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GDC-0276, a potent, selective, reversible, and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM, offers potential for pain treatment while overcoming limitations associated with current pain medications, including addiction and off-target side effects. It is well tolerated and demonstrates a favorable pharmacokinetic profile.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,530 | 6-8 weeks | |
50 mg | $1,990 | 6-8 weeks | |
100 mg | $2,800 | 6-8 weeks |
Description | GDC-0276, a potent, selective, reversible, and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM, offers potential for pain treatment while overcoming limitations associated with current pain medications, including addiction and off-target side effects. It is well tolerated and demonstrates a favorable pharmacokinetic profile. |
Targets&IC50 | Nav1.7 electrophysiology:0.4 nM |
In vivo | GDC-0276 is not detected in urine;?however, metabolites in urine were enriched in 14C with observed specific activities of 19.6 μCi/mg.e.GDC-0276 (oral adminstration; 0.5-5 mg/kg) shows enrichment of 14C with observed specific activities of 22.6 μCi/mg. |
Molecular Weight | 462.58 |
Formula | C24H31FN2O4S |
Cas No. | 1494581-70-2 |
Relative Density. | 1.39 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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