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GNE-131

Catalog No.GC31065

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

Products are for research use only. Not for human use. We do not sell to patients.

GNE-131 Chemical Structure

Cas No.: 1629063-81-5

Size Price Stock Qty
10mM (in 1mL DMSO)
$455.00
In stock
5mg
$414.00
In stock
10mg
$597.00
In stock
25mg
$1,011.00
In stock
50mg
$1,609.00
In stock
100mg
$2,712.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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

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].

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].

[1]. Focken T, et al. Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain. J Med Chem. 2018 Jun 14;61(11):4810-4831.

Chemical Properties

Cas No. 1629063-81-5 SDF
Canonical SMILES O=S(NC1=NN=C2N1C=C(C3CC3)C(OCC45C[C@@H](C6)C[C@@H](C[C@@H]6C5)C4)=C2)(C7CC7)=O
Formula C23H30N4O3S M.Wt 442.57
Solubility DMSO : 125 mg/mL (282.44 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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 0.226 mL 1.1298 mL 2.2595 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 17 reference(s) in Google Scholar.)

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