PDE5 Inhibitor

PF-00489791 (PF-489791) is a potent inhibitor of phosphodiesterase 5A with IC₅₀ of 1.5 nM. PF-00489791 can enhance the relaxation of blood vessels within the kidney and so reduce blood pressure, improving renal function.

PDE5-IN-4 is a phosphodiesterase 5 inhibitor. PDE5-IN-4 can be used for the research of acute myocardial infarction and damage caused by reperfusion, gastrointestinal diseases, damage caused by diabetes, and liver failure.

TPN171 is a potent, selective and oral bioavailable inhibitor of phosphodiesterase type 5 (PDE5) with an IC₅₀ of 0.62 nM, being developed for the treatment of pulmonary arterial hypertension (PAH).

MY-5445 is a specific inhibitor of the cyclic GMP phosphodiesterase, phosphodiesterase type 5 (PDE5), with a K_i of 1.3 μM. MY-5445 inhibits human platelet aggregation. MY-5445 is a selective modulator of ATP-binding cassette (ABC) transporter ABCG2, with anti-proliferative effect.

Robustine, a furoquinoline alkaloid, from Dictamnus albus, exhibits inhibitory potency against human phosphodiesterase 5 (hPDE5A) in vitro.

Gisadenafil besylate (UK 369003-26) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC₅₀ of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP).

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.

CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC₅₀ values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer’s disease.

(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.

MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE V; PDE5) inhibitor with an IC₅₀ of 19 nM. MBCQ lacks inhibitory activity toward other PDE isozymes (all IC₅₀s>100 μM). MBCQ dilates coronary arteries via specific inhibition of cGMP-PDE.

Acetildenafil is a Sildenafil (HY-15025) analogue, a phosphodiesterase 5 (PDE5) inhibitor. Acetildenafil can be isolated from herbal products.

Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC₅₀ of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC₅₀s of 0.30 μM, 0.17 μM, 17.89 μg/mL, 10.98 μM, 8.37 μM and 8.21 μM, respectively.

ent-Tadalafil (ent-IC-351), compound (6S,12aS), is a inactive cis-enantiomer of compound (6R,12aS). compound (6R,12aS) is a potent PDE5 inhibitor with an IC₅₀ of 0.090 μM, while ent-Tadalafil is inactive at concentrations up to 10 µM.

FR-229934 is a PDE V inhibitor extracted from patent WO2019130052A1. FR-229934 can be used for the research of pulmonary arterial hypertension and erectile dysfunction.

Carbodenafil is a Sildenafil (UK-92480) related compound found in health foods. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.

Kuraridine is a prenylated flavonol extract from the roots of Sophora flavescens. Kuraridine has an inhibitory effect on cGMP specific phosphodiesterase type 5 (PDE5) (IC₅₀=0.64 μM).

Lodenafil carbonate, a dimer that acts as a proagent delivering Lodenafil in vivo, is an orally active phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).

Yonkenafil (Tunodafil) hydrochloride, a novel phosphodiesterase 5 (PDE5) inhibitor, is effective in reducing cerebral infarction, neurological deficits, edema, and neuronal damage in the infarcted area. Yonkenafil (Tunodafil) hydrochloride may improve cognitive function by modulating neurogenesis and has a potential therapeutic effect on Alzheimer's disease.

Thioquinapiperifil dihydrochloride (KF31327), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC₅₀ of 0.074 nM) inhibitor, is used for sexual enhancement study.

T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC₅₀=0.23 nM). T-0156 inhibits PDE6 (IC₅₀=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC₅₀>10 μM). T-0156 enhances the nitric oxide (NO)/cGMP pathway.