Referencia número: HY-13801

Fexinidazole

(Synonyms: HOE 239)

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

Fexinidazole (HOE 239) is an orally active, potent nitroimidazole antitrypanosomal agent. Fexinidazole shows trypanocidal activity against T. brucei subspecies and strains with IC₅₀s of 0.7-3.3 μM (0.2-0.9 μg/ml). Fexinidazol has the potential for human sleeping sickness (HAT) caused by infection with T. brucei.

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Pureza: 99.84%
No. CAS: 59729-37-2
Fòrmula: C₁₂H₁₃N₃O₃S
Peso molecular:279.31

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Fexinidazole Chemical Structure

No. CAS: 59729-37-2

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (4)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

Trypanosoma

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Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	CC₅₀	>200 μM Compound: Fexinidazole	Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 29885575]
HepG2	CC₅₀	>200 μM Compound: Fexinidazole	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30092366]
HepG2	CC₅₀	>200 μM Compound: Fexinidazole	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 30655943]
HepG2	CC₅₀	>200 μM Compound: Fexinidazole	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 32292551]
HepG2	CC₅₀	>200 μM Compound: Fexinidazole	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32652409]
HepG2	CC₅₀	>200 μM Compound: Fexinidazole	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32795774]
L6	IC₅₀	>90 μg/mL Compound: Fexinidazole	Cytotoxicity against in rat L6 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay Cytotoxicity against in rat L6 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay	[PMID: 21353728]
L6	IC₅₀	377 μM Compound: 7a, fexinidazole	Cytotoxicity against rat L6 cells after 72 hrs by SRB assay Cytotoxicity against rat L6 cells after 72 hrs by SRB assay	[PMID: 21211967]
THP-1	CC₅₀	>200 μM Compound: Fexinidazole	Cytotoxicity against human THP-1 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human THP-1 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32652409]
THP-1	CC₅₀	>62.5 μM Compound: Fexinidazole	Cytotoxicity against human THP1 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human THP1 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 29885575]
THP-1	CC₅₀	>62.5 μM Compound: Fexinidazole	Cytotoxicity against human THP1 cells after 72 hrs by MTT assay Cytotoxicity against human THP1 cells after 72 hrs by MTT assay	[PMID: 30655943]
THP-1	CC₅₀	3.6 μM Compound: Fexinidazole	Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human THP1 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 30092366]
THP-1	EC₅₀	2.8 μM Compound: D	Antileishmanial activity against intracellular amastigote stage of Leishmania donovani MHOM/IN/00/DEVI infected in human THP1 cells assessed as decrease infected macrophages after 120 hrs by microscopy Antileishmanial activity against intracellular amastigote stage of Leishmania donovani MHOM/IN/00/DEVI infected in human THP1 cells assessed as decrease infected macrophages after 120 hrs by microscopy	[PMID: 25846065]
Vero	EC₅₀	3 μM Compound: Fexinidazole	Antitrypanosomal activity against Trypanosoma cruzi CL Brener amastigotes infected in African green monkey Vero cells assessed as reduction in parasite growth incubated for 120 hrs at 24 hrs post-infection and measured on day 6 post-infection by hemocytom Antitrypanosomal activity against Trypanosoma cruzi CL Brener amastigotes infected in African green monkey Vero cells assessed as reduction in parasite growth incubated for 120 hrs at 24 hrs post-infection and measured on day 6 post-infection by hemocytom	[PMID: 32292551]

In Vitro

Fexinidazole (HOE 239) has two principal metabolites, sulfoxide and sulfone. They have shown trypanocidal activity in vitro with IC₅₀s of 0.7-3.3 μM (0.2-0.9 μg/ml) range against all parasite strains tested^[1].

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

In Vivo

Fexinidazole (HOE 239; 20-50 mg/kg/day of IP or 25-100 mg/kg/day of PO; four consecutive days) has antitrypanosomal activities^[1].

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

Animal Model:

Adult female NMRI mice weighing between 20 and 25 g T. b. rhodesiense^[1]
Dosage:

20, 50 mg/kg (IP) or 25, 50, 100 mg/kg (PO)
Administration:

IP or PO; daily; four consecutive days
Result:

Had antitrypanosomal activities, with 100 mg/kg/day p.o. being 100% curative.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 59729-37-2
Appearance Solid
Peso molecular 279.31
Fòrmula C₁₂H₁₃N₃O₃S
Color Light yellow to yellow
SMILES

O=[N+](C1=CN=C(COC2=CC=C(SC)C=C2)N1C)[O-]
Synonyms

HOE 239
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Molecules

Free Radical Production Induced by Nitroimidazole Compounds Lead to Cell Death in Leishmania infantum Amastigotes. [Abstract]

2024 Aug 26;29(17):4041. PMID: 39274889
bioRxiv

Fexinidazole and Corallopyronin A target Wolbachia-infected sheath cells present in filarial nematodes. [Abstract]

2025 Jan 26:2025.01.23.634442. PMID: 39896488

Solvente y solubilidad

In Vitro:

DMSO : 50 mg/mL (179.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.5803 mL

17.9013 mL

35.8025 mL

5 mM

0.7161 mL

3.5803 mL

7.1605 mL

10 mM

0.3580 mL

1.7901 mL

3.5803 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (8.95 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (8.95 mM); Clear solution; Need warming

This protocol yields a clear solution of 2.5 mg/mL. 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Kaiser M, et al. Antitrypanosomal activity of fexinidazole, a new oral nitroimidazole drug candidate for treatment of sleeping sickness. Antimicrob Agents Chemother. 2011 Dec;55(12):5602-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.5803 mL	17.9013 mL	35.8025 mL	89.5063 mL
	5 mM	0.7161 mL	3.5803 mL	7.1605 mL	17.9013 mL
	10 mM	0.3580 mL	1.7901 mL	3.5803 mL	8.9506 mL
	15 mM	0.2387 mL	1.1934 mL	2.3868 mL	5.9671 mL
	20 mM	0.1790 mL	0.8951 mL	1.7901 mL	4.4753 mL
	25 mM	0.1432 mL	0.7161 mL	1.4321 mL	3.5803 mL
	30 mM	0.1193 mL	0.5967 mL	1.1934 mL	2.9835 mL
	40 mM	0.0895 mL	0.4475 mL	0.8951 mL	2.2377 mL
	50 mM	0.0716 mL	0.3580 mL	0.7161 mL	1.7901 mL
	60 mM	0.0597 mL	0.2984 mL	0.5967 mL	1.4918 mL
	80 mM	0.0448 mL	0.2238 mL	0.4475 mL	1.1188 mL
	100 mM	0.0358 mL	0.1790 mL	0.3580 mL	0.8951 mL

Keywords

Fexinidazole

4 Cited Publications

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Fexinidazole

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Publications Citing Use of MedChemExpress (MCE) Fexinidazole

Ver todos los productos específicos de isoformas Parasite

Actividad biológica

Chemical Information

Publications (4)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Fexinidazole

Anti-Infection Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

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Drug-Induced Liver Injury (DILI) Compound Library

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Publications Citing Use of MedChemExpress (MCE) Fexinidazole

Ver todos los productos específicos de isoformas Parasite

Actividad biológica

Chemical Information

Publications (4)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Fexinidazole Related Classifications

HY-13801 Related Classifications