pde2

CP 461 (UNII-68OJX9I7DT), a specific PDE2A inhibitor, is a novel pro-apoptotic compound that inhibits cyclic GMP phosphodiesterase but not cyclooxygenase-1 or -2. CP 461 inhibits the growth of a variety of human tumor cell lines in vitro and selectively induces apoptosis in cancer cell lines, but not in normal cells.

Indomethacin is an orally active nonsteroidal anti-inflammatory drug (NSAID) that non-selectively inhibits cyclooxygenase enzymes COX-1 and COX-2, with IC₅₀ values of 18 nM and 26 nM, respectively. It exhibits good blood-brain barrier permeability and shows significant anti-inflammatory, anti-tumor, and anti-infective activities. Indomethacin is widely used in research related to cancer, inflammation, and viral infections, and is also commonly used to induce gastric ulcer models in animals.

Luteolin (Luteolol) belongs to the flavonoid group of natural products and is a Nrf2 inhibitor, PDE inhibitor. Luteolin has a wide range of biological activities including antitumor, antioxidant, anti-inflammatory, antimicrobial, antiviral, antiallergic, and procoagulant.

Milrinone (Win 47203) is a Phosphodiesterase 3 Inhibitor. The mechanism of action of milrinone is as a Phosphodiesterase 3 Inhibitor.

Zomepirac sodium salt (McN-2783-21-98) is a prostaglandin synthetase inhibitor.

EHNA hydrochloride is a selective inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2) and adenosine deaminase (ADA) with anticancer activity, increasing intracellular adenosine concentration in a treatment time-dependent manner. EHNA hydrochloride inhibits PHA and NaI04 mitogenesis.

Bay 60-7550 is a selective and potent PDE2 inhibitor (Ki: 3.8 nM) that exerts positive inotropic effects on rat heart by increasing PKA-mediated phosphorylation and can be used to ameliorate cognitive impairments and memory disorders.

PF-05180999 (PF-999) is a selective and potent phosphodiesterase 2A (PDE2A) inhibitor that enhances long-term memory in a contextual fear conditioned reflex model in rats.

Carbazeran (UK-31,557) is an inhibitor of PDE2 and PDE3 and can be used for studies about metabolic diseases. Carbazeran shows inotropic and chronotropic effects in vivo(EC50 = 100 μM).

RS-25344 is a potent and selective phosphodiesterase (PDE) 4 inhibitor. It inhibits eosinophil chemotaxis and increases progressive motility of spermatozoa in vitro.

PDE2/PDE10-IN-1 is an inhibitor of phosphodiesterase 2 (PDE2) and PDE10, with IC50 values of 29 nM and 480 nM, respectively.

PDE2 inhibitor6 (Compound 1) is an orally active phosphodiesterase (PDE) inhibitor, effectively inhibiting PDE2A, PDE3B, and PDE10A2 with IC50 values of 0.95 nM, 6.17 μM (pIC50=5.21), and 87.1 nM (pIC50=7.06), respectively. It modulates AMPA receptor activity, enhances synaptic plasticity, and improves learning and memory in rat models. Furthermore, PDE2 inhibitor6 possesses blood-brain barrier permeability.

PDE2A-IN-1 is a phosphodiesterase 2A (PDE2A) inhibitor with an IC50 value of 1.3 nM.

inhibitor of phosphodiesterase type 5 (PDE5).This compound is unstable in powder form and other related salt forms are recommended.

T-0156 is a novel, potent and selective phosphodiesterase type 5 inhibitor that inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) with low affinity for PDE6, PDE1, PDE2, PDE3 and PDE4.

Vardenafil (Vivanza) is an oral therapy for the treatment of erectile dysfunction. It is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). Penile erection is a hemodynamic process initiated by the relaxation of smooth muscle in the corpus cavernosum and its associated arterioles. During sexual stimulation, nitric oxide is released from nerve endings and endothelial cells in the corpus cavernosum. Nitric oxide activates the enzyme guanylate cyclase resulting in increased synthesis of cyclic guanosine monophosphate (cGMP) in the smooth muscle cells of the corpus cavernosum. The cGMP in turn triggers smooth muscle relaxation, allowing increased blood flow into the penis, resulting in erection. The tissue concentration of cGMP is regulated by both the rates of synthesis and degradation via phosphodiesterases (PDEs). The most abundant PDE in the human corpus cavernosum is the cGMPspecific phosphodiesterase type 5 (PDE5); therefore, the inhibition of PDE5 enhances erectile function by increasing the amount of cGMP.

Ibudilast (MN-166)(KC-404;AV-411;MN-166) is a relatively nonselective phosphodiesterase inhibitor. It is approved for use as an anti-inflammatory in Japan.

ICI 63197 (2-Amino-6-methyl-4-propyl-[1,2,4]triazolo[1,5-a]pyrimidin-5(4H)-one) is a PDE4 inhibitor.

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

Vardenafil hydrochloride is a New Phosphodiesterase Type 5(PDE5) Inhibitor, in the Treatment of Erectile Dysfunction in Men With Diabetes

RS 25344 hydrochloride is a phosphodiesterase (PDE) 4 inhibitor

K134 is an inhibitor of phosphodiesterase 3. The IC50s of K134 for PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 μM, respectively.

EHNA is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2) (IC50 = 4 μM) and adenosine deaminase (ADA). It exhibits concentration-dependent inhibition of cGMP-stimulated PDE2 activity, with IC50 values of 0.8 μM in humans and 2 μM in porcine myocardium, but shows limited inhibition on unstimulated PDE2. EHNA is involved in modulating various pharmacological responses, such as antiviral, antitumor, and antiarrhythmic effects.

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.