| Description | DSM265 (PfSPZ) is a dihydroorotic acid dehydrogenase inhibitor with antimalarial activity (IC50: 8.9 nM).DSM265 inhibits the growth of Pf3D7 parasites and can be used for the treatment and prophylaxis of malaria infections. |
| In vivo | 在 NOD-scid IL-2Rγnull (NSG) 小鼠（23-36克）中，DSM265 （0.5 - 75 mg/kg；口服给药；每日两次；持续4天）的结果表明，DSM265 具有强效的抗疟活性[2]。 |
| Target activity | PfDHODH:8.9 nM, P. falciparum (3D7 parasites):4.3 nM (EC50) |
| Synonyms | PfSPZ |
| molecular weight | 415.33 |
| Molecular formula | C14H12F7N5S |
| CAS | 1282041-94-4 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: < 0.1 mg/mL (insoluble.) Ethanol: 5 mg/mL (12.04 mM), Sonication is recommended. DMSO: 30 mg/mL (72.23 mM), Sonication is recommended. |
| References | 1. Kokkonda S, et al. Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparumDihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity. J Med Chem. 2016 Jun 9;59(11):5416-31. 2. Phillips MA, et al. A long-duration dihydroorotate dehydrogenase inhibitor (DSM265) for prevention and treatment of malaria. Sci Transl Med. 2015 Jul 15;7(296):296ra111. |