Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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Other Sizes |
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Fexinidazole (Hoe239; Hoe-239) is a novel, potent and nitroimidazole-based antiparasitic agent that has been approved in 2021 by FDA as the first all-oral medication to treat African trypanosomiasis caused by Trypanosoma brucei gambiense. It acts well against diseases in both their initial and advanced stages. Its use in Chagas disease is also supported by some evidence.
Targets |
Trypanosoma
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ln Vitro |
Fexinidazole (HOE 239) has sulfoxide and sulfone as its two main metabolites. With IC50s ranging from 0.7-3.3 μM (0.2-0.9 μg/ml), they have demonstrated trypanocidal activity in vitro against every tested parasite strain[1].
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ln Vivo |
Fexinidazole (HOE 239; four consecutive days; 20–50 mg/kg/day of IP or 25–100 mg/kg/day of PO) exhibits antitrypanosomal properties[1].
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Animal Protocol |
Adult female NMRI mice weighing between 20 and 25 g T. b. rhodesiense
20, 50 mg/kg (IP) or 25, 50, 100 mg/kg (PO) IP or PO; daily; four consecutive days |
References |
Molecular Formula |
C12H13N3O3S
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Molecular Weight |
279.314
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Exact Mass |
279.07
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Elemental Analysis |
C, 51.60; H, 4.69; N, 15.04; O, 17.18; S, 11.48
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CAS # |
59729-37-2
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Appearance |
Solid powder
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SMILES |
CN1C(=CN=C1COC2=CC=C(C=C2)SC)[N+](=O)[O-]
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InChi Key |
MIWWSGDADVMLTG-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C12H13N3O3S/c1-14-11(13-7-12(14)15(16)17)8-18-9-3-5-10(19-2)6-4-9/h3-7H,8H2,1-2H3
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Chemical Name |
1-methyl-2-[(4-methylsulfanylphenoxy)methyl]-5-nitroimidazole
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Synonyms |
Hoe239; Hoe 239; Fexinidazole; Hoe-239
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: 50~56 mg/mL (179.0~200.5 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.95 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (8.95 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05607173 | Completed | Drug: Fexinidazole (HOE239) |
Hepatic Function Abnormal | Sanofi | January 18, 2023 | Phase 1 |
NCT02571062 | Completed | Drug: Fexinidazole | Trypanosomiasis, African | Drugs for Neglected Diseases | March 2015 | Phase 1 |
NCT03025789 | Completed | Drug: Fexinidazole | Trypanosomiasis, African Sleeping Sickness |
Drugs for Neglected Diseases | November 10, 2016 | Phase 3 |
NCT02169557 | Completed | Drug: Fexinidazole | Human African Trypanosomiasis (HAT) |
Drugs for Neglected Diseases | April 30, 2014 | Phase 2 Phase 3 |
NCT01340157 | Completed | Drug: Fexinidazole | PK in Healthy Volunteers | Drugs for Neglected Diseases | February 2011 | Phase 1 |