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.
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- No. CAS: 2653225-38-6
- Fòrmula: C19H19F3N6O
- Peso molecular:404.39
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Chemical Information
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Actividad biológica
Descripciòn
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 (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.
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Animal Model:SCID mice were inoculated with parasites[1]
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Dosage:3, 10, 20, 50, 100, 200 mg/kg
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Administration:P.o. twice a day for 6 days
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Result:Killed parasite in a dose dependent manner and fully suppressed parasitemia by days 7-8.
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Animal Model:Swiss Outbred Mice[1]
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Dosage:2.6 and 24 mg/kg for p.o.; 2.3 mg/kg for i.v. (Pharmacokinetic Analysis)
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Administration:A single p.o. and i.v.
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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.
Chemical Information
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No. CAS 2653225-38-6
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Peso molecular 404.39
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Fòrmula C19H19F3N6O
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
DSM705 Related Classifications
HY-132171 Related Classifications
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