GDC-0276

TargetMol
Product Code: TAR-T11377
Supplier: TargetMol
CodeSizePrice
TAR-T11377-5mg5mg£370.00
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here.
Quantity:
TAR-T11377-50mg50mg£1,669.00
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here.
Quantity:
TAR-T11377-100mg100mg£2,319.00
Special offer! Add £1 to your order to get a TargetMol CCK-8 Kit. Read more here.
Quantity:
Prices exclude any Taxes / VAT

Overview

Regulatory Status: RUO
Shipping:
cool pack
Storage:
-20℃

Images

1 / 1

Further Information

Bioactivity:
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. GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile.
CAS:
1494581-70-2
Formula:
C24H31FN2O4S
Molecular Weight:
462.58
Purity:
0.98
SMILES:
Fc1cc(OCC23CC4CC(CC(C4)C2)C3)c(cc1C(=O)NS(=O)(=O)N1CCC1)C1CC1

References

1. Rothenberg ME, et al. Safety, Tolerability, and Pharmacokinetics of GDC-0276, a Novel NaV1.7 Inhibitor, in a First-in-Human, Single- and Multiple-Dose Study i 2. Steven J. McKerrall, et al. Nav1.7 inhibitors for the treatment of chronic pain. Bioorganic & Medicinal Chemistry Letters (2018) 3. Takahashi RH,et al.Unequal Absorption of Radiolabeled and Nonradiolabeled Drug from the Oral Dose Leads to Incorrect Estimates of Drug Absorption and Circulating Metabolites in a Mass Balance Study.Drug Metab Lett. 2019;13(1):37-44.