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PF-03049423

Names

[ CAS No. ]:
402955-58-2

[ Name ]:
PF-03049423

[Synonym ]:
Pf-03049423 Hydrochloride
3-[4-(2-Hydroxyethyl)-1-piperazinyl]-7-(6-methoxy-3-pyridinyl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one hydrochloride (1:1)
Pyrido[3,4-b]pyrazin-2(1H)-one, 3-[4-(2-hydroxyethyl)-1-piperazinyl]-7-(6-methoxy-3-pyridinyl)-1-(2-propoxyethyl)-, hydrochloride (1:1)

Biological Activity

[Description]:

PF-03049423 is a potent, selective, orally active, and brain penetrant inhibitor of PDE5 with IC50 of 0.2 nM; displays 158-fold and 2460-fold selectivity over PDE6 and PDE11, respectively; possesses an excellent potency and selectivity profile and demonstrates robust in vivo blood pressure lowering in a spontaneously hypertensive rat (SHR) model. Stroke Phase 2 Discontinued

[References]

References 1. Hughes RO, et al. J Med Chem. 2010 Mar 25;53(6):2656-60. 2. Di Cesare F, et al. J Stroke Cerebrovasc Dis. 2016 Mar;25(3):642-9. View Related Products by Target Phosphodiesterase (PDE) Stroke

Chemical & Physical Properties

[ Molecular Formula ]:
C24H32N6O4

[ Molecular Weight ]:
505.010

[ Exact Mass ]:
504.225189

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ Precautionary Statements ]:
P301 + P312 + P330

[ RIDADR ]:
NONH for all modes of transport

Related Compounds