生物活性
Clorsulon is a competitive 8-phosphoglycerate kinase and phospho-glyceromutase inhibitor. Clorsulon is used as a potent internal and external parasites inhibitor. Clorsulon is an antihelminthic compound. Clorsulon is agent belonging to the benzenesulphonamide family which is recommended for the treatment and control of adult liver flukes in cattle as suspension for oral use or injectable formulations for subcutaneous administrations. Clorsulon inhibits the enzymes involved in the glycolytic pathway, the primary source of energy in flukes. Clorsulon also depresses ATP levels in the fluke. The acute toxicity of clorsulon is tested after oral and intraperitoneal administration in mice and rats. The oral LD50 value is higher than 10g/kg body weight in both species while those obtained after intraperitoneal administrations ranged between 678 to 938 mg/kg body weight.
化学数据
分子量 | 380.66 |
分子式 | C8H8Cl3N3O4S2 |
CAS号 | 60200-06-8 |
纯度 | >98% |
溶解性(25°C) | DMSO 70 mg/mL |
储存和运输条件 | 固体粉末: -20°C 冷藏长期储存 常温运输及临时存放 |
实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
动物实验 |
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动物模型 | Rat |
配制 | 1:2 mixture of polyethylene glycol 400:dimethyl sulphoxide |
剂量 | 12.5 mg/kg |
给药处理 | Orally |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 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。
储备液配制
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
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1 mM | 2.627 mL | 13.1351 mL | 26.2702 mL |
5 mM | 0.5254 mL | 2.627 mL | 5.254 mL |
10 mM | 0.2627 mL | 1.3135 mL | 2.627 mL |