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BP165159
BIO-X

PF05085727

A potent inhibitor of cGMP-dependent phosphodiesterase 2A (PDE2A) with IC50 = 2 nM. It is a highly selective compound for PDE2A with > 500-fold higher affinity over other phosphodiesterases. The compound demonstrated in vivo activity as evidenced by the increase of cGMP in rodent brain. It has improved brain penetration, which makes it suitable for the treatment of neurological disorders. The compound is able to reverse anxiolytic behaviour, enhance performance of new object recognition and social recognition tasks.  It potentiates NMDA signalling and reverses the behavioural effects of NMDA antagonists.

Technical Data

CAS No: 1415637-72-7
Product Code: BP165159
Chemical Formula: C20H18F3N7
Molecular Weight: 413.40

Literature

References
  • Helal et al., 2017. Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor. J. Med. Chem. 60 (13), 5673–5698.

Solubility

Stability

Datasheets


PF05085727

CAS No:
1415637-72-7
Chemical Formula:
Molecular Weight:
413.40
Product Structure
References:
1. Helal et al., 2017. Application of Structure-Based Design and Parallel Chemistry to Identify a Potent, Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor. J. Med. Chem. 60 (13), 5673–5698.

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