WR99210

Names

[ Name ]:
WR99210

[Synonym ]:
1,6-Dihydro-6,6-dimethyl-1-[3-(2,4,5-trichlorophenoxy)propoxy]-1,3,5-triazine-2,4-diamine

Biological Activity

[Description]:

WR99210 is a effective inhibitor of dihydrofolate reductase (DHFR) with an IC50 of <0.075 nM[1]. WR99210 is effective against the most pyrimethamine-resistant Plasmodium falciparum strains[2].

[Related Catalog]:

Research Areas >> Others

Signaling Pathways >> Others >> Others

[Target]

IC50: <0.075 nM (DHFR)[1]

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₄H₁₈Cl₃N₅O₂

[ Molecular Weight ]:
394.68400

[ Exact Mass ]:
393.05300

[ PSA ]:
98.46000

[ LogP ]:
3.23810

MSDS

Click to get detail MSDS

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Articles

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...