GNF179 - ≥99% , CAS No.1261114-01-5

CAS: 1261114-01-5 Cat. No.: G647347 Peso molecular: 427.90

GRADE & PURITY ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Descripción general

GNF179 is an optimized 8,8-dimethyl imidazolopiperazine analog that exhibits antimalarial potency ( IC 50 of 4.8 nM against the multidrug resistant strain W2). GNF179 is orally active

In Vitro

GNF179 does not rapidly inhibit parasite protein biosynthesis nor is it likely to target parasite cytochrome bc1, which has been validated as a hepatic stage target for Atovaquone . GNF179 may act against sporozoites instead of hepatic stages. GNF179 (5-100 nM; 48 h) shows high inhibition of gametocyte sexual life cycle progression in the mosquito as it abolished oocyst formation at 5 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GNF179 (15 mg/kg; p.o.; single dose) shows antimalarial activity in rodent malaria model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Naïve Balb/C mice infected with P. berghei Dosage: 15 mg/kg Administration: Oral, single dose Result: Protected against an infectious P. berghei sporozoite. Animal Model: Naïve Balb/C mice Dosage: 3 or 20 mg/kg Administration: IV or PO (Pharmacokinetic Analysis) Result: Pharmacokinetics of GNF179 in naïve Balb/C mice . Dose AUC (0-∞) (hrs*µM) AUC/dose t 1/2 (hrs) MRT (hrs) CL (ml/min/kg) V ss (L/kg) C 0 or C max (µM) F (%) 3 mg/kg i.v. 8.88 3.0 8.9 9.0 22 11.8 6.1 nd 20 mg/kg p.o. 20.70 1.0 8.4 nd nd nd 1.2 58 AUC, Area Under the Curve; T 1/2 , half life; CL, clearance; V SS , steady-state volume of distribution; C 0 , initial concentration; C max maximum concentration; F, fraction of dose absorbed; hrs, hours; nd, not determined.

Form:Solid

IC50& Target:Plasmodium

Specifications

Especificaciones y pureza

≥99%

Mecanismos bioquímicos y fisiológicos

GNF179 is an optimized 8, 8-dimethyl imidazolopiperazine analog that exhibits antimalarial potency ( IC 50 of 4.8 nM against the multidrug resistant strain W2). GNF179 is orally active.

Condiciones de almacenamiento de almacenamiento

Store at -20°C

Enviado en

Ice chest + Ice pads

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

Tipo de acción

INHIBITOR

Pureza

≥99%

Nombres e identificadores

• Peso molecular: 427.90

Propiedades químicas y físicas

• Solubilidad: DMSO : 100 mg/mL (233.70 mM; Need ultrasonic)