Triclabendazole sulfoxide (Synonyms: TCBZ-SO)

Cat. No.: HY-136450 Purity: 98.78%: Data Sheet
COA

SDS
Handling Instructions
FAQs
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Triclabendazole sulfoxide (TCBZ-SO) is an orally active ABCG2 inhibitor with antiparasitic activity. Triclabendazole sulfoxide inhibits ABCG2-mediated active efflux and ATPase activity. Triclabendazole sulfoxide increases the intracellular accumulation of Mitoxantrone (HY-13502). Triclabendazole sulfoxide reduces the apical-directed transepithelial transport of Nitrofurantoin and Danofloxacin, while increasing their basolateral-directed transepithelial transport. Triclabendazole sulfoxide elevates the plasma levels of sulfasalazine in wild-type mice. Triclabendazole sulfoxide decreases ABCG2-mediated secretion of Nitrofurantoin into milk in wild-type lactating mice. Triclabendazole sulfoxide can be used in the research of insecticidal agents and cancers such as breast cancer.

For research use only. We do not sell to patients.

Triclabendazole sulfoxide Chemical Structure

CAS No. : 100648-13-3

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Other Forms of Triclabendazole sulfoxide:

Triclabendazole sulfoxide-d₃ Get quote
Triclabendazole sulfoxide-¹³C,d₃ Get quote
Triclabendazole sulfoxide (Standard) Get quote

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Biological Activity
Purity & Documentation
References
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Description

In Vitro

Triclabendazole sulfoxide (0.01-10 μM; 1 h) inhibits human ABCG2 ATPase activity at concentrations above 1 μM^[1].
Triclabendazole sulfoxide (0.01-25 μM) inhibits the activities of murine ABCG2 and human ABCG2 in MDCK-II cells, with maximum inhibitory efficacies of 40% (25 μM, murine cells) and 55% (10 μM, human cells)^[1].
Triclabendazole sulfoxide (15 μM; 4 h) moderately inhibits mouse ABCG2-mediated transepithelial transport of Nitrofurantoin (HY-A0090) and Danofloxacin (HY-W011117), and almost completely suppresses human ABCG2-mediated transport of the aforementioned substrates in MDCK-II cell monolayers^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TCBZSO (50 mg/kg; p.o.; single dose) significantly increases plasma sulfasalazine levels by more than 1.5-fold in wild-type mice via Abcg2-specific inhibition^[1].
TCBZSO (50-100 mg/kg; i.p.; single dose) inhibits Abcg2-mediated nitrofurantoin secretion into milk by more than 2-fold and 4-fold, respectively, in wild-type lactating mice, reducing milk-to-plasma ratios by 3-fold and almost 4-fold^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	FVB (male, wild-type and Abcg2^-/^-, 9 to 13 weeks old)^[1]
Dosage:	50 mg/kg
Administration:	p.o.; single dose
Result:	Increased plasma sulfasalazine concentrations in wild-type mice by more than 1.5-fold (0.63 μg/mL versus 0.40 μg/mL in vehicle controls; P < 0.05). Caused no significant change in plasma sulfasalazine concentrations in Abcg2^-/^- mice.

Animal Model:	FVB (lactating female, wild-type and Abcg2^-/^-, 9 to 13 weeks old)^[1]
Dosage:	50 mg/kg; 100 mg/kg
Administration:	i.p.; single dose
Result:	Reduced milk nitrofurantoin concentrations in wild-type mice by more than 2-fold at 50 mg/kg. Reduced the milk-to-plasma ratio in wild-type mice by 3-fold at 50 mg/kg. Reduced milk nitrofurantoin concentrations in wild-type mice by more than 4-fold at 100 mg/kg. Reduced the milk-to-plasma ratio in wild-type mice by almost 4-fold at 100 mg/kg. Caused no significant changes in nitrofurantoin plasma concentrations in wild-type mice at either dose. Caused no changes in milk nitrofurantoin concentrations or milk-to-plasma ratios in Abcg2^-/^- mice at either dose.

Molecular Weight

375.66

Formula

C₁₄H₉Cl₃N₂O₂S

CAS No.

100648-13-3

Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=NC2=CC(OC3=CC=CC(Cl)=C3Cl)=C(Cl)C=C2N1)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (266.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6620 mL	13.3099 mL	26.6198 mL
5 mM	0.5324 mL	2.6620 mL	5.3240 mL
10 mM	0.2662 mL	1.3310 mL	2.6620 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.78%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (248 KB) HNMR (269 KB) LCMS (91 KB)

Handling Instructions (2659 KB)

References

[1]. Barrera B, et al. The anthelmintic triclabendazole and its metabolites inhibit the membrane transporter ABCG2/BCRP. Antimicrob Agents Chemother. 2012;56(7):3535-3543. [Content Brief]

[2]. Boix N, et al. Triclabendazole sulfoxide causes stage-dependent embryolethality in zebrafish and mouse in vitro. PLoS One. 2015;10(3):e0121308. Published 2015 Mar 20.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6620 mL	13.3099 mL	26.6198 mL	66.5495 mL
	5 mM	0.5324 mL	2.6620 mL	5.3240 mL	13.3099 mL
	10 mM	0.2662 mL	1.3310 mL	2.6620 mL	6.6550 mL
	15 mM	0.1775 mL	0.8873 mL	1.7747 mL	4.4366 mL
	20 mM	0.1331 mL	0.6655 mL	1.3310 mL	3.3275 mL
	25 mM	0.1065 mL	0.5324 mL	1.0648 mL	2.6620 mL
	30 mM	0.0887 mL	0.4437 mL	0.8873 mL	2.2183 mL
	40 mM	0.0665 mL	0.3327 mL	0.6655 mL	1.6637 mL
	50 mM	0.0532 mL	0.2662 mL	0.5324 mL	1.3310 mL
	60 mM	0.0444 mL	0.2218 mL	0.4437 mL	1.1092 mL
	80 mM	0.0333 mL	0.1664 mL	0.3327 mL	0.8319 mL
	100 mM	0.0266 mL	0.1331 mL	0.2662 mL	0.6655 mL

Triclabendazole sulfoxide Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Triclabendazole sulfoxide100648-13-3TCBZ-SOParasiteBCRPBreast cancer resistance proteinABCG2danofloxacinsulfasalazinerodent preimplantation embryosmitoxantronemurine Abcg2zebrafish embryosnitrofurantoinwild-type miceMDCK-II cellsInhibitorinhibitorinhibit

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