| CAS |
No.60200-06-8 |
| 中文名称 |
克洛索隆 |
| 英文名称 |
Clorsulon |
| 别名 |
MK-401;L631529;氯舒隆 |
| 分子式 |
C8H8Cl3N3O4S2 |
| 分子量 |
380.66 |
| 溶解性 |
Soluble in DMSO ≥5mg/mL |
| 纯度 |
≥98% |
| 外观(性状) |
White to off-white Solid |
| 储存条件 |
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 262-100-2 |
| MDL |
MFCD00072006 |
| SMILES |
C1=C(C(=CC(=C1N)S(=O)(=O)N)S(=O)(=O)N)C(=C(Cl)Cl)Cl |
| InChIKey |
QOVTVIYTBRHADL-UHFFFAOYSA-N |
| InChI |
InChI=1S/C8H8Cl3N3O4S2/c9-7(8(10)11)3-1-4(12)6(20(14，17)18)2-5(3)19(13，15)16/h1-2H，12H2，(H2，13，15，16)(H2，14，17，18) |
| PubChem CID |
43231 |
| 靶点 |
Parasite |
| 通路 |
Anti-infection |
| 背景说明 |
是一种具有抗寄生虫活性的化合物。 |
| 生物活性 |
Clorsulon 是一种口服有效的杀虫剂，是3-磷酸甘油酸和ATP的竞争性抑制剂，Ki值为0.29 mM。[1-2] |
| In Vivo |
A single dose of 15 mg/kg was 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. Single oral doses up to 400 mg/kg were tolerated by sheep without gross toxic symptoms.[1] When cultured in vivo，Clorsulon severely damages the cortex and internal organs of the liver fluke.[3] |
| 动物实验 |
Male Sprague-Dawley rats infected with F. hepatica were dosed orally at 8-8.5 weeks post-infection with clorsulon at a concentration of 12.5 mg/kg body weight. After 24，48 and 72 h，rats were sacrificed by cervical dislocation and mature flukes recovered from the bile ducts.[3] |
| 数据来源文献 |
[1]. Mrozik H，et al. 4-amino-6-(trichloroethenyl)-1，3-benzenedisulfonamide，a new，potent fasciolicide. J Med Chem. 1977 Sep;20(9): 1225-7.
[2]. Schulman MD，et al. Mechanism of action of MK-401 against Fasciola hepatica: inhibition of phosphoglycerate kinase. Mol Biochem Parasitol. 1982 Mar;5(3): 133-45.
[3]. Meaney M，et al. 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 Feb;92(3): 232-41. |
| 规格 |
25mg 50mg 100mg 500mg |
| 单位 |
瓶 |
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