PF-04957325是一种高效，选择性的 PDE8 抑制剂，抑制PDE8A和PDE8B的IC₅₀值分别为0.7 nM和0.3 nM。

PF-04957325 is a highly potent and selective PDE8 inhibitor, with IC 50 s of 0.7 nM and 0.3 nM for PDE8A and PDE8B, respectively.

Solid

IC50: 0.7 nM (PDE8A), less than 0.3 nM (PDE8B)

PF-04957325 is over two orders of magnitude less efficient than PICL in suppressing polyclonal Teff cell proliferation, and shows no effect on cytokine gene expression in these cells, despite its robust effect on T cell adhesion. PF-04957325 is a selective PDE8 inhibitor and inhibits breast cancer cell migration. PF-04957325 greatly potentiates steroidogenesis in WT adrenal cells. PF-04957325 shows a reported IC50 of 0.7 nM against PDE8A, 0.2 nM against PDE8B, and > 1.5 μM against all other PDE isoforms. PF-04957325 treatment of WT Leydig cells or MA10 cells increases steroid production but has no effect in PDE8A (-/-)/B(-/-) double-knockout cells, confirming the selectivity of the drug. Moreover, under basal conditions, cotreatment with PF-04957325 plus rolipram, a PDE4-selective inhibitor, synergistically potentiates steroid production.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Vang AG, et al. Differential Expression and Function of PDE8 and PDE4 in Effector T cells: Implications for PDE8 as a Drug Target in Inflammation. Front Pharmacol. 2016 Aug 23;7:259.
[2]. Dong H, et al. Inhibition of breast cancer cell migration by activation of cAMP signaling. Breast Cancer Res Treat. 2015 Jul;152(1):17-28.

In Vitro: DMSO : ≥ 100 mg/mL (249.76 mM)配制储备液