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WR99210

WR99210用途

WR99210 是一种有效的二氢叶酸还原酶 (DHFR) 抑制剂,IC50 为 <0.075 nM。WR99210 有效抑制大多数抗乙胺嘧啶的恶性疟原虫株 (Plasmodium falciparum)。

WR99210名称

[ CAS 号 ]:
47326-86-3

[ 英文名 ]:
WR99210

[英文别名 ]:

WR99210生物活性

[ 描述 ]:

WR99210 是一种有效的二氢叶酸还原酶 (DHFR) 抑制剂,IC50 为 <0.075 nM。WR99210 有效抑制大多数抗乙胺嘧啶的恶性疟原虫株 (Plasmodium falciparum)。

[ 相关类别 ]:

研究领域 >> 其他

信号通路 >> 其他 >> 其他

[ 靶点 ]

IC50: <0.075 nM (DHFR)[1]

[参考文献]

[1]. Kiara SM, et al. In vitro activity of antifolate and polymorphism in dihydrofolate reductase of Plasmodium falciparum isolates from the Kenyan coast: emergence of parasites with Ile-164-Leu mutation. Antimicrob Agents Chemother. 2009 Sep;53(9):3793-8.

[2]. Hastings MD, et al. Pyrimethamine and WR99210 exert opposing selection on dihydrofolatereductase from Plasmodium vivax. Proc Natl Acad Sci U S A. 2002 Oct 1;99(20):13137-41.

WR99210物理化学性质

[ 分子式 ]:
C₁₄H₁₈Cl₃N₅O₂

[ 分子量 ]:
394.68400

[ 精确质量 ]:
393.05300

[ PSA ]:
98.46000

[ LogP ]:
3.23810

[ 外观性状 ]:
粉末

[ 储存条件 ]:
2-8°C，干燥，密封

WR99210MSDS

详细MSDS(安全技术说明书)

WR99210安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

WR99210文献

Development of a genetic tool for functional screening of anti-malarial bioactive extracts in metagenomic libraries.

Malaria Journal 14 , 233, (2015)

The chemical treatment of Plasmodium falciparum for human infections is losing efficacy each year due to the rise of resistance. One possible strategy to find novel anti-malarial drugs is to access th...

Functional analysis of Plasmodium vivax dihydrofolate reductase-thymidylate synthase genes through stable transformation of Plasmodium falciparum.

PLoS ONE 7(7) , e40416, (2012)

Mechanisms of drug resistance in Plasmodium vivax have been difficult to study partially because of the difficulties in culturing the parasite in vitro. This hampers monitoring drug resistance and res...

Novel Saccharomyces cerevisiae screen identifies WR99210 analogues that inhibit Mycobacterium tuberculosis dihydrofolate reductase.

Antimicrob. Agents Chemother. 46(11) , 3362-9, (2002)

The ongoing selection of multidrug-resistant strains of Mycobacterium tuberculosis has markedly reduced the effectiveness of the standard treatment regimens. Thus, there is an urgent need for new drug...

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