ARN25657

ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM) . ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP) -mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders[1].

Product Specifications

UNSPSC

12352005

Target

Dopamine Receptor; GSK-3; P-glycoprotein; PKA

Related Pathways

GPCR/G Protein; Membrane Transporter/Ion Channel; Neuronal Signaling; PI3K/Akt/mTOR; Stem Cell/Wnt; TGF-beta/Smad

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Smiles

O=C(N(C1=CC(C2=CC=CN=C2)=CC=C1N3)C3=O)NCCCN4CCN(C5=CC=CC=C5)CC4

Molecular Formula

C26H28N6O2

Molecular Weight

456.54

References & Citations

[1]Di Martino RMC, et al. Rational optimization of D3R/GSK-3β dual target-directed ligands as potential treatment for bipolar disorder: Design, synthesis, X-ray crystallography, molecular dynamics simulations, in vitro ADME, and in vivo pharmacokinetic studies. Eur J Med Chem. 2025 Jun 25;297:117899.