pde3

IBMX (Methylisobutylxanthine) is a broad-spectrum phosphodiesterase (PDE) inhibitor with inhibitory activity against PDE3, PDE4, and PDE5 (IC50=6.5 26.3 31.7 μM). IBMX enhances the intracellular cAMP level.

Isomazole is a novel orally available phosphodiesterase (PDE) inhibitor with calcium-sensitizing properties that inhibits PDE3 and PDE4.

Cilostazol (OPC 21) is a Phosphodiesterase 3 Inhibitor. The mechanism of action of cilostazol is as a Phosphodiesterase 3 Inhibitor.

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.

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.

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

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

Pumafentrine（BY 343） is a dual PDE3 PDE4 inhibitor that reduces clinical scores and TNF expression in experimental colitis in mice.

Vesnarinone HCl (OPC-8212 HCl) is an orally active phosphodiesterase 3 (PDE3) inhibitor.Vesnarinone HCl modulates calcium and potassium ions, increasing calcium flux and decreasing potassium flux.Vesnarinone HCl is a new positive inotropic compound that enhances myocardial contractility and can be be used in heart failure studies.

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.

Adibendan (Adibendanum) is a selective inhibitor of PDE3 with an IC50 of 2.0 μM.

Siguazodan (SKF 94836) is an effective, selective, orally active phosphodiesterase III ((PDE-III)) inhibitor with an IC50 of 117 nM. Siguazodan inhibited phenylephrine induced 5-HT release with an IC50 value of 4.2 μM。 Siguazodan can increase cAMP accumulation in intact platelets, with EC50 of 18.88 μM。

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

Vesnarinone (Arkin) (INN) is a mixed phosphodiesterase 3 inhibitor and ion-channel modifier that has modest, dose-dependent, positive inotropic activity, but minimal negative chronotropic activity. It also suppresses cell proliferation and induces apoptosis by inducing the expression of p21, an inhibitor of cyclin-dependent kinase activity in p53-mediated cell cycle arrest.

Cilomilast (SB-207499) is a potent PDE4 inhibitor with an IC50 of approximately 110 nM, demonstrating anti-inflammatory activity and minimal central nervous system effects. Phase 3.

NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3).

Fenspiride hydrochloride (Decaspiride) , an oxazolidinone spiro compound, is a drug used in the therapy of certain respiratory diseases. It is approved for use in Russia for the therapy of chronic and acute inflammatory diseases of ENT organs and the respiratory tract (like sinusitis, tracheobronchitis, otitis, laryngitis, and rhinopharyngitis), and for maintenance therapy of asthma.

Olprinone (Loprinone)(Loprinone) is a selective phosphodiesterase 3 (PDE3) inhibitor.Olprinone has been reported to improve microcirculation and attenuate inflammation. Olprinone is often used to increase cardiac output after cardiopulmonary bypass (CPB).

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 hydrochloride is a phosphodiesterase (PDE) 4 inhibitor

Ensifentrine (Ensifentrinum) is a PDE3 4 inhibitor, although its affinity for PDE3(IC50: 0.4 nM) is 3,440 times higher than that for PDE4(IC50: 1479 nM), that is under clinical development for the treatment of asthma and COPD and, potentially, cystic fibrosis.

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.

MBCQ is an inhibitor of cGMP-specific phosphodiesterase PDE5.

Pimobendan (UD-CG 115 BS) is a selective inhibitor of PDE3 (IC50: 0.32 μM).

Fenspiride-d5 is intended for use as an internal standard for the quantification of fenspiride by GC- or LC-MS. Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID). It inhibits histamine-induced contraction of isolated guinea pig trachea but not histamine-induced inotropy of isolated guinea pig heart. It also inhibits phosphodiesterase 4 (PDE4), PDE5, and PDE3 (IC50s = 69, ~158, and 363 µM, respectively, in isolated human bronchi derived from patients with lung cancer). It is selective for these phosphodiesterases over PDE1 and PDE2, where it provides less than 25% inhibition. Fenspiride potentiates the airway relaxant effects of isoproterenol and sodium nitroprusside indicating an effect on cAMP and cGMP phosphodiesterases, respectively. Aerosolized fenspiride (1 mg/ml) reverses bronchoconstriction induced by capsaicin and, when used at aerosolized concentrations ranging from 1-10 mg/ml, reduces cough induced by citric aci......

BRD9500 is an orally active inhibitor of phosphodiesterases 3 (PDE3) with IC 50 s of 10 and 27 nM for PDE3A and PDE3B, respectively. BRD9500 is active in an SK-MEL-3 xenograft model of cancer [1].

PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11. PF-05085727 is an effective, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM) .

Thioquinapiperifil is a type of phosphodiesterase-5 (PDE-5) inhibitor found in dietary supplements.

Piclamilast (RP 73401) is a PDE4 inhibitor.

Pimobendan hydrochloride is a selective inhibitor of PDE3 (IC50: 0.32 μM).

Enoximone is a selective inhibitor of phosphodiesterase III (PDE3), with treatment of congestive heart failure.

Theophylline (1,3-Dimethylxanthine) sodium glycinate is a potent phosphodiesterase (PDE) inhibitor that targets PDE3 to relax airway smooth muscle and is used in asthma and chronic obstructive pulmonary disease (COPD) research. It also functions as an adenosine receptor antagonist, histone deacetylase (HDAC) activator, and exhibits anti-inflammatory activity by increasing IL-10 levels and inhibiting NF-κB nuclear import, while inducing apoptosis [1] [2] [3] [4] [5].

KCA-1490 is an inhibitor of dual PDE3/4.

Org 9935 is a potent, selective PDE3 inhibitor with IC50 of 50 nM.

Enoximone sulfoxide is a selective phosphodiesterase III (PDE3) inhibitor with vasodilating and positive inotropic activity that does not cause changes in myocardial oxygen consumption. Enoximone prevents the degradation of cAMP by PDE, which prolongs signal transduction and its subsequent effects. It is used in patients with congestive heart failure.

Cilostamide (OPC3689) is a selective phosphodiesterase (PDE)3A and PDE3B inhibitor(IC50 values of 27 and 50 nM, respectively)

3-O-Methylquercetin is a selective and competitive PDE3 PDE4 inhibitor, and inhibits PDE3 than PDE4 with a low K(m) value; it inhibits total cAMP- and cGMP-phosphodiesterase (PDE) of guinea pig trachealis at low concentrations.

Thioquinapiperifil dihydrochloride is a phosphodiesterase (PDE-5) inhibitor (IC50: 0.074 nM) that is potent, selective and non-competitive for investigational maturation.

PDE3 inhibitor

Zardaverine (BY 290) is an orally available, selective and potent PDE3 4 inhibitor with bronchodilator activity and anti-hepatocarcinogenic activity.Zardaverine's action in platelets is mediated by PDE III isoenzymes and can be used in studies of acute renal failure and chronic airflow obstruction.

Quazinone is a selective inhibitor of phosphodiesterase 3 (PDE3) with positive inotropic and vasodilating properties. It induces relaxation of precontracted isolated human cavernous smooth muscle (IC50 = 4.2 μM), increases myocardial contractile force in anesthetized open-chest dogs in a dose-dependent manner (10-300 μg kg), decreases systolic and diastolic blood pressure, and inhibits DNA synthesis induced by the PDGF isoform PDGF-BB in bovine coronary artery smooth muscle cells in a concentration-dependent manner.

Parogrelil is a phosphodiesterase (PDE3/PDE5A) inhibitor potentially for the treatment of intermittent. Parogrelil suppress the asthmatic response in guinea pigs, with both bronchodilating and anti-inflammatory effects. Parogrelil improves reduced walking

(E Z)-Ensifentrine is a potent and selective PDE3 4 inhibitor that acts as a long-acting inhibitor of the phosphodiesterase enzymes PDE-3 and PDE-4, producing both bronchodilator and anti-inflammatory effects. It is being developed by Verona Pharma as a potential treatment for asthma and hay fever and is currently in clinical trials.

SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A); 1 nM (Aurora B / incenp); 3 nM (Aurora C / incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP 3A4 and PDE3 inhibition. In vitro, SAR156497 displayed high antiproliferative activity on a large panel of tumor cell lines without correlation with any particular genetic signature or Aurora kinases expression. It induced significant modulation of Aurora A and Aurora B biomarkers (p-Aurora A and pHH3, respectively) and cell polyploidy, as expected from Aurora A/B inhibitors.

Win-62005 is an inhibitor of cyclic AMP phosphodiesterase III (PDE III)(Kis: 25 and 26 nM for rat heart and canine aorta).

Motapizone (NAT 05-239) is a selective PDE3 inhibitor that moderately reduces cytokine release in lipopolysaccharide (LPS)-stimulated alveolar macrophages and suppresses human platelet aggregation by elevating intracellular cAMP levels [1] [2].

Olprinone Hydrochloride, also known as Loprinone, is a phosphodiesterase (PDE) 3 potent inhibitor, exhibiting IC50 values of 150, 100, 0.35, and 14 μM for PDE1, PDE2, PDE3, and PDE4, respectively. It is utilized in heart failure research for its positive inotropic and vasodilative properties. It also exhibits anti-inflammatory activity [1] [2].