Sigma-Aldrich DSM1 DHODH Inhibitor, 25mg

Sigma-Aldrich Calbiochem DSM1 DHODH Inhibitor, 25 mg Net Content, C16H13N5, Solid Form, Off-White, >=97 %, 2 to 8 deg C, 5-Methyl-N-(2-naphthyl)1,2,4triazolo1,5-apyrimidin-7-amine, Malaria Parasite Dihydroorotate Dehydrogenase Inhibitor, P. falciparum Dihydroorotate Dehydrogenase Inhibitor, Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitor, T, DHODH Inhibitor, DSM1 - Calbiochem, 275.3 g/mol Molecular Weight, HPLC Grade. A cell-permeable triazolopyrimidine compound that potently inhibits malaria parasite Plasmodium falciparum dihydroorotate dehydrogenase- (PfDHODH-) catalyzed electron transfer from FMNH2 to Coenzyme Q10 (CoQ or ubiquinone) in a potent (IC50 = 47 nM), CoQ-competitive (Ki = 15 nM) and species-specific manner, without affecting PfDHODH-catalyzed electron transfer from DHO to FMN or the enzymatic activity of human DHODH (<5% inhibition at 100 uM). Reported to inhibit the proliferation of P. falciparum parasites (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 uM. DSM1 is not recommended for in vivo use 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 parasite Plasmodium falciparum dihydroorotate dehydrogenase- (PfDHODH-) catalyzed electron transfer from FMNH2 to Coenzyme Q10 (CoQ or ubiquinone) in a potent (IC50 = 47 nM), CoQ-competitive (Ki = 15 nM) and species-specific manner, without affecting PfDHODH-catalyzed electron transfer from DHO to FMN or the enzymatic activity of human DHODH (<5% inhibition at 100 uM). Reported to inhibit the proliferation of P. falciparum parasites (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 uM. DSM1 is not recommended for in vivo use 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 (IC50 = 47 nM; Ki = 15 nM) - SIALGSK (Additional S&H or Hazmat Fees May Apply)