Fexinidazole

Modify Date: 2024-01-08 09:50:09

Fexinidazole Structure
Fexinidazole structure
Common Name Fexinidazole
CAS Number 59729-37-2 Molecular Weight 279.315
Density 1.3±0.1 g/cm3 Boiling Point 511.3±40.0 °C at 760 mmHg
Molecular Formula C12H13N3O3S Melting Point N/A
MSDS N/A Flash Point 263.0±27.3 °C

 Use of Fexinidazole


Fexinidazole is a 5-nitroimidazole drug currently in clinical development for the treatment of human sleeping sickness (human African trypanosomiasis [HAT]), caused by infection with species of the protozoan parasite Trypanosoma brucei. Target: Antiparasiticin vivo: Fexinidazole shows dose-related efficacy in the T. b. rhodesiense (STIB900) acute mouse model at intraperitoneal (i.p.) doses of 20 to 50 mg/kg/day and oral (per os [p.o.]) doses of 25 to 100 mg/kg/day given on four consecutive days, with 100 mg/kg/day p.o. being 100% curative. Fexinidazole is shown to be effective in the GVR35 mouse model, which mimics the advanced and fatal stage of the disease, when parasites have disseminated into the brain. [1]

 Names

Name 1-methyl-2-[(4-methylsulfanylphenoxy)methyl]-5-nitroimidazole
Synonym More Synonyms

 Fexinidazole Biological Activity

Description Fexinidazole is a 5-nitroimidazole drug currently in clinical development for the treatment of human sleeping sickness (human African trypanosomiasis [HAT]), caused by infection with species of the protozoan parasite Trypanosoma brucei. Target: Antiparasiticin vivo: Fexinidazole shows dose-related efficacy in the T. b. rhodesiense (STIB900) acute mouse model at intraperitoneal (i.p.) doses of 20 to 50 mg/kg/day and oral (per os [p.o.]) doses of 25 to 100 mg/kg/day given on four consecutive days, with 100 mg/kg/day p.o. being 100% curative. Fexinidazole is shown to be effective in the GVR35 mouse model, which mimics the advanced and fatal stage of the disease, when parasites have disseminated into the brain. [1]
Related Catalog
References

[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.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 511.3±40.0 °C at 760 mmHg
Molecular Formula C12H13N3O3S
Molecular Weight 279.315
Flash Point 263.0±27.3 °C
Exact Mass 279.067749
PSA 98.17000
LogP 2.28
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.629
Storage condition 2-8℃

 Safety Information

HS Code 2933290090

 Customs

HS Code 2933290090
Summary 2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

1-Methyl-2-{[4-(methylsulfanyl)phenoxy]methyl}-5-nitro-1H-imidazole
1-methyl-2-(4-methylthiophenyl-oxymethyl)-5-nitro-imidazole
1-Methyl-2-((4-(methylthio)phenoxy)methyl)-5-nitro-1H-imidazole
1-methyl-2-(4-methylsulfanyl-phenoxymethyl)-5-nitro-1H-imidazole
Fexinidazol
Fexinidazole
Fexinidazolum
1H-Imidazole, 1-methyl-2-[[4-(methylthio)phenoxy]methyl]-5-nitro-
1-Methyl-2-((p-(methylthio)phenoxy)methyl)-5-nitroimidazole
HOE-239
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