GW791343 trihydrochloride

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GW791343 trihydrochloride 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 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease.

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GW791343 trihydrochloride Chemical Structure

CAS No. : 309712-55-8

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Other In-stock Forms of GW791343 trihydrochloride:

GW791343 dihydrochloride

Other Forms of GW791343 trihydrochloride:

GW791343 dihydrochloride In-stock

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

P2X7 Receptor

6.9-7.2 (pIC₅₀)

In Vitro

GW791343 trihydrochloride (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 trihydrochloride (3, 10, 30 µM; 40 min) shows an anegative allosteric modulate activity to the human P2X7 receptor^[1].
GW791343 trihydrochloride (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

483.81

Formula

C₂₀H₂₇Cl₃F₂N₄O

CAS No.

309712-55-8

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

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]