1. Metabolic Enzyme/Protease
    Anti-infection
  2. Dihydroorotate Dehydrogenase
    Parasite
  3. DSM502

DSM502 

Cat. No.: HY-132170
Handling Instructions

DSM502 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM502 exhibits nanomolar potency againsts Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs.

For research use only. We do not sell to patients.

DSM502 Chemical Structure

DSM502 Chemical Structure

CAS No. : 2426616-55-7

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Description

DSM502 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM502 exhibits nanomolar potency againsts Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs[1].

IC50 & Target

IC50: 20 nM (P. falciparum DHODH), 16 nM (P. vivax DHODH)[1]

In Vitro

DSM502 shows inhibitory activity against P. falciparum DHODH (PfDHODH, IC50=20 nM), P. vivax DHODH (PvDHODH, IC50=14 nM) and Pf3D7 cells (EC50=14 nM), with no inhibition of the human enzyme[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

DSM502 (10 and 50 mg/kg; p.o. once daily for 4 days) results in 97% parasite clearance in confirmatory SCID study compared to 85% clearance in the GSK study[1].
DSM502 (18.3 and 50 mg/kg; a single p.o.) exhibits high oral bioavailability (>100%, >100%), apparent t1/2 (2.6, 3.6 h) and Cmax (8.4, 42.3 μM) in mice[1].
DSM502 (2.8 mg/kg; a single i.v.) exhibits apparent t1/2 (2.8 h), plasma clearance (26.1 mL/min/kg), and Vss (1.2 L/kg) in mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice (23-36 g) were inoculated with parasites[1]
Dosage: 10 and 50 mg/kg
Administration: P.o. once daily for 4 days starting on day 3 after mice had been inoculated with parasites
Result: Resulted in 97% parasite clearance compared to 85% clearance in the GSK study.
The 10 mg/kg mouse died on day 5.
Molecular Weight

323.31

Formula

C₁₆H₁₆F₃N₃O

CAS No.
SMILES

O=C(C1=C(C)C(CC2=CC=C(C(F)(F)F)N=C2)=CN1)NC3CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

DSM502DSM 502DSM-502Dihydroorotate DehydrogenaseParasiteDHODHPlasmodiumparasitesInhibitorinhibitorinhibit

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