PF-2545920

• CAT Number: I005378
• CAS Number: 898562-94-2
• Molecular Formula: C25H20N4O
• Molecular Weight: 392.5
• Purity: ≥95%
• Target: PDE10A
• Solubility: DMSO: ≥ 45 mg/mL
• Storage: -20°C
• IC50: 0.37 nM
• IUPAC Name: 2-[[4-(1-methyl-4-pyridin-4-ylpyrazol-3-yl)phenoxy]methyl]quinoline
• InChI: InChI=1S/C25H20N4O/c1-29-16-23(18-12-14-26-15-13-18)25(28-29)20-7-10-22(11-8-20)30-17-21-9-6-19-4-2-3-5-24(19)27-21/h2-16H,17H2,1H3
• InChIKey: AZEXWHKOMMASPA-UHFFFAOYSA-N
• SMILES: CN1C=C(C(=N1)C2=CC=C(C=C2)OCC3=NC4=CC=CC=C4C=C3)C5=CC=NC=C5

PF-2545920 (Cat.No:I005378) is a selective inhibitor of the protein kinase C theta (PKCθ) enzyme. It has shown potential in modulating immune responses and inflammation. PF-2545920 has been investigated for its therapeutic applications in various immune-mediated disorders, including autoimmune diseases and organ transplantation. Clinical studies are underway to evaluate its efficacy and safety.

Reference

1:The Phosphodiesterase 10A Inhibitor PF-2545920 Enhances Hippocampal Excitability and Seizure Activity Involving the Upregulation of GluA1 and NR2A in Post-synaptic Densities. Zhang Y, Gao B, Zheng F, Lu S, Li Y, Xiong Y, Yang Q, Yang Y, Fu P, Xiao F, Wang X.Front Mol Neurosci. 2017 Apr 7;10:100. doi: 10.3389/fnmol.2017.00100. eCollection 2017. PMID: 28439226 Free PMC Article
2:Phosphodiesterase 10A inhibitor, MP-10 (PF-2545920), produces greater induction of c-Fos in dopamine D2 neurons than in D1 neurons in the neostriatum. Wilson JM, Ogden AM, Loomis S, Gilmour G, Baucum AJ 2nd, Belecky-Adams TL, Merchant KM.Neuropharmacology. 2015 Dec;99:379-86. doi: 10.1016/j.neuropharm.2015.08.008. Epub 2015 Aug 7. PMID: 26256420
3:Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia. Verhoest PR, Chapin DS, Corman M, Fonseca K, Harms JF, Hou X, Marr ES, Menniti FS, Nelson F, O/'Connor R, Pandit J, Proulx-Lafrance C, Schmidt AW, Schmidt CJ, Suiciak JA, Liras S.J Med Chem. 2009 Aug 27;52(16):5188-96. doi: 10.1021/jm900521k. PMID: 19630403