1. Metabolic Enzyme/Protease
    Anti-infection
  2. Dihydroorotate Dehydrogenase
    Parasite
  3. DSM705

DSM705 

Cat. No.: HY-132171
Handling Instructions

DSM705 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 exhibits nanomolar potency againsts Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs. DSM705 is a potent antimalarial compound.

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

DSM705 Chemical Structure

DSM705 Chemical Structure

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Description

DSM705 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 exhibits nanomolar potency againsts Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs. DSM705 is a potent antimalarial compound[1].

IC50 & Target

IC50: 95 nM (P. falciparum DHODH), 52 nM (P. vivax DHODH)[1]

In Vitro

DSM705 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].

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

In Vivo

DSM705 (3-200 mg/kg; p.o. twice a day for 6 days) 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.) 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.) exhibits plasma clearance (CL=2.8 mL/min/kg) and Vss (1.3 L/kg) in mice[1].

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

Animal Model: SCID mice were inoculated with parasites[1]
Dosage: 3, 10, 20, 50, 100, 200 mg/kg
Administration: P.o. twice a day for 6 days
Result: Killed parasite in a dose dependent manner and fully suppressed parasitemia by days 7-8.
Animal Model: Swiss Outbred Mice[1]
Dosage: 2.6 and 24 mg/kg for p.o.; 2.3 mg/kg for i.v. (Pharmacokinetic Analysis)
Administration: A single p.o. and i.v.
Result: P.o.: F=74/70%, t1/2=3.4/4.5 h, Cmax=2.6/20 μM.
I.v.: CL=2.8 mL/min/kg, Vss=1.3 L/kg.
Molecular Weight

404.39

Formula

C₁₉H₁₉F₃N₆O

SMILES

C[[email protected]](C1=NC=NN1)NC(C2=C(C(C3(C4=CC=C(N=C4)C(F)(F)F)CC3)=CN2)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

DSM705DSM 705DSM-705Dihydroorotate DehydrogenaseParasiteDHODHPlasmodiumparasitesInhibitorinhibitorinhibit

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DSM705
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