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

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

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (DSM705 hydrochloride) usually boasts enhanced water solubility and stability.

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

DSM705 Chemical Structure

DSM705 Chemical Structure

CAS No. : 2653225-38-6

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Description

DSM705 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 exhibits nanomolar potency against 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].

MedChemExpress (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].

MedChemExpress (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

CAS No.
SMILES

C[C@H](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.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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DSM705
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HY-132171
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