PF 05180999

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-05180999 (PF 5180999) 是一种有效、选择性、脑穿透性、口服生物可利用的磷酸二酯酶 2A (PDE2A) 抑制剂，IC50 为 1 nM。

PF-05180999 (PF 5180999) is a potent, selective, brain-penetrating and orally bioavailable phosphodiesterase 2A (PDE2A) inhibitor with IC50 of 1 nM; displays >1,000-fold selectivity over PDE10; shows potential for treatment of schizophrenia.Schizophrenia Phase 1 Discontinued.

PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM. PF-05180999 binds to the rat, dog and monkey PDE2A, with Kis of 4.2, 8.4, and 5.5 nM and IC50s of 2.6, 5.2, and 3.4 nM, respectively. PF-05180999 shows weak activity against PDE, with IC50s of 2.03 μM (PDE10A1), 26.969 μM (PDE7B), 50.09 μM (PDE11A4), and >56.25 μM (PDE1B1, PDE3A1, PDE4D3, PDE5A1, PDE6 (bovine), PDE8B, PDE9A1), respectively. PF-05180999 is also a weak inducer of CYP3A4, and with no direct inhibition of human recombinant cytochrome P450 (CYP) enzymes (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A) and no induction of CYP1A2.

PF-05180999 (Compound 30; 0.032-0.32 mg/kg mg/kg, s.c.) dramatically reduces the working memory errors produced by ketamine in a working memory radial arm maze (RAM) model in rats. PF-05180999 causes acute and exposure-dependent elevation in the accumulation of cGMP bulk levels in the cortex, striatum, and hippocampus, but with no changes in cAMP and the associated downstream phospho-cAMP response element-binding protein (p-CREB) in mice.

PF-05180999 | PF05180999 | PF 5180999

Angiogenesis

PDE

PDE

Neurological Disease

Schizophrenia

1394033-54-5

414.396

C19H17F3N8

>98% (HPLC)

DMSO : 50 mg/mL 120.66 mM

FC(C1=CN=C(C2=C(C3=C4C(N5CCC5)=NC=NN4C(C)=N3)C=NN2C)C=C1)(F)F

4-(1-Azetidinyl)-7-methyl-5-[1-methyl-5-[5-(trifluoromethyl)-2-pyridinyl]-1H-pyrazol-4-yl]-imidazo[5,1-f][1,2,4]triazine

(-20℃)

With Ice Pack

≥ 2 years