1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. GW791343 dihydrochloride

GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease.

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GW791343 dihydrochloride Chemical Structure

GW791343 dihydrochloride Chemical Structure

CAS No. : 1019779-04-4

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mg USD 144 In-stock
50 mg USD 456 In-stock
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Description

GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease[1][2].

IC50 & Target

P2X7 Receptor

6.9-7.2 (pIC50)

In Vitro

GW791343 dihydrochloride (0.01, 0.03, 0.1, 0.3, 1, 3, 10 µM; 40 min) shows a non-competitive antagonistic activity to the human P2X7 receptor[1].
GW791343 dihydrochloride (3, 10, 30 µM; 40 min) shows an anegative allosteric modulate activity to the human P2X7 receptor[1].
GW791343 dihydrochloride (5 µM; 24-48 h; ATP measured every 4 h) enhances ATP rhythm in SCN cells[2].

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

Cell Viability Assay[1]

Cell Line: HEK293 cells (expressing human recombinant P2X7 receptors)
Concentration: 0.01, 0.03, 0.1, 0.3, 1, 3, 10 µM
Incubation Time: 40 min (pre-incubate for 10 min and incubate with other P2X7 receptor antagonists for another 30 min)
Result: Inhibited agonist-stimulated ethidium accumulation in both sucrose and NaCl buffer.
Reduced maximal responses toATP and BzATP in sucrose buffer.

Cell Viability Assay[1]

Cell Line: HEK293 cells (expressing human recombinant P2X7 receptors)
Concentration: 3, 10, 30 µM
Incubation Time: 40 min (pre-incubate for 10 min and incubate with other P2X7 receptor antagonists for another 30 min)
Result: Showed slow reversal effects at the human P2X7 receptor (after 45 min had reversed sufficiently), and had a rapid dissociation rate.

Cell Viability Assay[2]

Cell Line: SCN cells (from 16-to 21- day-old Wistar rats, which are kept under a controlled 12-12 h light-dark cycle from birth)
Concentration: 5 µM (replace the medium with fresh drug-containing culture medium every 4 h).
Incubation Time: 24-48 h (ATP measured every 4 h)
Result: Enhanced the amplitude of ATP release rhythm and extracellular ATP accumulation to 144 of control levels.
Molecular Weight

447.35

Formula

C20H26Cl2F2N4O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC(CN2CCNCC2)=CC=C1C)CNC3=CC=C(F)C(F)=C3.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (223.54 mM; Need ultrasonic)

DMSO : 20 mg/mL (44.71 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 2.2354 mL 11.1769 mL 22.3539 mL
5 mM 0.4471 mL 2.2354 mL 4.4708 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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This equation is commonly abbreviated as: C1V1 = C2V2

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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 mg/mL (4.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
  • Protocol 2

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

    Solubility: ≥ 2 mg/mL (4.47 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 50 mg/mL (111.77 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
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 (stored under nitrogen). 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 / H2O 1 mM 2.2354 mL 11.1769 mL 22.3539 mL 55.8847 mL
5 mM 0.4471 mL 2.2354 mL 4.4708 mL 11.1769 mL
10 mM 0.2235 mL 1.1177 mL 2.2354 mL 5.5885 mL
15 mM 0.1490 mL 0.7451 mL 1.4903 mL 3.7256 mL
20 mM 0.1118 mL 0.5588 mL 1.1177 mL 2.7942 mL
25 mM 0.0894 mL 0.4471 mL 0.8942 mL 2.2354 mL
30 mM 0.0745 mL 0.3726 mL 0.7451 mL 1.8628 mL
40 mM 0.0559 mL 0.2794 mL 0.5588 mL 1.3971 mL
H2O 50 mM 0.0447 mL 0.2235 mL 0.4471 mL 1.1177 mL
60 mM 0.0373 mL 0.1863 mL 0.3726 mL 0.9314 mL
80 mM 0.0279 mL 0.1397 mL 0.2794 mL 0.6986 mL
100 mM 0.0224 mL 0.1118 mL 0.2235 mL 0.5588 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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GW791343 dihydrochloride 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.

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GW791343 dihydrochloride
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