GNE-131 - Moligand™, 10mM in DMSO , Inhibitor of Na v1.1;Inhibitor of Na v1.2;Inhibitor of Na v1.5;Inhibitor of Na v1.6;Inhibitor of Na v1.7, CAS No.1629063-81-5, Inhibitor of Na v1.1;Inhibitor of Na v1.2;Inhibitor of Na v1.5;Inhibitor of Na v1.6;Inhibitor of Na v1.7

CAS: 1629063-81-5 Cat. No.: G654724 Molecular Weight: 442.57 PubChem CID: 91666633

GRADE & PURITY Moligand™, 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7 , with an IC 50 of 3 nM.

In Vitro

GNE-131 (Compound 13) shows moderate clearance in human liver microsomes and excellent functional activity against human NaV1.7 with an IC 50 of 0.003±0.001 μM. GNE-131 shows excellent potency, good in vitro metabolic stability. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:Na v 1.7 3 nM (IC 50 )

Specifications

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7 , with an IC 50 of 3 nM.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of Na v1.1;Inhibitor of Na v1.2;Inhibitor of Na v1.5;Inhibitor of Na v1.6;Inhibitor of Na v1.7

Names and Identifiers

• Isomeric SMILES: C1CC1C2=CN3C(=NN=C3NS(=O)(=O)C4CC4)C=C2OCC56CC7CC(C5)CC(C7)C6
• PubChem CID: 91666633
• Molecular Weight: 442.57

Associated Targets(Human)

SCN2A Tclin Sodium channel protein type 2 subunit alpha (2 Activities)

Discover Target: SCN2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SCN5A Tclin Sodium channel protein type 5 subunit alpha (2 Activities)

Discover Target: SCN5A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SCN9A Tclin Sodium channel protein type 9 subunit alpha (5 Activities)

Discover Target: SCN9A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SCN1A Tclin Sodium channel protein type 1 subunit alpha (2 Activities)

Discover Target: SCN1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SCN8A Tclin Sodium channel protein type 8 subunit alpha (2 Activities)

Discover Target: SCN8A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)