GW791343 dihydrochloride

Cat. No.: HY-15469 Purity: 98.03%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

GW791343 dihydrochloride Chemical Structure

CAS No. : 1019779-04-4

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 92	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 92	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 144	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 456	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Other Forms of GW791343 dihydrochloride:

GW791343 trihydrochloride Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

1019779-04-4

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
10 mM	0.2235 mL	1.1177 mL	2.2354 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

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2 mg/mL (4.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

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

Purity: 98.03%

Select Batch:

Data Sheet (275 KB) SDS (393 KB)

COA (245 KB) LCMS (121 KB)

Handling Instructions (2659 KB)

References

[1]. Michel AD, et al. Negative and positive allosteric modulators of the P2X(7) receptor. Br J Pharmacol. 2008 Feb;153(4):737-50. [Content Brief]

[2]. Svobodova I, et al. Circadian ATP Release in Organotypic Cultures of the Rat Suprachiasmatic Nucleus Is Dependent on P2X7 and P2Y Receptors. Front Pharmacol. 2018 Mar 6;9:192. [Content Brief]

Complete Stock Solution Preparation Table

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.