GSK932121 | P.f Cyt bc1 inhibitor | Probechem Biochemicals

Chemical Structure : GSK932121

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GSK932121 (GSK-932121)

货号: PC-20294Not For Human Use, Lab Use Only.

GSK932121 is a potent, selective inhibitor of P. falciparum cytochrome bc1 with IC50 of 7 nM, binds to Qi site of cytochrome bc1 and shows potent antimalarial activity in vitro and in vivo.

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生物&药学活性

GSK932121 is a potent, selective inhibitor of P. falciparum cytochrome bc1 with IC50 of 7 nM, binds to Qi site of cytochrome bc1 and shows potent antimalarial activity in vitro and in vivo.
GSK932121 shows weak inhibition for cytochrome bc1 from HEK293 cells with IC50 of 400 nM (57-fold selectivity).
GSK932121 displays potent antimalarial activity against Plasmodium falciparumin vitro (P. falciparum 3D7A, IC50=6 nM, whole cell assay).
GSK932121 is potent against P. falciparum Pf3D70087/N9 as pyrimethamine in both HM-β2 mnull mice (ED90=0.6 mg/kg) and HM-IL2Rγnull mice (ED90=0.6 mg/kg).

物理化学性质&存储条件

分子量	425.79
分子式	C20H15ClF3NO4
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	3-chloro-6-(hydroxymethyl)-2-methyl-5-(4-(4-(trifluoromethoxy)phenoxy)phenyl)pyridin-4(1H)-one

参考文献

1. Bueno JM, et al. Future Med Chem. 2012 Dec;4(18):2311-23.

2. Capper MJ, et al. Proc Natl Acad Sci U S A. 2015 Jan 20;112(3):755-60.

3. María Belén Jiménez-Díaz, et al. Antimicrob Agents Chemother. 2009 Oct;53(10):4533-6.

GSK932121 (GSK-932121)

生物&药学活性

物理化学性质&存储条件

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GSK932121 (GSK-932121)

生物&药学活性

物理化学性质&存储条件

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