1. Membrane Transporter/Ion Channel
  2. Sodium Channel

GNE-131 

Cat. No.: HY-112279
Handling Instructions

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

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

GNE-131 Chemical Structure

GNE-131 Chemical Structure

CAS No. : 1629063-81-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 650 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

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

IC50 & Target

IC50: 3 nM (hNaV1.7)[1].

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[1].

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[1].

Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2595 mL 11.2976 mL 22.5953 mL
5 mM 0.4519 mL 2.2595 mL 4.5191 mL
10 mM 0.2260 mL 1.1298 mL 2.2595 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.70 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.70 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.70 mM); Clear solution

References
Molecular Weight

442.57

Formula

C₂₃H₃₀N₄O₃S

CAS No.

1629063-81-5

SMILES

O=S(NC1=NN=C2N1C=C(C3CC3)C(OCC45C[[email protected]@H](C6)C[[email protected]@H](C[[email protected]@H]6C5)C4)=C2)(C7CC7)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
GNE-131
Cat. No.:
HY-112279
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GNE-131

Cat. No.: HY-112279