Halofuginol (MAZ1805)

Chemical Structure : Halofuginol

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货号: PC-49608Not For Human Use, Lab Use Only.

Halofuginol (MAZ1805) is a halofuginone analog targeting the Plasmodium falciparum prolyl-tRNA synthetase (PfcPRS, Ki=71.1 nM), is highly active against both liver and asexual blood stages of the malaria parasite (EC50=5.8 nM, P. falciparum 3D7 parasite strain).

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生物&药学活性

Halofuginol (MAZ1805) is a halofuginone analog targeting the Plasmodium falciparum prolyl-tRNA synthetase (PfcPRS, Ki=71.1 nM), is highly active against both liver and asexual blood stages of the malaria parasite (EC50=5.8 nM, P. falciparum 3D7 parasite strain).
Halofuginol is approximately 65 times more selective for P. falciparum than primary mouse embryonic fibroblasts.
Halofuginol has similar activity (EC50=14 nM) to halofuginone (EC50 = 17 nM) in the in vitro P. berghei ANKA liver stage model.
Halofuginol (5 mg/kg, i.p. or 10 mg/kg p.o) is active against the asexual erythrocytic and liver stages of the malaria parasite in P. berghei sporozoite challenge model, reduces parasite burden by more than 95%.

物理化学性质&存储条件

分子量	416.7
分子式	C16H19BrClN3O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	7-bromo-6-chloro-3-((S)-2-hydroxy-3-((2R,3S)-3-hydroxypiperidin-2-yl)propyl)quinazolin-4(3H)-one

参考文献

1. Jonathan D Herman, et al. Sci Transl Med. 2015 May 20;7(288):288ra77.