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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Theophylline monohydrate
0 ImagesSynonyms: 1,3-Dimethylxanthine monohydrate; Theo-24 monohydrateTheophylline (1,3-Dimethylxanthine) monohydrate is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) monohydrate inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) monohydrate has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) monohydrate induces apoptosis. Theophylline (1,3-Dimethylxanthine) monohydrate can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
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OR-1896
0 ImagesOR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K+ channels and has Ca2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation.
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AGS-16C3F
0 ImagesCat. No.: HY-171544Purity: 99.81%Synonyms: AGS-16M8FAGS-16C3F is an antibody-drug conjugate (ADC) targeting ENPP3. AGS-16C3F is composed of ENPP3-targeting Anti-ENPP3/CD203c Antibody (HY-P990315) linked to Monomethyl auristatin F (HY-15579) via a linker. AGS-16C3F has anti-tumor activity and can be used in the study of metastatic renal cell carcinoma (mRCC).
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Morcamilast
0 ImagesSynonyms: ME3183; PDE4-IN-14Morcamilast (ME3183) is a potent, orally active, selective phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 1.28 nM, 2.33 nM and 1.63 nM against human PDE4A1A, PDE4B1 and PDE4D2, respectively. Morcamilast inhibits the production of TNF-α, IL-12/23p40, IL-23, IL-17A, IL-4, IL-5 and IL-13 in human PBMCs and T cells, and alleviates chronic Oxazolone (HY-126360)-induced dermatitis, Substance P (HY-P0201)-induced pruritus, Imiquimod (HY-B0180)-induced psoriasis-like dermatitis and LPS (HY-D1056)-induced arthritis. Morcamilast is used for the research of psoriasis, atopic dermatitis, psoriatic arthritis and other inflammatory and immune-related diseases.
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Vardenafil hydrochloride trihydrate
0 ImagesVardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].
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PDE3B-IN-1
0 ImagesPDE3B-IN-1 is a potent selective PDE3B inhibitor that demonstrates PDE3B inhibitory activity (pIC50 = 6.5) and >300-fold PDE3B/A selectivity.
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Tofisopam
0 ImagesTofisopam, 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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MBCQ
0 ImagesMBCQ 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.
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Olprinone Hydrochloride
0 ImagesSynonyms: Loprinone HydrochlorideOlprinone (Loprinone) Hydrochloride 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 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 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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Sp-cAMPS
0 ImagesCat. No.: HY-100530BCAS No.: 71774-13-5Sp-cAMPS, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS binds the PDE10 GAF domain with an EC50 of 40 μM.
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EMD 53998
0 ImagesEMD 53998 is a cardiotonic agent that increases myocardial contractility as an inhibitor for phosphodiesterase III (PDE III) and a calcium sensitizer. EMD 53998 increases myocardial contractility, reduces energy consumption and the risk of inducing arrhythmias.
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RS-25344 hydrochloride
0 ImagesRS-25344 hydrochloride is a selective cAMP-phosphodiesterase 4 (PDE 4; PDE IV) inhibitor with an IC50 of 0.28 nM in human lymphocytes. RS-25344 hydrochloride has only weak inhibitory effects on PDE I, II, III (IC50 of >100 μM, 160 μM, 330 μM, respectively). RS-25344 hydrochloride has anti-inflammatory, memory- and cognition enhancing, and antineoplastic effects.
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Motapizone
0 ImagesCat. No.: HY-106739CAS No.: 90697-57-7Synonyms: NAT 05-239Motapizone (NAT 05-239) is a selective PDE3 inhibitor. Motapizone moderately inhibits cytokine release in lipopolysaccharide (LPS)-induced alveolar macrophages. Motapizone also inhibits human platelet aggregation by increasing intracellular cAMP.
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Thioquinapiperifil dihydrochloride
0 ImagesSynonyms: KF31327Thioquinapiperifil dihydrochloride (KF31327), 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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T-0156
0 ImagesCat. No.: HY-105349CAS No.: 324572-93-2T-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.
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PF-04822163
0 ImagesCat. No.: HY-120741CAS No.: 1798334-07-2PF-04822163 is an orally active, selective, and blood-brain barrier permeable PDE1 inhibitor with IC50 values of 2 nM, 2.4 nM, and 7 nM for PDE1A, PDE1B, and PDE1C respectively. PF-04822163 can be used in the research of attention deficit hyperactivity disorder or Parkinson's disease.
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WIN-63291
0 ImagesCat. No.: HY-105418CAS No.: 144967-96-4WIN-63291 is a selective and orally active phosphodiesterase (PDE) III inhibitor. WIN-63291 can be used for the research of cardiovascular disease.
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Sp-cAMPS triethylamine
0 ImagesCat. No.: HY-110005CAS No.: 93602-66-5Sp-cAMPS triethylamine, a cAMP analog, is potent activator of cAMP-dependent PKA I and PKA II. Sp-cAMPS triethylamine is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS triethylamine binds the PDE10 GAF domain with an EC50 of 40 μM.
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Giclanfentrine
0 ImagesCat. No.: HY-171827CAS No.: 2408152-69-0Giclanfentrine is a potent PDE3A inhibitor with an IC50 of 0.0058 μM. Giclanfentrine inhibits PDE4B1 activity with an IC50 of 12.9 μM. Giclanfentrine is applicable to studies related to PDE3/cAMP signaling.
