GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM.

Product information

CAS Number: 1629063-81-5

Molecular Weight: 442.57

Formula: C23H30N4O3S

Chemical Name: N-(6-cyclopropyl-7-{[(3R,5S,7s)-adamantan-1-yl]methoxy}-[1,2,4]triazolo[4,3-a]pyridin-3-yl)cyclopropanesulfonamide

Smiles: O=S(=O)(NC1=NN=C2C=C(OCC34C[C@@H]5C[C@H](C3)C[C@H](C4)C5)C(=CN21)C1CC1)C1CC1

InChiKey: FPERPEQIXLOVIK-QUXYOMGYSA-N

InChi: InChI=1S/C23H30N4O3S/c28-31(29,18-3-4-18)26-22-25-24-21-8-20(19(12-27(21)22)17-1-2-17)30-13-23-9-14-5-15(10-23)7-16(6-14)11-23/h8,12,14-18H,1-7,9-11,13H2,(H,25,26)/t14-,15+,16-,23?

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 125 mg/mL (282.44 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

GNE-131 (Compound 13) shows moderate clearance in human liver microsomes and excellent functional activity against human NaV1.7 with an IC50 of 0.003±0.001 μM. GNE-131 shows excellent potency, good in vitro metabolic stability.

In Vivo:

GNE-131 shows low in vivo clearance in mouse, rat, and dog. GNE-131 also displays excellent efficacy in a transgenic mouse model of induced pain.

Products are for research use only. Not for human use.