Fexinidazole

• CAT Number: I004241
• CAS Number: 59729-37-2
• Molecular Formula: C12H13N3O3S
• Molecular Weight: 279.30
• Purity: 98%
• Synonyms: 1-methyl-2-[[4-(methylthio)phenoxy]methyl]-5-nitro-1H-imidazole
• Target: Antiparasitic
• Target Protein: P08235
• Solubility: 10 mM in DMSO
• Appearance: Solid
• Storage: Dry, dark and at 2 - 8 °C for six months or -20°C for two years.
• IC50: EC50 =5.6 µM against the G. lamblia WB strain
• IUPAC Name: 1-methyl-2-[(4-methylsulfanylphenoxy)methyl]-5-nitroimidazole
• InChI: 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
• InChIKey: MIWWSGDADVMLTG-UHFFFAOYSA-N
• SMILES: CN1C(=CN=C1COC2=CC=C(C=C2)SC)[N+](=O)[O-]

Fexinidazole(Cat No.:I004241) is an antiprotozoal medication used for the treatment of human African trypanosomiasis, also known as sleeping sickness. It is a nitroimidazole compound that is active against both the early and late stages of the Trypanosoma brucei parasite, which causes the disease. Fexinidazole is taken orally and works by killing the parasites through the production of toxic compounds within their cells. It is considered an important addition to the treatment options for sleeping sickness, particularly as it offers a convenient oral regimen that can be administered outside of specialized healthcare facilities, improving access to treatment in remote areas.

Reference

1: Bahia MT, de Andrade IM, Martins TA, do Nascimento áF, Diniz Lde F, Caldas IS,
Talvani A, Trunz BB, Torreele E, Ribeiro I. Fexinidazole: a potential new drug
candidate for Chagas disease. PLoS Negl Trop Dis. 2012;6(11):e1870. doi:
10.1371/journal.pntd.0001870. Epub 2012 Nov 1. PubMed PMID: 23133682; PubMed
Central PMCID: PMC3486905.

2: Torreele E, Bourdin Trunz B, Tweats D, Kaiser M, Brun R, Mazué G, Bray MA,
Pécoul B. Fexinidazole–a new oral nitroimidazole drug candidate entering
clinical development for the treatment of sleeping sickness. PLoS Negl Trop Dis.
2010 Dec 21;4(12):e923. doi: 10.1371/journal.pntd.0000923. PubMed PMID: 21200426;
PubMed Central PMCID: PMC3006138.

3: Jennings FW, Atouguia JM, Murray M. Topical chemotherapy for experimental
murine African CNS-trypanosomiasis: the successful use of the arsenical,
melarsoprol, combined with the 5-nitroimidazoles, fexinidazole or MK-436. Trop
Med Int Health. 1996 Oct;1(5):590-8. PubMed PMID: 8911443.

4: Raether W, Seidenath H. The activity of fexinidazole (HOE 239) against
experimental infections with Trypanosoma cruzi, trichomonads and Entamoeba
histolytica. Ann Trop Med Parasitol. 1983 Feb;77(1):13-26. PubMed PMID: 6411009.

5: Jennings FW, Urquhart GM. The use of the 2 substituted 5-nitroimidazole,
Fexinidazole (Hoe 239) in the treatment of chronic T. brucei infections in mice.
Z Parasitenkd. 1983;69(5):577-81. PubMed PMID: 6636983.