PDE3
Phosphodiesterase 3 (PDE3) is a dual-substrate cyclic nucleotide phosphodiesterase that hydrolyzes both cAMP and cGMP and serves as a key regulator of intracellular cyclic nucleotide signaling pathways controlling cardiovascular and metabolic function[1][2]. PDE3-mediated regulation of cAMP signaling influences cardiac contractility, vascular smooth muscle tone, platelet activity, energy homeostasis, and insulin-responsive metabolic processes, thereby linking second-messenger turnover to diverse physiological responses[1][2][3]. Mechanistically, PDE3 enzymes display high affinity for both cyclic nucleotides but preferentially hydrolyze cAMP, while cGMP acts as a competitive inhibitor of cAMP degradation, creating functional cAMP-cGMP signaling crosstalk[1]. In disease-relevant systems, altered PDE3 signaling has been implicated in heart failure, ischemia-reperfusion injury, obesity-associated metabolic dysregulation, and abnormal insulin secretion, making PDE3 an important experimental target in cardiovascular and metabolic research[2][3][4]. Compared with related isoforms, PDE3A is predominantly associated with cardiac myocytes, vascular tissues, platelets, and reproductive function, whereas PDE3B is enriched in adipocytes, hepatocytes, pancreatic β-cells, and other metabolic tissues where it mediates insulin-, IGF-1-, and leptin-responsive signaling pathways[1][2][3]. This isoform-specific distribution underlies distinct biological functions and supports the use of selective genetic or pharmacological approaches to dissect cardiovascular versus metabolic mechanisms[2][3][4]. For experimental applications, PDE3 inhibitors are widely used to enhance cAMP signaling and investigate cardiac contractility, platelet aggregation, vascular relaxation, and metabolic regulation in cellular and animal models[1][2].
References:
- [1]. Murata T, et al. Phosphodiesterase 3 (PDE3): structure, localization and function. Cardiovasc Hematol Agents Med Chem. 2009 Jul;7(3):206-11. [Content Brief]
- [2]. Movsesian M, et al. Functions of PDE3 Isoforms in Cardiac Muscle. J Cardiovasc Dev Dis. 2018 Feb 6;5(1):10. [Content Brief]
- [3]. Degerman E, et al. From PDE3B to the regulation of energy homeostasis. Curr Opin Pharmacol. 2011 Dec;11(6):676-82. [Content Brief]
- [4]. Chung YW, et al. Targeted disruption of PDE3B, but not PDE3A, protects murine heart from ischemia/reperfusion injury. Proc Natl Acad Sci U S A. 2015 Apr 28;112(17):E2253-62. [Content Brief]
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PDE3 Related Products (93)
Related Products (93)
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PDE5-IN-15
0 ImagesCat. No.: HY-177298CAS No.: 366444-83-9PDE5-IN-15 (compound 21) is a xanthine derivative and PDE5 inhibitor, with IC50 values of 0.002, 0.180, 2.85 and 2.22 μM against hPDE5, bPDE6, bPDE1 and hPDE3, respectively. PDE5-IN-15 has good oral bioavailability in dogs. PDE5-IN-15 can be used in research on male erectile dysfunction.
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S-Petasin
0 ImagesCat. No.: HY-N17617CAS No.: 70238-51-6S-Petasin is a phosphodiesterase (PDE) inhibitor with IC50 values of 25.5 μM and 17.5 μM for PDE3 and PDE4, respectively. S-Petasin inhibits cholesterol side-chain cleavage enzyme, 11β-hydroxylase, PPAR-γ, and iNOS induction at RNA and protein levels. S-Petasin induces apoptosis, activates caspases, cleaves PARP, modulates mitochondrial membrane permeability, and regulates BCL2/BAX, p53, Bcl-XL, MMP-2, MMP-9, p21, CDK4, and cyclin D1 expression. S-Petasin reduces inflammatory cell accumulation, cytokine and IgE levels, and enhances serum IgG2a levels. S-Petasin relaxes isolated sensitized guinea pig trachealis and exhibits gastrointestinal anti-spasmodic activity. S-Petasin reduces tonsillitis severity and asthmatic attack frequency. S-Petasin can be used for the research of prostate cancer, obesity, melanoma, allergic asthma, asthma, and peritonitis.
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Lixazinone hydrogensulfate
0 ImagesCat. No.: HY-113822CAS No.: 101626-67-9Synonyms: RS-82856 hydrogensulfateLixazinone (RS-82856) hydrogensulfate is a selective inhibitor of cGMP-inhibited phosphodiesterase (PDE3) with an IC50 value of 22 nM. Lixazinone hydrogensulfate exhibits positive inotropic effects, afterload reduction and antithrombotic properties. Lixazinone hydrogensulfate increases cyclic adenosine monophosphate (cAMP) levels in human platelets, inhibits thrombin-induced aggregation of human platelets, and blocks the photolabeling of PDE3 active sites by [32P]cGMP. Lixazinone hydrogensulfate can be used in the research of polycystic kidney disease and congestive heart failure.
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Fenspiride
0 ImagesFenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
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PDE4D inhibitor 1
0 ImagesCat. No.: HY-173290PDE4-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.
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GSK4394835A
0 ImagesCat. No.: HY-179595CAS No.: 3032458-06-0GSK4394835A is a reversible covalent inhibitor of PDE3B with a pIC50 of 6.2. GSK4394835A can be used for cardiovascular disease research.
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Oberadilol
0 ImagesCat. No.: HY-19088CAS No.: 114856-44-9Synonyms: CID-3047798Oberadilol (CID-3047798) is a Phosphodiesterase III inhibitor, non-selective β-adrenergic receptor blocker, vasodilator and positive inotropic agent. Oberadilol reduces left ventricular end-diastolic volume. Oberadilol is used in research related to chronic congestive heart failure and SARS-CoV-2 infection.
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SLU-12091
0 ImagesCat. No.: HY-189060CAS No.: 3065124-09-3SLU-12091 is a phosphodiesterase (PDE) inhibitor and the more potent enantiomer of rac-11. SLU-12091 inhibits the activities of hPDE5, hPDE11, hPDE2A1, hPDE3A, hPDE3B, hPDE4A1A and hPDE4D2. SLU-12091 inhibits the growth of Cryptosporidium parvum without inhibiting the growth of host cells at the highest concentration tested. SLU-12091 can be used for the research of cryptosporidiosis.
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Olprinone hydrochloride hydrate
0 ImagesCat. No.: HY-14254BCAS No.: 2072803-95-1Synonyms: Loprinone hydrochloride hydrateOlprinone (Loprinone) hydrochloride hydrate is a potent and selective phosphodiesterase 3 (PDE3) inhibitor, with IC50 values of 150, 100, 0.35, and 14 μM against PDE1, PDE2, PDE3, and PDE4, respectively. Olprinone hydrochloride hydrate exerts comprehensive protective effects including anti-inflammatory, antioxidant, and anti-apoptotic activities by elevating intracellular cAMP levels and inhibiting the NF-κB and MAPK signaling pathways. Olprinone hydrochloride hydrate can be used in studies related to lung injury, spinal cord injury, heart failure, myocardial ischemia-reperfusion injury, and cerebral ischemic injury.
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Lixazinone
0 ImagesCat. No.: HY-105931CAS No.: 94192-59-3Synonyms: RS-82856Lixazinone (RS-82856) is a selective inhibitor of cGMP-inhibited phosphodiesterase (PDE3) with an IC50 value of 22 nM. Lixazinone exhibits positive inotropic effects, afterload reduction and antithrombotic properties. Lixazinone increases cyclic adenosine monophosphate (cAMP) levels in human platelets, inhibits thrombin-induced aggregation of human platelets, and blocks the photolabeling of PDE3 active sites by [32P]cGMP. Lixazinone can be used in the research of polycystic kidney disease and congestive heart failure.
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Theophylline sodium acetate
0 ImagesSynonyms: 1,3-Dimethylxanthine sodium acetate; Theo-24 sodium acetateTheophylline (1,3-Dimethylxanthine) sodium acetate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) sodium acetate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) sodium acetate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) sodium acetate induces apoptosis. Theophylline (1,3-Dimethylxanthine) sodium acetate can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
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PDE3/4-IN-2
0 ImagesPDE3/4-IN-2 is a dual PDE3A and PDE4B1 inhibitor, with an IC50 of 0.13 nM against PDE3A and 50 nM against PDE4B1. PDE3/4-IN-2 exhibits higher systemic exposure and longer retention time in lung tissues in ICR mice. PDE3/4-IN-2 can be used in research on respiratory diseases such as asthma and chronic obstructive pulmonary disease, as well as autoimmune inflammation-related studies.
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PDE3/4-IN-4
0 ImagesCat. No.: HY-181088CAS No.: 3088024-27-2PDE3/4-IN-4 is an orally active PDE3A and PDE4B inhibitor with IC50 values of 10 nM and 9.4 nM, respectively. PDE3/4-IN-4 shows selective activity relative to most other PDE family members. PDE3/4-IN-4 modulates the cAMP/PKA/CREB signaling pathway. PDE3/4-IN-4 inhibits pro-inflammatory factor IL-6. PDE3/4-IN-4 reduces expression of inflammatory markers in liver tissue. PDE3/4-IN-4 attenuates liver fibrosis. PDE3/4-IN-4 limits liver damage in cholestatic and sepsis-induced liver disease mice models. PDE3/4-IN-4 can be used for the research of liver injury, cholestatic liver diseases, sepsis-induced liver injury.
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TC-E 5005
0 ImagesCat. No.: HY-10568CAS No.: 959705-64-7TC-E 5005 is a potent and selective PDE10A inhibitor with IC50 values of 7.28, 239, 779, 919, 3,100, and 3,700 nM for PDE10A, 2A, 11A, 5A, 7B and 3A, respectively. TC-E 5005 inhibits adrenergic and neurogenic smooth muscle contractions in the human prostate.
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Tofisopam (Standard)
0 ImagesTofisopam (Standard) is the analytical standard of Tofisopam (HY-A0165). This product is intended for research and analytical applications. Tofisopam, a 2,3-benzodiazepine compound, is an orally active anxiolytic agent. Tofisopam can inhibit phosphodiesterase PDE isoenzyme activity, withIC50 values of 2.11 μM, 1.98 μM, 0.42 μM, and 0.92 μM for PDE-2A3, PDE-3A, PDE-4A1, and PDE-10A1, respectively. Tofisopam can be used for the study of anxiety.
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Antitumor agent-100
0 ImagesCat. No.: HY-153802CAS No.: 2841750-32-9Antitumor agent-100 is an orally active molecular glue that promotes the PDE3A-SLFN12 interaction and induces cell death. Antitumor agent-100 binds to the catalytic pocket of PDE3A, extends hydrophobic groups to mediate the hydrophobic interaction between PDE3A and SLFN12, and stabilizes the PDE3A-SLFN12 complex. Antitumor agent-100 induces cancer cell apoptosis and inhibits tumor growth in mouse xenograft models. Antitumor agent-100 can be used for the research of cervical cancer.
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PDE1-IN-4
0 ImagesCat. No.: HY-147946CAS No.: 3031349-98-8PDE1-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.
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Ensifentrine tosylate
0 ImagesCat. No.: HY-119708ACAS No.: 3098314-20-3Synonyms: RPL-554 tosylateEnsifentrine (RPL-554) tosylate is an inhaled dual inhibitor of PDE3 and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine tosylate blocks PDE3 and PDE4 enzymes, thereby increasing the levels of cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) in lung cells, dilating the bronchi, and inhibiting the activation and migration of inflammatory cells. Ensifentrine tosylate can be used in the research of chronic obstructive pulmonary disease (COPD).
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MS 857
0 ImagesCat. No.: HY-106804CAS No.: 107189-96-8MS 857 is an orally active nonglycoside and nonsympathomimetic cardiotonic agent. MS 857 exhibits cardiac and coronary vasodilator effect.
