DHODH Inhibitor, DSM1-Calbiochem

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一般描述

A cell-permeable triazolopyrimidine compound that potently inhibits malaria parasitePlasmodium falciparumdihydroorotate dehydrogenase- (PfDHODH-) catalyzed electron transfer from FMNH₂to Coenzyme Q₁₀(CoQ or ubiquinone) in a potent (IC₅₀= 47 nM), CoQ-competitive (K_i= 15 nM), and species-specific manner, without affectingPfDHODH-catalyzed electron transfer from DHO to FMN or the enzymatic activity of human DHODH (<5% inhibition at 100 ?M). Reported to inhibit the proliferation ofP. falciparumparasites (EC₅₀= 79 nM against 3D7 strain)in vitro, including the drug-resistant strain Dd2 (EC₅₀= 140 nM), while displaying no inhibitory potency against murine lymphocytic leukemia cell line L1210 even at concentrations as high as 10 ?M. DSM1 is not recommended forin vivouse due to reduced plasma exposure upon repeat dosing in mice.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
A cell-permeable triazolopyrimidine compound that potently inhibits malaria parasitePlasmodium falciparumdihydroorotate dehydrogenase- (PfDHODH-) catalyzed electron transfer from FMNH₂to Coenzyme Q₁₀(CoQ or ubiquinone) in a potent (IC₅₀= 47 nM), CoQ-competitive (K_i= 15 nM), and species-specific manner, without affectingPfDHODH-catalyzed electron transfer from DHO to FMN or the enzymatic activity of human DHODH (<5% inhibition at 100 ?M). Reported to inhibit the proliferation ofP. falciparumparasites (EC₅₀= 79 nM against 3D7 strain)in vitro, including the drug-resistant strain Dd2 (EC₅₀= 140 nM), while displaying no inhibitory potency against murine lymphocytic leukemia cell line L1210 even at concentrations as high as 10 ?M. DSM1 is not recommended forin vivouse due to reduced plasma exposure upon repeat dosing in mice.
DHODH Inhibitor, DSM1, is a highly potent, competitive, tight-binding inhibitor of Plasmodium falciparum dihydroorotate dehydrogenase (IC?? = 47 nM; K_i= 15 nM).

生化/生理作用

Cell permeable: yes
Primary Target
Pf*DHODH

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Guler, J.L., et al. 2013.PLoS Pathog.9,e1003375.

Ke, H., et al. 2011.Eukaryot. Cell.10,1053.
Ganesan, S.M., et al. 2011.Mol. Biochem. Parasitol.177,29.
Booker, M.L., et al. 2010.J. Biol. Chem.285,33054.
Gujjar, R., et al. 2009.J. Med. Chem.52,1864.
Phillips, M.A., et al. 2008.J. Med. Chem.51,3649.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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