PDE11 Inhibitor

PF-05180999 (PF-999) is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC₅₀ of 1.6 nM.

BC11-38 is a potent, selective, and biologically active PDE11 inhibitor, with IC₅₀s of 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively. BC11-38 elevates cAMP levels, PKA-mediated ATF-1 phosphorylation, and cortisol production in H295R cells.

PF-04822163 is an orally active, selective, and blood-brain barrier permeable PDE1 inhibitor with IC₅₀ values of 2 nM, 2.4 nM, and 7 nM for PDE1A, PDE1B, and PDE1C respectively. PF-04822163 can be used in the research of attention deficit hyperactivity disorder or Parkinson's disease.

TPN729MA (TPN729 maleate) is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC₅₀ value of 2.28 nM. TPN729MA affects erectile function and it can be used for the research of erectile dysfunction.

TPN729 is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC₅₀ value of 2.28 nM. TPN729 affects erectile function and it can be used for the research of erectile dysfunction.

PDE11A4-IN-2 is a selective PDE11A4 inhibitor with an IC₅₀ of 33 nM. PDE11A4-IN-2 functionally inhibits PDE11A4-mediated catalytic activities of cAMP and cGMP in cellular models. PDE11A4-IN-2 is applicable to the research of age-related cognitive decline.

PDE3/4-IN-4 is an orally active PDE3A and PDE4B inhibitor with IC₅₀ values of 10 nM and 9.4 nM, respectively. PDE3/4-IN-4 shows selective activity relative to most other PDE family members. PDE3/4-IN-4 modulates the cAMP/PKA/CREB signaling pathway. PDE3/4-IN-4 inhibits pro-inflammatory factor IL-6. PDE3/4-IN-4 reduces expression of inflammatory markers in liver tissue. PDE3/4-IN-4 attenuates liver fibrosis. PDE3/4-IN-4 limits liver damage in cholestatic and sepsis-induced liver disease mice models. PDE3/4-IN-4 can be used for the research of liver injury, cholestatic liver diseases, sepsis-induced liver injury.

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.

PDE11-IN-1 is a PDE11 inhibitor and can be used for adrenal insufficiency research.

PDE11A4-IN-1 is a selective, cell-permeable inhibitor of phosphodiesterase 11A4 (PDE11A4) with an IC₅₀ of 12 nM. PDE11A4-IN-1 inhibits PDE11A4-mediated hydrolysis of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) to the same extent. PDE11A4-IN-1 can be used in the research of age-related cognitive decline.

PDE5-IN-13 (Compound 14b) inhibits phosphodiesterase 5 (PDE5A) with an IC₅₀ of 3 nM. PDE5-IN-13 is a potential candidate for PAH (pulmonary arterial hypertension) research. PDE5-IN-13 has high selectivity for targets over PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11. PDE5-IN-13 is orally active.

TC-E 5005 is a potent and selective PDE10A inhibitor with IC₅₀ values of 7.28, 239, 779, 919, 3,100, and 3,700 nM for PDE10A, 2A, 11A, 5A, 7B and 3A, respectively. TC-E 5005 inhibits adrenergic and neurogenic smooth muscle contractions in the human prostate.