DSM502 - Moligand™, 10mM in DMSO , Plasmodium falciparum dihydroorotate dehydrogenase, CAS No.2426616-55-7, Plasmodium falciparum dihydroorotate dehydrogenase

CAS: 2426616-55-7 Cat. No.: D656251 Fórmula: C₁₆H₁₆F₃N₃O Peso molecular: 323.31

GRADE & PURITY Moligand™, 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

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

In Vitro

DSM502 shows inhibitory activity against P. falciparum DHODH ( Pf DHODH, IC 50 =20 nM), P. vivax DHODH ( Pv DHODH, IC 50 =14 nM) and Pf 3D7 cells (EC 50 =14 nM), with no inhibition of the human enzyme. 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 . DSM502 (18.3 and 50 mg/kg; a single p.o.) exhibits high oral bioavailability (>100%, >100%), apparent t 1/2 (2.6, 3.6 h) and C max (8.4, 42.3 μM) in mice . DSM502 (2.8 mg/kg; a single i.v.) exhibits apparent t 1/2 (2.8 h), plasma clearance (26.1 mL/min/kg), and V ss (1.2 L/kg) in mice . 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 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.

IC50& Target:Plasmodium

Specifications

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Plasmodium falciparum dihydroorotate dehydrogenase

Nombres e identificadores

• Peso molecular: 323.31

Objetivos asociados (humanos)

DHODH Tclin Dihydroorotate dehydrogenase (quinone), mitochondrial (0 Activities)

Discover Target: DHODH

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)