Theophylline (1,3-Dimethylxanthine) 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 (1,3-Dimethylxanthine) 抑制 PDE3 活性,放松气道平滑肌。Theophylline (1,3-Dimethylxanthine) 通过增加 IL-10 和抑制 NF-κ B进入细胞核而具有抗炎活性。Theophylline (1,3-Dimethylxanthine) 诱发细胞凋亡 (apoptosis)。Theophylline (1,3-Dimethylxanthine) 可用于哮喘和慢性阻塞性肺疾病 (COPD) 的研究。
生物活性 | Theophylline (1,3-Dimethylxanthine) is a potentphosphodiesterase (PDE)inhibitor,adenosine receptorantagonist, andhistone deacetylase (HDAC)activator. Theophylline (1,3-Dimethylxanthine) inhibitsPDE3activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increaseIL-10and inhibitNF-κBinto the nucleus. Theophylline (1,3-Dimethylxanthine) inducesapoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research[1][2][3][4][5]. |
IC50& Target | IL-10 | IL-6 | PDE3 | Human Endogenous Metabolite |
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体外研究 (In Vitro) | Theophylline (1,3-Dimethylxanthine) (1-1000 μM) inhibits cAMP hydrolysis by PDE in homogenates of bronchial tissue to relax human bronchus and pulmonary arteries[1]. Theophylline (1,3-Dimethylxanthine) (10 μg/mL; 24 h; eosinophils) induces apoptosis through a reduction in the antiapoptotic protein Bcl-2[2]. Theophylline (1,3-Dimethylxanthine) (0-500 μM; 2 h; A549 cells) 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 (1,3-Dimethylxanthine) (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 concentration-dependent manner. |
Western Blot Analysis[2] Cell Line: | Eosinophils | Concentration: | 10 μg/mL | Incubation Time: | 24 hours | Result: | Decreased the expression of Bcl-2. |
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体内研究 (In Vivo) | Theophylline (1,3-Dimethylxanthine) (100 mg/kg; i.p.; daily, for 9 d; male Swiss mice) has anti-inflammatory activity in mice and increases IL-6 and IL-10 levels and inhibits TNF-α and NO[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. |
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来源 | - Plants
- Theaceae
- Camellia sinensis(L.) O. Ktze.
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
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溶解性数据 | In Vitro: DMSO : 11.11 mg/mL(61.67 mM;Need ultrasonic) H2O : 5 mg/mL(27.75 mM;Need ultrasonic) 配制储备液 1 mM | 5.5506 mL | 27.7531 mL | 55.5062 mL | 5 mM | 1.1101 mL | 5.5506 mL | 11.1012 mL | 10 mM | 0.5551 mL | 2.7753 mL | 5.5506 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: PBS Solubility: 11 mg/mL (61.06 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1.11 mg/mL (6.16 mM); Clear solution
此方案可获得 ≥ 1.11 mg/mL (6.16 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 11.1 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 1.11 mg/mL (6.16 mM); Clear solution
此方案可获得 ≥ 1.11 mg/mL (6.16 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 11.1 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 1.11 mg/mL (6.16 mM); Clear solution
此方案可获得 ≥ 1.11 mg/mL (6.16 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 11.1 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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