GDC-0276 - 10mM in DMSO , CAS No.1494581-70-2

CAS: 1494581-70-2 Cat. No.: G656623 Peso molecular: 462.58

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC 50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects

In Vivo

GDC-0276 (oral adminstration; 0.5-5 mg/kg) shows enrichment of 14 C with observed specific activities of 22.6 µCi/mg. GDC-0276 is not detected in urine; however, metabolites in urine were enriched in 14 C with observed specific activities of 19.6 µCi/mg. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Six drug-naïve beagle dogs Group 1 four dogs (n=2 per sex) and Group 2 2 BDC dogs (n=2 male)Dosage: 0.5, 1, 2, 3, 4, 5 mg/kg Administration: Oral adminstration Result: Showed mean specific activities of 12.2 µCi/mg (a 24% enrichment) (n=4 animals) and 23.5 µCi/mg (a 139% enrichment) (n=2 animals) for Groups 1 and 2, respectively.

IC50& Target:Nav1.7

Specifications

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC 50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address short

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Tipo de acción

INHIBITOR

Nombres e identificadores

• Peso molecular: 462.58