Lodoxamide
(Synonyms: 洛度沙胺,U-42585E free acid) 目录号 : GC18282
A potent agonist of GPR35 and a mast cell stabilizer
Cas No.:53882-12-5
Sample solution is provided at 25 µL, 10mM.
Lodoxamide is an antiallergic compound acting as a mast-cell stabilizer for the treatment of asthma and allergic conjunctivitis.
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].
Lodoxamide has been demonstrated to have cromolyn-like activity when studied in the rat peritoneal mast cell assay (PCA) model3 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. anesthetized 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]. Patients treated with lodoxamide tromethamine demonstrate an improvement in daytime breathing difficulty, cough, sputum production, and sleep[4].
References:
[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.
[4]. Mann JS, et al. Inhaled lodoxamide tromethamine in the treatment of perennial asthma: a double-blind placebo-controlled study. J Allergy Clin Immunol. 1985 Jul;76(1):83-90.
Cas No. | 53882-12-5 | SDF | |
别名 | 洛度沙胺,U-42585E free acid | ||
化学名 | 2,2'-[(2-chloro-5-cyano-1,3-phenylene)diimino]bis[2-oxo-acetic acid] | ||
Canonical SMILES | ClC1=C(NC(C(O)=O)=O)C=C(C#N)C=C1NC(C(O)=O)=O | ||
分子式 | C11H6ClN3O6 | 分子量 | 311.6 |
溶解度 | DMSO : 20 mg/mL (36.11 mM) | 储存条件 | Store at -20°C |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
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1 mg | 5 mg | 10 mg |
1 mM | 3.2092 mL | 16.0462 mL | 32.0924 mL |
5 mM | 0.6418 mL | 3.2092 mL | 6.4185 mL |
10 mM | 0.3209 mL | 1.6046 mL | 3.2092 mL |
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给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >99.50%
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