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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Trequinsin
0 ImagesCat. No.: HY-18740CAS No.: 79855-88-2Synonyms: HL 725 free baseTrequinsin (HL 725 free base) is a PDE inhibitor, CatSper channel activator, and sperm potassium channel modulator. Trequinsin targets PDE3 with an IC50 of <1 nM. Trequinsin enhances currents and elevates intracellular calcium and cGMP levels via direct activation of the CatSper channel, while inhibiting the outward current conductance of sperm potassium channels. Without inducing premature acrosome reaction, Trequinsin significantly enhances sperm hyperactivated motility, forward motility, and the ability to penetrate viscous media. Trequinsin exerts age-specific positive inotropic and positive lusitropic effects on rabbit ventricular papillary muscles. Trequinsin has been used in studies on the mechanisms underlying male infertility (e.g., asthenozoospermia).
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OPC 33540
0 ImagesCat. No.: HY-112631CAS No.: 189362-27-4OPC-33540 is a highly selective and competitive PDE3 inhibitor with IC50 values of 0.32 nM (PDE3A) and 1.5 nM (PDE3B). OPC-33540 exhibits IC50s against PDE1, PDE2, PDE4, PDE5, and PDE7 of 42.9, 52.3, 100.8, 2.5, and 51.3 μM, respectively. OPC-33540 significantly enhances cAMP accumulation in platelets and effectively inhibits thrombin-induced platelet aggregation. OPC-33540 can be used in antithrombotic studies.
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Antitumor agent-100 hydrochloride
0 ImagesCat. No.: HY-153802ACAS No.: 2841750-53-4Antitumor agent-100 hydrochloride is an orally active molecular glue that promotes the PDE3A-SLFN12 interaction and induces cell death. Antitumor agent-100 hydrochloride 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 hydrochloride induces cancer cell apoptosis and inhibits tumor growth in mouse xenograft models. Antitumor agent-100 hydrochloride can be used for the research of cervical cancer.
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Meribendan
0 ImagesCat. No.: HY-106474CAS No.: 119322-27-9Meribendan is a phosphodiesterase (PDE)-III inhibitor.
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Thioquinapiperifil
0 ImagesCat. No.: HY-119611CAS No.: 220060-39-9Synonyms: KF31327 free baseThioquinapiperifil (KF31327 free base), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC50 of 0.074 nM) inhibitor, is used for sexual enhancement study.
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Theophylline L-lysine
0 ImagesCat. No.: HY-130054CAS No.: 83920-54-1Synonyms: Lysine theophyllinateTheophylline L-lysine (Lysine theophyllinate) is a soluble derivative of Theophylline (HY-B0809). Theophylline L-lysine is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline L-lysine inhibits PDE3 activity to relax airway smooth muscle. Theophylline L-lysine has anti-inflammatory activity by increasing IL-10 and inhibiting NF-κB into the nucleus. Theophylline L-lysine induces apoptosis. Theophylline L-lysine can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
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PDE3/4-IN-3
0 ImagesCat. No.: HY-176524SCAS No.: 2939748-69-1PDE3/4-IN-3 (Compound 7) is an orally active dual PDE3/4 inhibitor with IC50 s of 0.17 and ≤50 nM for PDE3A and PDE4B2, respectively. PDE3/4-IN-3 significantly inhibits methacholine-induced bronchoconstriction in guinea pigs. PDE3/4-IN-3 can be used for chronic obstructive pulmonary disease (COPD) and asthma research.
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Imazodan hydrochloride
0 ImagesCat. No.: HY-106045ACAS No.: 89198-09-4Synonyms: CI 914Imazodan hydrochloride is the hydrochloride form of Imazodan (HY-106045). Imazodan hydrochloride is a selective inhibitor for phosphodiesterase III (PDE III), which increases myocardial contractility by blocking the cAMP degradation, and improves the contractile function of heart. Imazodan hydrochloride serves also as a peripheral vasodilator.
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PDE5-IN-13
0 ImagesCat. No.: HY-170435PDE5-IN-13 (Compound 14b) inhibits phosphodiesterase 5 (PDE5A) with an IC50 of 3 nM. PDE5-IN-13 is a potential candidate for PAH (pulmonary arterial hypertension) research. PDE5-IN-13 has high selectivity for targets over PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11. PDE5-IN-13 is orally active.
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CK-2289
0 ImagesCat. No.: HY-115269CAS No.: 101183-99-7CK-2289 is an inhibitor of type III cyclic 3'5'-adenosine monophosphate phosphodiesterase (PDE). CK-2289 can inhibit platelet aggregation and decreases mean arterial blood pressure. CK-2289 can be used for the research of cardiovascular disease, such as congestive heart failure.
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MDL 19205
0 ImagesCat. No.: HY-105057CAS No.: 84490-12-0MDL 19205 is a cardiotonic agent with inotropic effect. MDL 19205 can be used for the research of cardiovascular disease, such as heart failure.
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Multitarget AD-IN-6
0 ImagesCat. No.: HY-181762Multitarget AD-IN-6 (Compound 39) is a multi-target inhibitor, with an IC50 of 15.54 μM against PDE4B, 15.15 μM against PDE7A, 8.39 μM against PDE3A, and a Kd of 37.7 μM against CHIT1. Multitarget AD-IN-6 acts as a TRPA1 antagonist, reduces the level of the NLRP3 inflammasome multiprotein complex to inhibit its activation, while inhibiting PDE4B, PDE7A and CHIT1, and decreasing the phosphorylation of NF-κB. Multitarget AD-IN-6 improves the pathology of elastase-induced emphysema in mice. Multitarget AD-IN-6 is applicable for the research of chronic obstructive pulmonary disease.
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AN-2898
0 ImagesCat. No.: HY-111167CAS No.: 906673-33-4AN-2898 is a selective PDE4 inhibitor with IC50 of 0.027 μM over other phosphodiesterase enzymes, such as PDE1A, PDE2A and PDE3A. AN-2898 also potently inhibits PDE4 subtypes (PDE4B1, PDE4A1A and PDE4D2). AN-2898 significantly inhibits the production of TNF-α, IL-2, IFN-γ, IL-5 and IL-10. AN-2898 can be used for mild to moderate atopic dermatitis (AD) and psoriasis research.
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PDE/TRPA1/CHIT1-IN-1
0 ImagesCat. No.: HY-179503PDE/TRPA1/CHIT1-IN-1 is a phosphodiesterases (PDEs), TRPA1, and hCHIT1 (KD of 37.7 μM) inhibitor. PDE/TRPA1/CHIT1-IN-1 is a broad-spectrum PDE inhibitor, potently targeting key isoforms including PDE4B, PDE7A, PDE3A, and PDE8A with IC50s of 15.54, 15.15, 8.39 and 16.46 μM. PDE/TRPA1/CHIT1-IN-1 suppresses NLRP3 inflammasome activation and inhibits NF-κB phosphorylation, downregulating the expression of pro-inflammatory genes (TNF-α and IL-6) in vivo. PDE/TRPA1/CHIT1-IN-1 can be used for chronic obstructive pulmonary disease (COPD) and related inflammatory lung disorders research.
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ORG-20241
0 ImagesCat. No.: HY-105520CAS No.: 145261-31-0ORG-20241 is a PDE3/PDE4 dual inhibitor. ORG-20241 has a significant bronchodilator effect and completely prevents allergen induced airway hyperresponsiveness. ORG-20241 can significantly inhibit eosinophil infiltration at high concentrations. ORG-20241 can be used for research on asthma.
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Anagrelide hydrochloride monohydrate
0 ImagesCat. No.: HY-B0523BCAS No.: 823178-43-4Anagrelide hydrochloride monohydrate is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide hydrochloride monohydrate, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide hydrochloride monohydrate inhibits bone marrow megakaryocytopoiesis. Anagrelide hydrochloride monohydrate decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide hydrochloride monohydrate is a platelet-lowering agent and plays in the antithrombopoietic action.
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GPR61 Inverse agonist 3
0 ImagesCat. No.: HY-182271GPR61 Inverse agonist 3 is a selective and brain-penetrant GPR61 inverse agonist with human IC50 of 4.0 nM, mouse IC50 of 8.8 nM, human Ki of 0.34 nM, mouse Ki of 1.1 nM. GPR61 Inverse agonist 3 disrupts GPR61-Gαs protein interactions to abolish GPR61 constitutive activity. GPR61 Inverse agonist 3 moderately inhibits GABAA chloride channel and PDE3A1 with IC50 values of 4.6 and 8.9 μM. GPR61 Inverse agonist 3 shows no functional effect on food intake in adult mice co-administered with a pan-CYP inhibitor. GPR61 Inverse agonist 3 can be used for the research of cachexia/sarcopenia.
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Benafentrine maleate
0 ImagesCat. No.: HY-W700638ACAS No.: 76166-55-7Synonyms: AH 21-132Benafentrine maleate is a phosphodiesterase 3 (PDE3) and phosphodiesterase 4 (PDE4) inhibitor with bronchodilator activity. Benafentrine maleate has IC50 values of 1.74 μM and 1.76 μM for guinea pig platelet PDE3 and neutrophil PDE4, respectively. Benafentrine maleate can be used in research related to obstructive airway diseases.
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LH17
0 ImagesCat. No.: HY-180803LH17, a Kaempferol (HY-14590) derivative, is a potent and selective PDE4 inhibitor (PDE4D2 IC50 = 73 nM, PDE4B2 IC50 = 190 nM). LH17 exhibits remarkable selectivity (>136-fold) against other PDE isoforms (PDE1B/2A/3A/5A/8A/9A/10A) (IC50 > 10000 nM), with the exception of PDE7A1 (IC50 = 300 nM). LH17 distinctly interacts with PDE4 M-pocket. LH17 demonstrates remarkable anti-fibrotic efficacy in both in vitro and in vivo models. LH17 can be used for idiopathic pulmonary fibrosis (IPF) research.
