PDE4/5-IN-1 

PDE4/5-IN-1 is a selective phosphodiesterase 4/5 (PDE4/5) dual inhibitor. PDE4/5-IN-1 functionally inhibits PDE5, PDE4B2, and PDE4D2 activity. PDE4/5-IN-1 relaxes isolated rat prostate tissue, enhances nitric oxide-induced relaxation in isolated rat prostate tissue, and reduces alpha-1 adrenoceptor-mediated contractile responses in isolated rat prostate tissue. PDE4/5-IN-1 inhibits proliferation of human hyperplastic prostate cells. PDE4/5-IN-1 can be used for the research of benign prostatic hyperplasia^[1].

PDE4/5-IN-1 (Compound VIII) (1-10 μM) exhibits dual inhibitory activity against PDE4 (specifically PDE4B2 and PDE4D2) and PDE5 enzymes at 1 μM, and also inhibits PDE6 and PDE11 enzymes at 10 μM in cell-free assays^[1].
PDE4/5-IN-1 (0.003 μM-3 μM) significantly inhibits the proliferation of RWPE-1, BPH-1, and WPMY-1 human prostate cell lines, with the strongest effect in WPMY-1 stromal cells^[1].
PDE4/5-IN-1 (3 μM) significantly potentiates SNP (HY-B0564)-induced relaxation and reduces alpha-1 adrenoceptor-mediated contractile responses in rat prostatic tissue^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

433.41

C₂₃H₁₉N₃O₆

1807631-43-1

O=C1CN(CCO)C(C2=C(C3=CNC4=C3C=CC=C4)OC(C5=CC=C(OCO6)C6=C5)N21)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Helfstein DR, et al. Synthesis and Pharmacological Evaluation of 6,7-Dihydro‑3H‑Oxazolo[3,4‑a]Pyrazine-5,8-Dione Compounds as Inhibitors of Phosphodiesterases 4 and 5. ACS Med Chem Lett. 2026;17(2):341-350. Published 2026 Jan 20.  [Content Brief]