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
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GDC-0276
CAS number：1494581-70-2(DMSO) molecular formula：C24H31FN2O4S
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1494581-70-2(DMSO) | molecular formula | C24H31FN2O4S |
| molecular weight | 462.58 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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