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MCE 国际站:Theophylline
中文名:茶碱
CAS:58-55-9
品牌:MedChemExpress (MCE)
存储条件:Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
生物活性:Theophylline (1,3-Dimethylxanthine) 是一种有效的磷酸二酯酶 (PDE) 抑制剂、腺苷受体 拮抗剂和组蛋白脱乙酰酶 (HDAC) 激活剂。 Theophylline (1,3-Dimethylxanthine) 抑制 PDE3 活性以松弛气道平滑肌。 Theophylline (1,3-Dimethylxanthine) 通过增加 IL-10 和抑制 NF-κB 入核而具有抗炎活性。 Theophylline (1,3-Dimethylxanthine) 诱导细胞凋亡。茶碱(1,3-二甲基黄嘌呤)可用于哮喘和慢性阻塞性肺疾病(COPD)的研究[1][2][3][4][5]。
体外:茶碱(1,3-二甲基黄嘌呤)(1-1000 µM) 抑制支气管组织匀浆中 PDE 对 cAMP 的水解,从而松弛人支气管和肺动脉[1]。茶碱 (1, 3-二甲基黄嘌呤)(10 µg/mL;24 小时;嗜酸性粒细胞)通过减少抗凋亡蛋白 Bcl-2[2] 来诱导细胞凋亡。茶碱(1,3-二甲基黄嘌呤) (0-500 µM; 2 h; A549 细胞) 以浓度依赖性方式抑制 NF-κB 激活、I kappa B α (I-κBα) 降解和降低 IL-6 水平[3].茶碱(1,3-二甲基黄嘌呤)(0-1000 µM;30 分钟;A549 细胞)诱导组蛋白脱乙酰酶活性以降低炎症基因表达[4]。
体内:茶碱(1,3-二甲基黄嘌呤)(100 mg/kg;腹腔注射;每日一次,持续 9 天;雄性瑞士小鼠)在小鼠中具有抗炎活性并增加 IL-6 和 IL-10 水平并抑制 TNF-α 和 NO [1]。
热销产品:Masitinib | Potassium 1H-indol-3-yl sulfate | Ouabain (Octahydrate) | L-778123 (hydrochloride) | Romosozumab | CHAPS | 1,2-Distearoyl-sn-glycero-3-phosphorylcholine | Denosumab | Cobimetinib | N,N,N′,N′-Tetracyclohexyl-3-oxapentanediamide
研究领域:Metabolic Enzyme/Protease | GPCR/G Protein | Cell Cycle/DNA Damage | Epigenetics | Apoptosis | Immunology/Inflammation
作用靶点:Phosphodiesterase (PDE) | Adenosine Receptor | HDAC | Apoptosis | Interleukin Related | TNF Receptor | Endogenous Metabolite
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
参考文献:[1]. Rabe KF, et, al. Theophylline and selective PDE inhibitors as bronchodilators and smooth muscle relaxants. Eur Respir J. 1995 Apr;8(4):637-42.
[2]. Németh ZH, et, al. Amrinone and theophylline differentially regulate cytokine and nitric oxide production in endotoxemic mice. Shock. 1997 May;7(5):371-5.
[3]. Ichiyama T, et, al. Theophylline inhibits NF-kappa B activation and I kappa B alpha degradation in human pulmonary epithelial cells. Naunyn Schmiedebergs Arch Pharmacol. 2001 Dec;364(6):558-61.
[4]. Ito K, et, al, Adcock IM, Barnes PJ. A molecular mechanism of action of theophylline: Induction of histone deacetylase activity to decrease inflammatory gene expression. Proc Natl Acad Sci U S A. 2002 Jun 25;99(13):8921-6.
[5]. Barnes PJ. Theophylline. Am J Respir Crit Care Med. 2013 Oct 15;188(8):901-6.
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