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CAS No.: 60200-06-8

氯舒隆 Catalog No. CSN10682

Synonyms: L631529;MK401;BRN-2821757

Clorsulon is used in the treatment of Fasciola hepatica infections.

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实验方案

技术信息

生物活性

描述Clorsulon is used in the treatment of Fasciola hepatica infections in calves and sheep. Clorsulon (a single dose of 15 mg/kg) is effective in removing over 90% of immature Fasciola hepatica from sheep (6 weeks after infection) and calves (8 weeks after infection). A 2.5 mg/kg dose removed over 90% of mature (16 weeks old) liver fluke from sheep^[2]. The bioavailability of orally administered clorsulon was approximately 55% in goats and 60% in sheep. In both goats and sheep, approximately 50% of the i.v. dose was recovered in urine as parent drug at 48 h after administration, whereas 41% and 30% of the dose was recovered after oral administration for goats and sheep, respectively^[3]. Clorsulon causes severe disruption to the tegument and gut of Fasciola hepatica after in vivo incubation^[1]. A daily oral 5 mg/kg dose of clorsulon for 28 days in calves given Fasciola hepatica cysts at 3, 5, and 7 days after initiation of treatment was highly effective in reducing worm burdens (98%) and preventing liver pathology. In similarly infected and treated sheep, clorsulon showed little effect as a prophylactic for delaying the onset of liver pathology. The size of flukes recovered from treated sheep was reduced^[4].
参考文献

[1] Meaney M, Fairweather I, Brennan GP, Forbes AB. Transmission electron microscope study of the ultrastructural changes induced in the tegument and gut of Fasciola hepatica following in vivo drug treatment with clorsulon. Parasitol Res. 2004;92(3):232‐241
[2] Mrozik H, Bochis RJ, Eskola P, et al. 4-amino-6-(trichloroethenyl)-1,3-benzenedisulfonamide, a new, potent fasciolicide. J Med Chem. 1977;20(9):1225‐1227
[3] Sundlof SF, Whitlock TW. Clorsulon pharmacokinetics in sheep and goats following oral and intravenous administration. J Vet Pharmacol Ther. 1992;15(3):282‐291
[4] Fetterer RH, Rew RS, Gasbarre LC, Ostlind DA. Prophylactic efficacy of clorsulon against Fasciola hepatica in calves and sheep. Vet Parasitol. 1985;18(1):21‐27

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6270 mL
- 13.1352 mL
- 26.2705 mL
- 5 mM
- 0.5254 mL
- 2.6270 mL
- 5.2541 mL
- 10 mM
- 0.2627 mL
- 1.3135 mL
- 2.6270 mL

技术信息

CAS号

60200-06-8

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C8H8Cl3N3O4S2

运输

蓝冰

分子量

380.66

别名

L631529;MK401;BRN-2821757;L-631,529;氯舒隆

溶解度

DMSO	75.0 mg/mL (197.0 mM)
Water	Insoluble
Ethanol	7.0 mg/mL (18.4 mM)

动物实验配方

1% DMSO+30% polyethylene glycol+1% Tween 80+water

30 mg/mL

suspension

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