GSK-1482160

GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat) . GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI) [1][2][3].

Product Specifications

CAS Number

[1001389-72-5]

UNSPSC

12352005

Target

Interleukin Related; P2X Receptor

Type

Reference compound

Related Pathways

Immunology/Inflammation; Membrane Transporter/Ion Channel

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/gsk-1482160.html

Concentration

10mM

Purity

98.67

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C([C@H](CC1)N(C)C1=O)NCC2=CC=CC(C(F)(F)F)=C2Cl

Molecular Formula

C14H14ClF3N2O2

Molecular Weight

334.72

References & Citations

[1]Ali Z, et al. Pharmacokinetic and pharmacodynamic profiling of a P2X7 receptor allosteric modulator GSK1482160 in healthy human subjects. Br J Clin Pharmacol. 2013;75 (1) :197-207. doi:10.1111/j.1365-2125.2012.04320.x|[2]Abdi MH, et al. Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor. Bioorg Med Chem Lett. 2010 Sep 1;20 (17) :5080-4.|[3]Liu X, et al. Unlocking the therapeutic potential of P2X7 receptor: a comprehensive review of its role in neurodegenerative disorders. Front Pharmacol. 2024 Jul 30;15:1450704.