Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DSM502, a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor, demonstrates potent nanomolar activity against Plasmodium DHODH and Plasmodium parasites, while not inhibiting mammalian DHODHs.
Description | DSM502, a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor, demonstrates potent nanomolar activity against Plasmodium DHODH and Plasmodium parasites, while not inhibiting mammalian DHODHs. |
Targets&IC50 | DHODH (P. vivax):16 nM (IC50), DHODH (P. falciparum):20 nM (IC50) |
In vitro | DSM502 exhibits inhibitory effects on Plasmodium falciparum dihydroorotate dehydrogenase (Pf DHODH, IC50 = 20 nM), Plasmodium vivax DHODH (Pv DHODH, IC50 = 14 nM), and Pf 3D7 cells (EC50 = 14 nM), without hindering human DHODH enzyme activity[1]. |
In vivo | DSM502 administered orally at doses of 10 and 50 mg/kg once daily for four days resulted in a 97% parasite clearance in a confirmatory SCID mouse study, outperforming the 85% clearance observed in the GSK study[1]. When given as a single oral dose (18.3 and 50 mg/kg), DSM502 showed high oral bioavailability (>100% for both doses), with apparent half-life (t 1/2) of 2.6 and 3.6 hours, and peak concentration (C max) values of 8.4 and 42.3 μM, respectively, in mice[1]. Additionally, a single intravenous dose of DSM502 at 2.8 mg/kg revealed an apparent half-life (t 1/2) of 2.8 hours, plasma clearance rate of 26.1 mL/min/kg, and a steady-state volume of distribution (V ss) of 1.2 L/kg in mice[1]. The study used SCID mice weighing between 23 and 36 g, inoculated with parasites. Despite the high efficacy observed at both the 10 and 50 mg/kg doses in oral administration, one mouse receiving the 10 mg/kg dose died on the fifth day[1]. |
Molecular Weight | 323.319 |
Formula | C16H16F3N3O |
CAS No. | 2426616-55-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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DSM502 2426616-55-7 DSM 502 DSM-502 inhibitor inhibit