PF-03049423

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-03049423 是一种有效、选择性、口服活性、脑渗透性 PDE5 抑制剂，IC50 为 0.2 nM。

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.

——

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.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. Animal Model:Male Sprague-Dawley rats, middle cerebral artery occlusion (MCA-o) model 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.

PF 03049423

Angiogenesis

PDE

PDE

Neurological Disease

Stroke

402955-58-2

468.55

C24H32N6O4

>98% (HPLC)

——

CCCOCCN1C2=CC(=NC=C2N=C(C1=O)N3CCN(CC3)CCO)C4=CN=C(C=C4)OC.Cl

3-[4-(2-Hydroxyethyl)-1-piperazinyl]-7-(6-methoxy-3-pyridinyl)-1-(2-propoxyethyl)-pyrido[3,4-b]pyrazin-2(1H)-one

(-20℃)

With Ice Pack

≥ 2 years