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GDC-0276

$450$2,400

Products Details

Product 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].

Web ID

– HY-114237

Storage Temperature

– -20°C, 3 years; 4°C, 2 years (Powder)

Shipping

– Room Temperature

Applications

– Neuroscience-Neuromodulation

Molecular Formula

– C24H31FN2O4S

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.

CAS Number

– 1494581-70-2

Molecular Weight

– 462.58

Compound Purity

– 99.95

SMILES

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

Clinical Information

– Phase 1

Research Area

– Neurological Disease

Solubility

– DMSO : 125 mg/mL (ultrasonic)

Target

– Sodium Channel

Isoform

– Nav1.7

Pathway

– Membrane Transporter/Ion Channel

Product type

– Reference compound

Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.

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