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Fexinidazole DNA/RNA Synthesis inhibitor

Cat.No.S2600

Fexinidazole (HOE-239, Fexinidazole Winthrop) is a 5-nitroimidazole derivative. This compound is a DNA synthesis inhibitor and the only, all-oral agent for Human African Trypanosomiasis(HAT or sleeping sickness).
Fexinidazole DNA/RNA Synthesis inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 279.31

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Quality Control

Batch: S260001 DMSO]56 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.89%
99.89

Solubility

In vitro
Batch:

DMSO : 56 mg/mL (200.49 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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

mg/kg
g
μL

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.

Chemical Information, Storage & Stability

Molecular Weight 279.31 Formula

C12H13N3O3S

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 59729-37-2 -- Storage of Stock Solutions

Synonyms HOE-239, Fexinidazole Winthrop SMILES CN1C(=CN=C1COC2=CC=C(C=C2)SC)[N+](=O)[O-]

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
DNA synthesis
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05645822 Withdrawn
Sleeping Sickness|Trypanosomiasis African
Institute of Tropical Medicine Belgium|Ministry of Public Health Democratic Republic of the Congo|Institut National de Recherche Biomédicale. Kinshasa République Démocratique du Congo|SANRU Asbl Soins de Santé Primaires en Milieu Rural République Démocratique du Congo|Drugs for Neglected Diseases
 2024-01-01 --
NCT05607173 COMPLETED
Hepatic Function Abnormal
Sanofi
 2023-01-18 PHASE1
NCT05607173 Completed
Hepatic Function Abnormal
Sanofi
 2023-01-18 Phase 1
NCT03974178 COMPLETED
Trypanosomiasis, African; Sleeping Sickness; Trypanosoma Brucei Rhodesiense; Infection
Drugs for Neglected Diseases
 2019-09-29 PHASE2; PHASE3
NCT03025789 COMPLETED
Trypanosomiasis, African; Sleeping Sickness; Trypanosomiasis; Gambian
Drugs for Neglected Diseases
 2016-11-10 PHASE3
NCT03587766 COMPLETED
Chagas' Disease (Chronic) Nos
Drugs for Neglected Diseases
 2017-11-13 PHASE2

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