Triclabendazole

Catalog No.S4114

Triclabendazole is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis.

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Triclabendazole Chemical Structure

Triclabendazole Chemical Structure
Molecular Weight: 359.66

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description Triclabendazole is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis.
Targets Tubulin [1]
In vitro 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. [1] 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. [2]
In vivo Triclabendazole 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. [3] 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. [4] Triclabendazole (40 mg/kg) kills 99% of adult flukes in the rat. [5]
Features Rapidly removed by the liver and oxidized to the sulphoxide and sulphone metabolites.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Moll L, et al. Vet Parasitol, 2000, 91(1-2), 153-158.

[2] Robinson MW, et al. Parasitology, 2002, 124(Pt 3), 325-338.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-06-27)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01931085 Available Parasitic Disease University of Colorado, Denver null --

Chemical Information

Download Triclabendazole SDF
Molecular Weight (MW) 359.66
Formula

C14 H9Cl3N2OS

CAS No. 68786-66-3
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms CGA-89317
Solubility (25°C) * In vitro DMSO 72 mg/mL (200.18 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 1H-Benzimidazole, 6-chloro-5-(2,3-dichlorophenoxy)-2-(methylthio)-

Tech Support & FAQs

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