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GDC-0310

Cat. No. M21126
GDC-0310 Structure
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Quality Control & Documentation
Biological Activity

GDC-0310 is a selective Nav1.7 acyl sulfonamide inhibitor with an IC50 value of 0.6 nM for hNav1.7. It is an oral primary clinical candidate for the study of pain.

Chemical Information
Molecular Weight 543.48
Formula C25H29Cl2FN2O4S
CAS Number 1788063-52-4
Solubility (25°C) DMSO : 4 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Brian S Safina, et al. J Med Chem. Discovery of Acyl-sulfonamide Nav1.7 Inhibitors GDC-0276 and GDC-0310

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  Catalog
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