Theophylline (1,3-Dimethylxanthine) sodium glycinate 是有效的磷酸二酯酶 (PDE) 抑制剂,腺苷受体拮抗剂,和组蛋白脱乙酰酶 (HDAC) 活化剂。Theophylline sodium glycinate 抑制 PDE3 活性,放松气道平滑肌。Theophylline sodium glycinate 通过增加 IL-10 和抑制 NF-κ B进入细胞核而具有抗炎活性。Theophyllin sodium glycinate 诱发细胞Apoptosis" style="display: inline; color: #c13a36">凋亡 (Apoptosis)。Theophylline sodium glycinate 可用于哮喘和慢性阻塞性肺疾病 (COPD) 的研究。
产品描述
Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline sodium glycinate inhibits PDE3 activity to relax airway smooth muscle. Theophylline sodium glycinate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline sodium glycinate induces apoptosis. Theophylline sodium glycinate can be used for asthma and chronic obstructive pulmonary disease (COPD) research [1] [2] [3] [4] [5].
体外活性
Theophylline sodium glycinate (1-1000 μM) inhibits cAMP hydrolysis by PDE in homogenates of bronchial tissue to relax human bronchus and pulmonary arteries [1]. Theophylline sodium glycinate (10 μg/mL; 24 h) induces apoptosis through a reduction in the antiapoptotic protein Bcl-2 in eosinophils [2]. Theophylline sodium glycinate (0-500 μM; 2 h) inhibits NF-κB activation, I kappa B alpha (I-κBα) degradation and decreases the level of IL-6 in a concentration-dependent manner [3]. Theophylline sodium glycinate (0-1000 μM; 30 min; A549 cells) induces histone deacetylase activity to decrease inflammatory gene expression [4]. Western Blot Analysis [3] Cell Line: A549 cells Concentration: 0, 20, 100 and 500 μM Incubation Time: 2 hours Result: Decreased the expression of NF-κB p65 and I-κBα degradation in a dose-dependent manner.
体内活性
Theophylline sodium glycinate (100 mg/kg; i.p.; daily, for 9 d) has anti-inflammatory activity in mice and increases IL-6 and IL-10 levels and inhibits TNF-α and NO in male Swiss mice [1]. Animal Model: Male Swiss mice [1] Dosage: 100 mg/kg Administration: Intraperitoneal injection; daily; for 9 days Result: Increased IL-6 and IL-10 levels and inhibited TNF-α and NO.
Cas No.
8000-10-0
分子式
C9H13N5NaO4+
分子量
278.22
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years