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PF-03049423 free base

Names

[ CAS No. ]:
954138-07-9

[ Name ]:
PF-03049423 free base

Biological Activity

[Description]:

PF-03049423 (Compound PF-5) free base is a potent and highly selective phosphodiesterase-5A inhibitor with an IC50 of about 0.2 nM for rat and human platelet enzyme. PF-03049423 free base can be used for the research of acute ischaemic stroke[1].

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)
Research Areas >> Neurological Disease

[Target]

PDE5A

rat and human platelet enzyme:~0.2 nM (IC50)


[In Vivo]

PF-03049423 (Compound PF-5) (1-10 mg/kg; s.c.; b.i.d. for 7 days) promotes functional recovery in a rat model of severe stroke induced by permanent middle cerebral artery occlusion[1]. PF-03049423 (1.0 mg/kg b.i.d. or 0.6 mg/kg q.d. for 7 days) improves poststroke sensory–motor behavioral outcome even when the treatment is initiated 24-72 hours after occlusion[1]. Animal Model: Male Sprague-Dawley rats, middle cerebral artery occlusion (MCA-o) model[1] Dosage: 0.1, 1, or 10 mg/kg Administration: Subcutaneous injection, b.i.d. for 7 days Result: Improved functional recovery at 1 mg/kg and 10 mg/kg.

Chemical & Physical Properties

[ Molecular Formula ]:
C24H32N6O4

[ Molecular Weight ]:
468.54900

[ Exact Mass ]:
468.24900

[ PSA ]:
105.84000

[ LogP ]:
1.40590


Related Compounds

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