货号:A423586
同义名:
ABC 12/3;Doxophylline
Doxofylline is a methylxanthine bronchodilator used to treat asthma, COPD and bronchospasm, whiel the anti-asthmatic effects are mediated primarily through inhibiting the activities of the phosphodiesterase (PDE) enzyme.
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产品名称 | PDE ↓ ↑ | PDE1 ↓ ↑ | PDE10A ↓ ↑ | PDE2 ↓ ↑ | PDE3 ↓ ↑ | PDE4 ↓ ↑ | PDE5 ↓ ↑ | PDE6 ↓ ↑ | 其他靶点 | 纯度 | |||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Doxofylline | ✔ | 99+% | |||||||||||||||||
Deltarasin |
+++
PDEδ , Kd: 38 nM |
99+% | |||||||||||||||||
7-(2,3-Dihydroxypropyl)theophylline | ✔ | 99%+ | |||||||||||||||||
Aminophylline |
+
PDE, IC50: 0.12 mM |
99%+ | |||||||||||||||||
Anagrelide HCl | ✔ | 99%+ | |||||||||||||||||
Irsogladine | ✔ | mAChR,AChR | 99%+ | ||||||||||||||||
PF-8380 |
+++
Autotaxin, IC50: 2.8 nM |
99%+ | |||||||||||||||||
Dipyridamole | ✔ | 99%+ | |||||||||||||||||
Balipodect |
++++
PDE10A, IC50: 0.3 nM |
99%+ | |||||||||||||||||
PF-2545920 |
++++
PDE10A, IC50: 0.37 nM |
97% | |||||||||||||||||
Luteolin |
+
PDE1, Ki: 15.0 μM |
++
PDE2, Ki: 6.4 μM |
+
PDE3, Ki: 13.9 μM |
+
PDE4, Ki: 11.1 μM |
+
PDE5, Ki: 9.5 μM |
98% | |||||||||||||
Milrinone |
++
PDE2, IC50: 5.2 μM |
++
PDE3, IC50: 2.1 μM |
ATPase | 99%+ | |||||||||||||||
Pimobendan |
++
PDE3, IC50: 0.32 μM |
99%+ | |||||||||||||||||
Cilostazol |
++
PDE3, IC50: 0.2 μM |
99%+ | |||||||||||||||||
Fenspiride HCl |
+
PDE3, pIC50: 3.44 |
+
PDE4, pIC50: 4.16 |
99%+ | ||||||||||||||||
(S)-(+)-Rolipram |
++
PDE4, IC50: 0.75 μM |
98% | |||||||||||||||||
Apremilast |
+++
PDE4, IC50: 74 nM |
98% | |||||||||||||||||
GSK256066 |
++++
PDE4B, IC50: 3.2 pM |
98+% | |||||||||||||||||
Roflumilast |
++++
PDE4A4, IC50: 4.3 nM PDE4A1, IC50: 0.7 nM |
99% | |||||||||||||||||
Rolipram |
+++
PDE4B, IC50: 130 nM |
99%+ | |||||||||||||||||
Cilomilast |
+++
LPDE4, IC50: 100 nM HPDE4, IC50: 120 nM |
98+% | |||||||||||||||||
Avanafil |
++++
PDE5, IC50: 1 nM |
99%+ | |||||||||||||||||
Vardenafil HCl Trihydrate |
++++
PDE5, IC50: 0.7 nM |
99%+ | |||||||||||||||||
Tadalafil |
++++
PDE5, IC50: 1.8 nM |
98% | |||||||||||||||||
Icariin |
++
PDE5, IC50: 0.432 μM |
98% | |||||||||||||||||
Sildenafil | ✔ |
+++
PDE6, IC50: 33 nM |
99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Doxofylline is an orally active inhibitor of phosphodiesterase IV (PDE IV) and an antagonist of the A1 adenosine receptor (A1AR). It is recognized for its anti-inflammatory effects on epithelial cells by inhibiting mitochondrial reactive oxygen species (ROS) production and improving various cellular pathways, such as the NLRP3-TXNIP inflammasome pathway. Doxofylline is particularly relevant for research into asthma, chronic obstructive pulmonary disease (COPD), and bronchospasm[1].[2].[3]. |
体内研究 | In mice, intraperitoneal injections of Doxofylline at doses of 0.3 and 1 mg/kg effectively inhibit LPS-induced pulmonary inflammation[2]. A pre-treatment dose of 0.3 mg/kg also significantly reduces cellular adhesion to vascular tissue and suppresses the expression of ICAM-1 induced by LPS in vivo[2]. |
体外研究 | In vitro, Doxofylline demonstrates significant anti-inflammatory activity in 16HBE epithelial cells. At concentrations of 5 and 10 µM over 48 hours, it effectively reduces the levels of prostaglandin E2 (PGE2), nitric oxide (NO), and mitochondrial ROS, which are induced by lipopolysaccharide (LPS)[1]. Doxofylline also decreases the expression of NADPH oxidase subunits and TXNIP in these cells, further suppressing inflammation[1]. Additionally, Doxofylline inhibits the activation of the NLRP3 inflammasome and the secretion of inflammatory cytokines IL-1β and IL-18, and mitigates the reduction of SIRT1 caused by LPS exposure[1]. In experimental models using bone marrow (BM) cells, Doxofylline markedly reduces leukocyte migration induced by fMLP (Formyl-Methionyl-Leucyl-Phenylalanine) at concentrations ranging from 0.1 to 10 µM within a short exposure time of 15 minutes[2]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02522013 | Post-dural Puncture Headache | Phase 3 | Completed | - | China, Anhui ... 展开 >> Suzhou municipal hospital Suzhou, Anhui, China China, Hebei the second hospital of Hebei medcial university Shijiazhuang, Hebei, China China, Henan Henan Province Hospital of Traditional Chinese Medicine Zhengzhou, Henan, China China, Liaoning Jinzhou central hospital Jinzhou, Liaoning, China 收起 << |
NCT01055041 | Moderate to Severe Persistent ... 展开 >>Bronchial Asthma 收起 << | Not Applicable | Completed | - | India ... 展开 >> Sir Takthasinhji General Hospital Bhavnagar, Gujarat, India Bhavnagar, Gujarat, India, 364001 收起 << |
NCT03388853 | COPD | Phase 4 | Not yet recruiting | March 2019 | Turkey ... 展开 >> Cukurova University Faculty of Medicine, Chest Diseases Department Adana, Turkey Health Sciences University, Sureyyapasa Chest Diseases and Thoracic Surgery Training and Research Hospital Istanbul, Turkey 收起 << |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
3.76mL 0.75mL 0.38mL |
18.78mL 3.76mL 1.88mL |
37.56mL 7.51mL 3.76mL |
CAS号 | 69975-86-6 |
分子式 | C11H14N4O4 |
分子量 | 266.253 |
别名 | ABC 12/3;Doxophylline;3;ABC12;DO-309;ALT-07;ABC-1213;ABC-12-3;Ansimar;2-(7'-Theophyllinemethyl)-1,3-dioxolane |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 | |
动物实验配方 |