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Merck
CN

SML2524

Fexinidazole

≥98% (HPLC)

别名:

1-methyl-2-[[4-(methylthio)phenoxy]methyl]-5-nitro-1H-imidazole, HOE 239

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关于此项目

经验公式(希尔记法):
C12H13N3O3S
化学文摘社编号:
分子量:
279.31
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
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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

InChI key

MIWWSGDADVMLTG-UHFFFAOYSA-N

SMILES string

CN1C(COC2=CC=C(SC)C=C2)=NC=C1[N+]([O-])=O

assay

≥98% (HPLC)

form

powder

color

light yellow to dark brown

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

Biochem/physiol Actions

Anti Trypanosoma, Leishmania agent.
Fexinidazole is a potent anti-Trypanosoma agent. Trypanosoma species human protozoan pathogens are responsible for sleeping sickness and Chagas disease. In vivo, fexinidazole is oxidized to sulfoxide and sulfone metabolites that are effective in blocking the progression of the parasitic disease visceral leishmaniasis. The mechanism of action appears to be by reductive activation via an NADH-dependent nitroreductase expressed by the parasites.

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number

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Alan H Fairlamb et al.
Current medicinal chemistry (2018-04-28)
Interest in nitroheterocyclic drugs for the treatment of infectious diseases has undergone a resurgence in recent years. Here we review the current status of monocyclic and bicyclic nitroheterocyclic compounds as existing or potential new treatments for visceral leishmaniasis, Chagas' disease
Victor Kande Betu Ku Mesu et al.
Lancet (London, England), 391(10116), 144-154 (2017-11-09)
Few therapeutic options are available to treat the late-stage of human African trypanosomiasis, a neglected tropical disease, caused by Trypanosoma brucei gambiense (g-HAT). The firstline treatment is a combination therapy of oral nifurtimox and intravenous eflornithine that needs to be
Marcel Kaiser et al.
Antimicrobial agents and chemotherapy, 55(12), 5602-5608 (2011-09-14)
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. The compound and its two principal metabolites, sulfoxide and

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