For research use only. Not for therapeutic Use.
DSM705 hydrochloride, an orally active antimalarial compound, is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 hydrochloride exhibits nanomolar potency against Plasmodium DHODH and Plasmodium parasites (IC50=95, 52 nM for P. falciparum and P. vivax DHODH, respectively), with no inhibition of mammalian DHODHs[1].
DSM705 hydrochloride shows inhibitory activity against P. falciparum DHODH (PfDHODH, IC50=95 nM), P. vivax DHODH (PvDHODH, IC50=52 nM) and Pf3D7 cells (EC50=12 nM), with no inhibition of the human enzyme[1].
DSM705 (3-200 mg/kg; p.o. twice a day for 6 days) hydrochloride provides the maximum rate of parasite killing at the dose of 50 mg/kg and fully suppresses parasitemia by days 7-8[1].
DSM705 (2.6 and 24 mg/kg; a single p.o.) hydrochloride exhibits high oral bioavailability (74%, 70%), apparent t1/2 (3.4, 4.5 h) and Cmax (2.6, 20 μM) in Swiss outbred mice[1].
DSM705 (2.3 mg/kg; a single i.v.) hydrochloride exhibits plasma clearance (CL=2.8 mL/min/kg) and Vss (1.3 L/kg) in mice[1].
| Catalog Number | I044174 |
| CAS Number | 2989908-08-7 |
| Synonyms | 3-methyl-N-[(1R)-1-(1H-1,2,4-triazol-5-yl)ethyl]-4-[1-[6-(trifluoromethyl)pyridin-3-yl]cyclopropyl]-1H-pyrrole-2-carboxamide;hydrochloride |
| Molecular Formula | C19H20ClF3N6O |
| Purity | ≥95% |
| InChI | InChI=1S/C19H19F3N6O.ClH/c1-10-13(8-24-15(10)17(29)27-11(2)16-25-9-26-28-16)18(5-6-18)12-3-4-14(23-7-12)19(20,21)22;/h3-4,7-9,11,24H,5-6H2,1-2H3,(H,27,29)(H,25,26,28);1H/t11-;/m1./s1 |
| InChIKey | RHFZUAKKIHNLHI-RFVHGSKJSA-N |
| SMILES | CC1=C(NC=C1C2(CC2)C3=CN=C(C=C3)C(F)(F)F)C(=O)NC(C)C4=NC=NN4.Cl |
| Reference | [1]. Palmer MJ, et, al. Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series. J Med Chem. 2021 May 13;64(9):6085-6136. |
