罗氟司特 T1024

Product Introduction
Bioactivity


英文名: Roflumilast

描述: 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。

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].

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）。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 12 mg/mL (29.8 mM)
DMSO : 50 mg/mL (124 mM)


关键字: BY217 | Respiratory syncytial virus | BYK20869 | RSV | Phosphodiesterase (PDE) | BY-217 | inhibit | APTA2217 | Inhibitor | APTA-2217 | BYK-20869 | Roflumilast

相关产品: BW-A 78U | Lirimilast | Siguazodan | Milrinone | PDE7-IN-2 | MR-L2 | Ensifentrine | RS-25344 hydrochloride | Olprinone | Z-HA155

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Pediatric Drug Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Anti-Infection Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途