GW791343 trihydrochloride
Based on 1 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- CAS No.: 309712-55-8
- Formula: C20H27Cl3F2N4O
- Molecular Weight:483.81
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) GW791343 trihydrochloride
MoreAll P2X Receptor Isoforms
More
Biological Activity
|
P2X7 Receptor 6.9-7.2 (pIC50) |
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 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 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 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.
Chemical Information
-
CAS No. 309712-55-8
-
Molecular Weight 483.81
-
Formula C20H27Cl3F2N4O
-
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.
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Neurol Res
Dl-3-n-Butylphthalide alleviates cerebral ischemia-reperfusion injury via the miR-20a-5p/XIAP axis. [Abstract]2026 May;48(5):658-673. PMID: 40888394
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GW791343 trihydrochloride Related Classifications
HY-15470 Related Classifications
Powered by Bioz