2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. GX-201

GX-201 is a selective NaV1.7 inhibitor, with an IC50 of <3.2 nM for hNaV1.7.

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

GX-201 Chemical Structure

GX-201 Chemical Structure

CAS No. : 1788071-27-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 396 In-stock
Solution
10 mM * 1 mL in DMSO USD 396 In-stock
Solid
5 mg USD 320 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

GX-201 is a selective NaV1.7 inhibitor, with an IC50 of <3.2 nM for hNaV1.7[1].

IC50 & Target[1]

Nav1.7

<3.2 nM (IC50)

In Vivo

GX-201 has a relatively long half-life in mice[1].
GX-201 produces analgesia at a free plasma concentration about 3 times the IC50 for high-affinity channel block[1].
GX-201 inhibits nociceptive responses induced by formalin and inflammatory pain caused by complete Freund’s adjuvant (CFA)[1].

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

Animal Model: Wild-Type Mice[1].
Dosage: 0.3, 1, 3 mg/kg.
Administration: Orally, once.
Result: Produced a dose-dependent inhibition of the nociceptive events.
Molecular Weight

563.00

Formula

C25H27ClF4N2O4S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(F)C=C(OCC2CCN(CC2)CC3=CC(C(F)(F)F)=CC=C3Cl)C(C4CC4)=C1)NS(=O)(C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (111.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7762 mL 8.8810 mL 17.7620 mL
5 mM 0.3552 mL 1.7762 mL 3.5524 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.08 mg/mL (3.69 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7762 mL 8.8810 mL 17.7620 mL 44.4050 mL
5 mM 0.3552 mL 1.7762 mL 3.5524 mL 8.8810 mL
10 mM 0.1776 mL 0.8881 mL 1.7762 mL 4.4405 mL
15 mM 0.1184 mL 0.5921 mL 1.1841 mL 2.9603 mL
20 mM 0.0888 mL 0.4440 mL 0.8881 mL 2.2202 mL
25 mM 0.0710 mL 0.3552 mL 0.7105 mL 1.7762 mL
30 mM 0.0592 mL 0.2960 mL 0.5921 mL 1.4802 mL
40 mM 0.0444 mL 0.2220 mL 0.4440 mL 1.1101 mL
50 mM 0.0355 mL 0.1776 mL 0.3552 mL 0.8881 mL
60 mM 0.0296 mL 0.1480 mL 0.2960 mL 0.7401 mL
80 mM 0.0222 mL 0.1110 mL 0.2220 mL 0.5551 mL
100 mM 0.0178 mL 0.0888 mL 0.1776 mL 0.4440 mL
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GX-201 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GX-2011788071-27-1GX201GX 201Sodium ChannelNa channelsNa+ channelspainNaV1.7CFAInhibitorinhibitorinhibit

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