pde9

PDE9-IN-1 is a selective and orally bioavailable Inhibitor of PDE9A(IC50 of 8.7 nM).

PDE-9 inhibitor is used for treatment neurodegenerative diseases.

PDE9-IN-(S)-C33 ((S)-C33) is a potent and selective inhibitor of PDE9 (IC50 = 11 nM). PDE9-IN-(S)-C33 can be used for central nervous system diseases and diabetes research.

PDE9-IN-2 (compound 6) is a PDE9 inhibitor that enhances heart failure management.

BAY 73-6691 is an inhibitor of brain penetrant PDE9A.

PF-04447943 (Edelinontrine) is a potent and selective phosphodiesterase 9A inhibitor with an IC50 of 12 nM, which is 78-fold more selective than that used for other PDE family members (IC50>1000 nM).PF-04447943 exhibits anti-inflammatory activity, attenuates inflammatory responses by inhibiting oxidative stress, inflammation, and modulating T-cell polarization, and may be useful for research on sickle cell anemia.

PF-04822163 is a potent inhibitor of PDE1 with IC50 value of 0.0024 μM.

(R)-Irsenontrine ((R)-E2027), the R-enantiomer of Irsenontrine, is a potent inhibitor of phosphodiesterase 9 (PDE9) with an IC50 of 0.041 μM, primarily used in neurological disease research [1].

Tovinontrine (IMR-687) (IMR-687) is a potent and selective inhibitor of phosphodiesterase-9 (PDE9), designed to target sickle cell disease treatment. It exhibits high efficacy, with IC 50 values of 8.19 nM and 9.99 nM for PDE9A1 and PDE9A2, respectively [1].

PDE1-IN-8 (Compound 3f) acts as an inhibitor of PDE1, with an IC50 of 11 nM. It hinders cAMP and cGMP signaling pathways, impeding the differentiation and proliferation of cells into myofibroblasts, and demonstrates antifibrotic effects in the Bleomycin-induced rat model of pulmonary fibrosis.

PF-04449613 is a phosphodiesterase 9A (PDE9A) inhibitor (IC50= 22 nM).1It is selective for PDE9A over PDE1C (IC50= >1,000 nM), as well as over a variety of other PDEs, inhibiting PDE2-8, -10, and -11 activity by less than 30% in a panel of enzymes, ion channels, and transporters at 1 μM but does inhibit the human dopamine transporter (DAT; Ki= 293 nM). PF-04449613 (0.1-100 mg/kg, s.c.) increases cerebrospinal fluid (CSF) levels of cyclic GMP (cGMP) in rats. Subcutaneous administration of PF-04449613 (10 mg/kg) increases the rate of dendritic spine formation and elimination in mouse primary motor cortex pyramidal neuronsin vivo.2It increases the average running speed of mice in an accelerating rotarod task, indicating improved motor learning, at the same dose. 1.Claffey, M.M., Helal, C.J., Verhoest, P.R., et al.Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitorsJ. Med. Chem.55(21)9055-9068(2012) 2.Lai, B., Li, M., Hu, A., et al.The phosphodiesterase 9 inhibitor PF-04449613 promotes dendritic spine formation and performance improvement after motor learningDev. Neurobiol.78(9)859-872(2018)

PDE1-IN-4 is a potent and selective inhibitor of PDE1 (phosphodiesterase-1), acting on PDE1C (IC50: 10 nM), PDE1A (IC50: 145 nM) and PDE1B (IC50: 354 nM). PDE1-IN-4 regulates cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate) and exhibits antifibrotic effects. PDE1-IN-4 can inhibit TGF-β1-induced differentiation of human lung fibroblasts, and can be used to study idiopathic pulmonary fibrosis (IPF).

BAY-7081 is a cyanopyridone-based compound that functions as a potent, selective, and orally active PDE9A inhibitor, demonstrating an inhibition concentration (IC 50) of 15 nM. It exhibits solubility in oral formulations.

Osoresnontrine is a potent and selective inhibitor of PDE9A (IC50 of 52 nM),and can be used in the research of memory.

Moracin M, a phenolic compound found in the skin of Morus alba Linn., effectively inhibits phosphodiesterase-4 (PDE4), exhibiting IC50 values of 2.9 μM and 4.5 μM for PDE4D2 and PDE4B2, respectively, and showing significantly lesser activity on PDE5A1 and PDE9A2 with values over 40 μM and 100 μM, respectively. This compound demonstrates notable anti-inflammatory activity.

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.

IMR687 is a PDE9 inhibitor that slows or stops the hydrolysis of cGMP. IMR687 can be regarded as a highly promising drug against Alzheimer's for improving memory.

Irsenontrine (E2027) is a selective and orally active inhibitor of phosphodiesterase 9 (PDE9), primarily used for researching neurological diseases.

Irsenontrine (E2027) maleate is a selective and orally active inhibitor of phosphodiesterase 9 (PDE9). It can be utilized in the study of neurological diseases.

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].