生物活性
产品描述 |
Lodoxamide is an antiallergic drug acting as a mast-cell stabilizer. It is effective in the treatment of asthma and allergic conjunctivitis. |
靶点活性 |
|
体外活性 |
Lodoxamide inhibits compound 48/80-induced histamine release and ionophore-induced 45Ca influx with associated histamine release in purified rat peritoneal mast cells [1]. The chemotactic response of eosinophils to fMLP as well as to IL-5 is significant and dose-dependent inhibited by Lodoxamide. Lodoxamide is also able to strongly inhibit the release of eosinophil peroxidase after IgA-dependent activation and, to a lesser extent, the release of eosinophil cationic protein and eosinophil-derived neurotoxin [2]. |
体内活性 |
Lodoxamide has been demonstrated to have cromolyn-like activity when studied in the rat peritoneal mast cell assay (PCA) model and in Ascaris antigen-sensitized rhesus monkeys. When given intravenously, orally, or intrabronchially by aerosol, lodoxamide significantly inhibits the increased respiratory frequency and decreased tidal volume induced by antigen challenge in Ascaris-sensitized. anaesthetized rhesus monkeys [1]. Addition of lodoxamide tromethamine to Euro-Collins or University of Wisconsin solution results in a marked decrease in lung reperfusion injury as demonstrated by increased oxygenation decreased microvascular permeability, and increased compliance [3]. |
化学信息
分子量 |
311.63 |
分子式 |
C11H6ClN3O6 |
CAS |
53882-12-5 |
溶解度 |
DMSO: 15 mg/mL ( < 1 mg/ml refers to the product slightly soluble or insoluble ) |
储存条件 |
store at -80°C |
备注 |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
配制溶液
1 mg | 5 mg | 10 mg | |
1 mM | 3.209 ml | 16.045 ml | 32.089 ml |
5 mM | 0.642 ml | 3.209 ml | 6.418 ml |
10 mM | 0.321 ml | 1.604 ml | 3.209 ml |
50 mM | 0.064 ml | 0.321 ml | 0.642 ml |
参考文献
- 1. Watt GD, et al. Protective effect opf lodoxamide tromethamine on allergen inhalation challenge. J Allergy Clin Immunol. 1980 Oct;66(4):286-94.
- 2. Capron M,et al. Inhibitory effects of lodoxamide on eosinophil activation. Int Arch Allergy Immunol. 1998 Jun;116(2):140-6.
- 3. Barr ML, et al. Addition of a mast cell stabilizing compound to organ preservation solutions decreases lung reperfusion injury. J Thorac Cardiovasc Surg. 1998 Mar;115(3):631-6; discussion 636-7.