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.
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- Fòrmula: C26H28N6O2
- Peso molecular:456.54
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Almacenamiento:
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]
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Actividad biológica
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Chemical Information
- Pureza y Documentación
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Actividad biológica
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D3 Receptor 15.2 nM (EC50) |
D3 Receptor 1.5 nM (Ki) |
GSK-3β 19.3 nM (IC50) |
ARN25657 (Compound 16) (1 μM, 10 μM) inhibits P-gp-mediated efflux of acetoxymethyl calcein efflux in MDR1-MDCKII cells, logD = 1.84, inhibition percentage 10.9 % at 10 μM[1].
ARN25657 (1 μM, 5 μM, 3 h) inhibits GSK-3β activity in neuronal SH-SY5Y cells[1].
ARN25657 (10 nM, 100 nM) exhibits high affinity for D3R (68 % inhibition of binding of (+)-butaclamol; Ki = 1.5 nM) at 100 nM in CHO cells and D2R at 10 nM (80 % inhibition of [3H]7-OH-DPAT binding; Ki = 1 nM) in HEK293 cells[1].
ARN25657 (0.1 μM, 10 μM) exhibits excellent GSK-3β selectivity over FYN, PKA and CDK5/p35 with selectivity ratio (compared to GSK-3β at 0.1 μM) of 0 h, 0.1 h, 0 h respectively in a KinaseProfiler assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Neuronal SH-SY5Y cells
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Concentration:1 μM, 5 μM
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Incubation Time:3 h
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Result:Increased the inactive phospho-GSK-3α/β (Ser21/9) form.
| Species | Dose | Route | Tmax | Cmax | AUC | F | Vd | T1/2 | CL |
|---|---|---|---|---|---|---|---|---|---|
| Mice | 10 mg/kg | p.o. | 15 min | 678 ng/mL | 24957 min·ng/mL | 15 % | 95.6 L/kg | 180 min | 368 mL/min/kg |
| Mice | 3 mg/kg | i.v. | 5 min | 1429 ng/mL | 49493 min·ng/mL | 15 % | 3.3 L/kg | 38 min | 60 mL/min/kg |
Chemical Information
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Peso molecular 456.54
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Fòrmula C26H28N6O2
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SMILES
O=C(N(C1=CC(C2=CC=CN=C2)=CC=C1N3)C3=O)NCCCN4CCN(C5=CC=CC=C5)CC4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ARN25657 Related Classifications
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