pde7

PDE7-IN-2 is an inhibitor of phosphodiesterase 7 (IC50 = 2.1 µM) and can be used in Parkinson's disease studies.

PDE7 inhibitor S14 is a cell-permeable PDE7 inhibitor that acts by targeting the cyclic adenosine monophosphate (cAMP) cAMP-response element-binding protein (CREB) pathway.

PDE7-IN-3 (Example 2) serves as an inhibitor of phosphodiesterase PDE7 and exhibits potential analgesic properties. It is applicable in the research of various pain types including inflammatory, neuropathic, visceral, and nociceptive pain [1].

PDE7A-IN-1 (Compound 26) is an orally active PDE7A inhibitor with an IC50 value of 3.7 nM. By inhibiting sclerostin, PDE7A-IN-1 significantly enhances bone mineral density, making it suitable for studies on osteoporosis and related bone metabolic disorders.

Avanafil (TA1790) is a selective inhibitor of phosphodiesterase type 5 (PDE5) and is used as therapy of erectile dysfunction.

BRL-50481 is a novel and selective PDE7 inhibitor with IC50 values of 0.15 μM for PDE7A, 12.1 μM for PDE7B, 62 μM for PDE4, and 490 μM for PDE3.

VP3.15 is an orally bioavailable and CNS-penetrant dual inhibitor of phosphodiesterase (PDE)7- GSK3 (IC50s: 1.59 μM and 0.88 μM for PDE7 and GSK-3).

PDE5-IN-13 (Compound 14b) inhibits phosphodiesterase 5 (PDE5A) with an IC50 of 3 nM and is applicable in pulmonary arterial hypertension research. It demonstrates high selectivity for its target compared to PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11, and it possesses oral bioavailability.

P7-2302 inhibits PDE7 and PDE4B with IC50 values of 0.18 nM and 77.3 nM, respectively. It also inhibits the efflux of P-gp and BCRP (breast cancer resistance protein) and shows low uptake in rat brains. When labeled with 18F, P7-2302 can be used as a PET tracer.

VP3.15 dihydrobromide is a potent, orally bioavailable, and CNS-penetrant dual inhibitor of phosphodiesterase (PDE7) and glycogen synthase kinase (GSK)3, with IC50 values of 1.59 μM and 0.88 μM, respectively.

GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380, 000-fold selectivity versus PDE1 2 3 5 6 and >2500-fold selectivity against PDE4B versus PDE7.Phase 2.

PDE4-IN-12 is a potent and safe ubiquitous PDE4 inhibitor with an IC50 of 3.5 nM (SI: 2.71) and also acts on PDE7 with an IC50 of 15 nM (SI: 4.27).

Avanafil dibesylate is a PDE5 inhibitor.

PDE11A4-IN-1 (compound 23b) is a potent, selective inhibitor of PDE11A4 with an IC50 of 12 nM, demonstrating high selectivity against PDE1, PDE2, PDE7, PDE8, and PDE9 [1].