PDE9 Inhibitor

Moracin M is a phenolic component that can be isolated from Mori Cortex, is a potent phosphodiesterase-4 (PDE4) inhibitor with IC₅₀ values of 2.9, 4.5, >40, and >100 μM for PDE4D2, PDE4B2, PDE5A1, and PDE9A2, respectively. Moracin M has anti-inflammatory activity.

Edelinontrine (PF-04447943) is a potent inhibitor of human recombinant PDE9A (IC₅₀=12 nM) with >78-fold selectivity, respectively, over other PDE family members (IC₅₀>1000 nM).

BAY 73-6691 ((R)-BAY 73-6691) is a potent, brain penetrant, and selective PDE9A inhibitor.

PF-04449613 is a selective PDE9A inhibitor with an IC50 of 22 nM[1]. PF-04449613 improved motor learning ability in a mouse model[2].

Osoresnontrine (BI-409306) is a potent and selective PDE9A inhibitor, with an IC₅₀ of 52 nM, and shows weak activity against other PDEs, such as PDE1A (IC₅₀, 1.4 µM), PDE1C (IC₅₀, 1.0 µM), PDE2A, PDE3A, PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC₅₀ all > 10 μM); Osoresnontrine can be used in the research of memory enhancement in CNS disorders.

PDE9-IN-1 is a potent, selective, and orally bioavailable phosphodiesterase-9A (PDE9A) Inhibitor with an IC₅₀ of 8.7 nM.

BAY-7081, a chemical probe, is a potent, selective, orally active and soluble cyanopyridone-based PDE9A inhibitor with an IC₅₀ of 15 nM.

Tovinontrine (IMR-687) is a highly potent and selective phosphodiesterase-9 (PDE9) inhibitor specifically for the treatment of sickle cell disease. IC₅₀s are 8.19 nM and 9.99 nM for PDE9A1 and PDE9A2, respectively.

(S)-C33 is a potent and selective PDE9 (phosphodiesterase-9) inhibitor, with an IC₅₀ of 11 nM. (S)-C33 can be used for central nervous system diseases and diabetes research.

PDE-9 inhibitor is a potent PDE-9 inhibitor. PDE-9 inhibitor can be used for neurodegenerative diseases, such as Alzheimer's disease and schizophrenia.

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.

Menabitan dihydrochloride (SP-204 dihydrochloride) is the dihydrochloride form of Menabitan (HY-160991). Menabitan dihydrochloride is an inhibitor for phosphodiesterase 9 (PDE 9), which acts as a non-opioid analgesic agent. Menabitan dihydrochloride lowers the intraocular pressure in rabbit model.

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.

Menabitan (SP-204) is an inhibitor for phosphodiesterase 9 (PDE 9), which acts as a non-opioid analgesic agent. Menabitan lowers the intraocular pressure in rabbit model.

(R)-Irsenontrine ((R)-E2027), the R-enantiomer of Irsenontrine (HY-132821), is a potent phosphodiesterase 9 (PDE9) inhibitor with an IC₅₀ value of 0.041 μM. (R)-Irsenontrine can be used for the research of neurological diseases.

LH17, a Kaempferol (HY-14590) derivative, is a potent and selective PDE4 inhibitor (PDE4D2 IC₅₀ = 73 nM, PDE4B2 IC₅₀ = 190 nM). LH17 exhibits remarkable selectivity (>136-fold) against other PDE isoforms (PDE1B/2A/3A/5A/8A/9A/10A) (IC₅₀ > 10000 nM), with the exception of PDE7A1 (IC₅₀ = 300 nM). LH17 distinctly interacts with PDE4 M-pocket. LH17 demonstrates remarkable anti-fibrotic efficacy in both in vitro and in vivo models. LH17 can be used for idiopathic pulmonary fibrosis (IPF) research.

PDE4-IN-1 is a PDE4 inhibitor with high potency (IC₅₀ : 8.6 nM) and selectivity over other PDE subtypes. PDE4-IN-1 inhibits the release of inflammatory cytokines and chemokines. PDE4-IN-1 greatly restores impaired cAMP-CREB signaling pathway. PDE4-IN-1 inhibits proliferation and promotes differentiation to reverse the formation of psoriasis.

PDE1-IN-4 (compound 2g) is a potent and selective PDE1 (phosphodiesterase-1) inhibitor, with IC₅₀ values of 10, 145, and 354 nM for PDE1C, PDE1A, and PDE1B, respectively. PDE1-IN-4 inhibits myofibroblast differentiation of human lung fibroblasts induced by TGF-β1. PDE1-IN-4 shows anti-fibrosis effects through the regulation of cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate). PDE1-IN-4 can be used for idiopathic pulmonary fibrosis (IPF) research.

PDE1-IN-8 (Compound 3f) is the inhibitor for PDE1 with an IC₅₀ of 11 nM. PDE1-IN-8 inhibits cAMP and cGMP signaling pathway, inhibits the differentiation and proliferation of cells into myofibroblast, and exhibits anti-fibrotic efficacy in Bleomycin (HY-17565)-induced rat pulmonary fibrosis model.