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Triclabendazole Microtubule Associated inhibitor

Name: Triclabendazole
Brand: Selleck Chemicals
SKU: S4114
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S4114

Triclabendazole (CGA-89317,tcbz) is a benzimidazole, it binds to tubulin impairing intracellular transport mechanisms and interferes with protein synthesis.

Chemical Structure

Molecular Weight: 359.66

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.04%

99.04

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Chemical Information, Storage & Stability

Molecular Weight	359.66	Formula	C₁₄H₉Cl₃N₂OS	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	68786-66-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CGA-89317,tcbz			Smiles	CSC1=NC2=CC(=C(C=C2N1)Cl)OC3=C(C(=CC=C3)Cl)Cl

Solubility

In vitro
Batch:

DMSO : 72 mg/mL ( (200.18 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 36 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.600mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 72 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.600mg/ml (10.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 72 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Features	Rapidly removed by the liver and oxidized to the sulphoxide and sulphone metabolites.
Targets/IC₅₀/Ki	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] This compound 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 (this compound sulphoxide) and 36-48 hours (this compound sulphone), neither this compound nor any other metabolites can be detected in plasma. This compound 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. This chemical 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 this chemical. ^[3] It is administered intraruminally at 10 mg/kg to sheep, this chemical 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. This compound 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] This chemical (40 mg/kg) kills 99% of adult flukes in the rat. ^[5]
References	https://pubmed.ncbi.nlm.nih.gov/10889368/ https://pubmed.ncbi.nlm.nih.gov/11922434/ https://pubmed.ncbi.nlm.nih.gov/16153316/ https://pubmed.ncbi.nlm.nih.gov/3586125/ https://pubmed.ncbi.nlm.nih.gov/3745874/

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