫调节和抗炎活性作用。Rolfumilast对抗CD28和CD3抗体激活的CD4+ T细胞具有抑制作用(IC30:7 nM),且分别对IL-2(IC20:1 nM),IL-4(IC30:7 nM),IL-5(IC25:13 nM),以及 IFN-v(IC35:8 nM)的合成有抑制作用。在人类嗜中性粒细胞中,Roflumilast抑制LTB4合成(IC50:2 nM)。在酸性粒细胞和中性粒细胞中,Roflumilast对fMLP刺激的ROS形成有抑制作用,IC35 分别是7 nM和4 nM。在单核细胞中,Roflumilast对脂多糖诱导的TNF-α合成有抑制作用(IC40:21 nM)。在源于单核细胞的树突状细胞中,Roflumilast对脂多糖诱导的TNF-α合成有抑制效果(IC20: 5 nM)。 |
激酶实验 | PDE activity is determined with some modifications. The assay mixture contain 50 mM Tris (pH 7.4), 5 mM MgCl2, 0.5 μM cAMP or cGMP, and [3H]cAMP or [3H]cGMP (about 30,000 cpm/assay), the indicated concentration of the inhibitor and an aliquot of the enzyme solution at a final assay volume of 200 μL. Stock solutions of the compounds are diluted 1:100 (v/v) in the Tris buffer mentioned above; appropriate dilutions are prepared in 1% (v/v) DMSO/Tris buffer, which are diluted 1:2 (v/v) in the assays to obtain the desired final concentrations of the inhibitors at a DMSO concentration of 0.5% (v/v). DMSO itself affected none of the PDE activities. After preincubation for 5 min at 37°C, the reaction is started by the addition of substrate (cAMP or cGMP) and the assays are incubated for further 15 min at 37°C. Then 50 μL of 0.2 N HCl is added to stop the reaction and the assays are left on ice for about 10 min. Following incubation with 25 μg of 5′-nucleotidase (Crotalus atrox snake venom) for 10 min at 37°C, the assays are loaded on QAE Sephadex A-25 (1 mL of bed volume in Poly-Prep chromatography columns). The columns are eluted with 2 mL of 30 mM ammonium formate (pH 6.0) and the eluate is counted for radioactivity. Results are corrected for blank values (measured in the presence of denatured protein) that are below 5% of total radioactivity. The amount of cyclic nucleotides hydrolyzed did not exceed 30% of the original substrate concentration[3]. |
别名 | 罗氟司特, B9302-107, BYK 20869, APTA 2217, BY 217 |
分子量 | 403.21 |
分子式 | C17H14Cl2F2N2O3 |
CAS No. | 162401-32-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 12 mg/mL (29.8 mM)
DMSO: 75 mg/mL (186 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.4801 mL | 12.4005 mL | 24.801 mL | 62.0024 mL |
5 mM | 0.496 mL | 2.4801 mL | 4.9602 mL | 12.4005 mL | |
10 mM | 0.248 mL | 1.24 mL | 2.4801 mL | 6.2002 mL | |
20 mM | 0.124 mL | 0.62 mL | 1.24 mL | 3.1001 mL | |
DMSO | 50 mM | 0.0496 mL | 0.248 mL | 0.496 mL | 1.24 mL |
100 mM | 0.0248 mL | 0.124 mL | 0.248 mL | 0.62 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。
Roflumilast 162401-32-3 Metabolism Microbiology/Virology PDE RSV BY217 Respiratory syncytial virus BYK20869 罗氟司特 B9302-107 BYK 20869 Phosphodiesterase (PDE) APTA 2217 BY-217 BY 217 inhibit APTA2217 Inhibitor APTA-2217 BYK-20869 inhibitor