1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. GDC-0276

GDC-0276 

Cat. No.: HY-114237
Handling Instructions

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. 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.

For research use only. We do not sell to patients.

GDC-0276 Chemical Structure

GDC-0276 Chemical Structure

CAS No. : 1494581-70-2

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Description

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. 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[1].

IC50 & Target

IC50:0.4 nM (NaV1.7 Electrophysiology)[1]

In Vivo

GDC-0276 (oral adminstration; 0.5-5 mg/kg) shows enrichment of 14C with observed specific activities of 22.6 µCi/mg. GDC-0276 is not detected in urine; however, metabolites in urine were enriched in 14C with observed specific activities of 19.6 µCi/mg[3].

Animal Model: Six drug-naïve beagle dogs Group 1 four dogs (n=2 per sex) and Group 2 2 BDC dogs (n=2 male)[3]
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.
Clinical Trial
Molecular Weight

462.58

Formula

C₂₄H₃₁FN₂O₄S

CAS No.

1494581-70-2

SMILES

O=C(NS(=O)(N1CCC1)=O)C2=CC(C3CC3)=C(OCC4(C5)CC6CC5CC(C6)C4)C=C2F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

GDC-0276GDC0276GDC 0276Sodium ChannelNa channelsNa+ channelspainaddictionoff-targetwell-toleratedInhibitorinhibitorinhibit

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GDC-0276
Cat. No.:
HY-114237
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