Erdosteine（厄多司坦）是一种具有口服和抗氧化活性的巯基化合物，可用于呼吸系统疾病的相关研究。
别名：KW-9144
Erdosteine is a mucolytic which is used in treatment of excessive viscous mucus. Erdosteine belongs to a class of medicines called expectorants. Erdosteine is a homocysteine-derived expectorant which experiences metabolic conversion to produce a thiol containing compound that has free radical scavenging and mucolytic activity. Erdosteine is used for acute episodes of bronchitis where there is a buildup of sticky mucus in the chest. Specifically erdosteine is a thiol derivative developed for the treatment of chronic obstructive bronchitis, including acute infective exacerbation of chronic bronchitis. Erdosteine works by helping to break down mucus secretions. This helps to make mucus runnier and less sticky. This means that it is easier to clear the mucus from the chest. Erdosteine contains two blocked sulfhydryl groups which are released following first-pass metabolism. The three active metabolites exhibit mucolytic and free radical scavenging activity. Erdosteine regulates mucus production and viscosity and increases mucociliary transport, thereby improving expectoration. Erdosteine also reveals inhibitory activity against the effects of free radicals produced by cigarette smoke. Erdosteine significantly inhibited citric acid-induced cough reflexes in guinea-pigs but did not suppress mechanical stimuli-induced cough reflexes. On the other hand, erdosteine is associated with a low incidence of adverse events, most of which are gastrointestinal and generally mild. The LD50 of erdosteine is very high ranging from 3,500 to 5,000 mg/kg.
| 分子量 | 249.31 |
| 分子式 | C8H11NO4S2 |
| CAS号 | 84611-23-4 |
| 溶解性（25°C） | DMSO 40 mg/mL |
| 储存条件 |
粉末型式 -20°C 3年；4°C 2年 溶于溶剂 -80°C 6个月；-20°C 1个月 |
| 运输方式 | 冰袋运输，根据产品的不同，可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4.0111 mL | 20.0554 mL | 40.1107 mL |
| 5 mM | 0.8022 mL | 4.0111 mL | 8.0221 mL |
| 10 mM | 0.4011 mL | 2.0055 mL | 4.0111 mL |
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
[1] Mario Cazzola, et al. Multifaceted Beneficial Effects of Erdosteine: More than a Mucolytic Agent
[3] Mario Cazzola, et al. Impact of erdosteine on chronic bronchitis and COPD: A meta-analysis
[4] Roberto W Dal Negro. Erdosteine: antitussive and anti-inflammatory effects
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