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Triclabendazole(CGA89317)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Triclabendazole(CGA89317)图片
CAS NO:68786-66-3
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)359.66
FormulaC14 H9Cl3N2OS
CAS No.68786-66-3
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 72 mg/mL (200.2 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Other info

Chemical Name: 6-Chloro-5-(2,3-dichlorophenoxy)-2-methylsulfanyl-1H-benzimidazole

InChi Key: NQPDXQQQCQDHHW-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H9Cl3N2OS/c1-21-14-18-9-5-8(16)12(6-10(9)19-14)20-11-4-2-3-7(15)13(11)17/h2-6H,1H3,(H,18,19)

SMILES Code: CSC1=NC2=CC(OC3=CC=CC(Cl)=C3Cl)=C(Cl)C=C2N1

SynonymsCGA 89317; EGA230B; NVP-EGA230; CGA-89317; EGA-230B; NVP-EGA 230; CGA89317; EGA 230B; Fasinex; NVP-EGA-230; Egaten.
实验参考方法
In Vitro

In vitro activity: Triclabendazole treatment produces percentage decreases of the fluke egg output by 15.3%, 4.3% and 36.6%, respectively, in sheep, dairy cows and heifers, these results indicate the presence of TCBZ-resistant Fasciola hepatica in sheep and cattle on this farm. Triclabendazole sulphoxide (50 mg/mL) results in extensive damage to the tegument of triclabendazole-susceptible F. hepatica, whereas triclabendazole-resistant flukes shows only localized and relatively minor disruption of the tegument covering the spines.

In VivoTriclabendazole is metabolized into a number of compounds, depending on the route of administration, plasma levels peak at 18-24 hours (Triclabendazole sulphoxide) and 36-48 hours (Triclabendazole sulphone), neither Triclabendazole nor any other metabolites can be detected in plasma. Triclabendazole sulphoxide blocks the transport of secretory bodies from the cell body to the tegumental surface, the block occurs at the site of their formation by the Golgi complex in the cell body, in their movement through the cytoplasmic connections to the syncytium, and in their movement from the base to the apex of the syncytium. Triclabendazole binds to the colchicine binding site on the β-tubulin molecule and this has been used at the basis for evaluating the relative acitvity of Triclabendazole. Triclabendazole is administered intraruminally at 10 mg/kg to sheep, Triclabendazole (TCBZ) metabolites present in plasma are only TCBZ sulphoxide (TCBZ-SO) and TCBZ sulphone, their maximum concentrations (greater than 13 mg/mL) at 18 hours and 36 hours, respectively. Triclabendazole metabolites are specifically bound to plasma albumin, which is believed to exert a major influence on the duration of plasma TCBZ metabolite concentrations and consequent exposure of liver fluke. Triclabendazole (40 mg/kg) kills 99% of adult flukes in the rat.
Animal modelSheep
Formulation & Dosage10 mg/kg; i.m.
References

Vet Parasitol. 2000 Jul 24;91(1-2):153-8; J Helminthol. 2005 Sep;79(3):227-34.