PDE2
Phosphodiesterase 2A (PDE2A) is a dual-substrate cyclic nucleotide phosphodiesterase that hydrolyzes both cAMP and cGMP and functions as a key regulator of intracellular cyclic nucleotide signaling networks.[1] A defining feature of PDE2A is its allosteric activation by cGMP through the GAF-B regulatory domain, which enhances catalytic activity and enables bidirectional crosstalk between cGMP and cAMP signaling pathways.[2][3] Through this mechanism, PDE2A influences diverse biological processes including synaptic plasticity, neuronal signaling, mitochondrial function, cardiac remodeling, and cellular stress responses.[3][4][5] Mechanistically, PDE2A controls localized cyclic nucleotide microdomains and thereby regulates downstream protein kinase signaling pathways that govern cellular adaptation and homeostasis.[3][5] In disease-related experimental models, altered PDE2A activity has been associated with heart failure, pulmonary hypertension, neurodegenerative disorders, and cognitive dysfunction, highlighting its importance in pathological cyclic nucleotide signaling.[6][7][8] Inhibition of PDE2 enhances neuronal cGMP signaling, promotes synaptic plasticity, and improves memory performance in preclinical studies. Compared with related phosphodiesterase families, PDE2A is unique because cGMP stimulates rather than inhibits its catalytic activity, allowing it to function as a central mediator of cAMP-cGMP signaling integration.[2][3] The PDE2A gene generates multiple isoforms, including PDE2A1, PDE2A2, and PDE2A3, which differ primarily in their N-terminal targeting sequences and subcellular localization rather than catalytic properties.[2][4] Notably, PDE2A2 localizes to mitochondria and regulates mitochondrial respiration, morphology, and mitophagy, distinguishing it from other PDE2A isoforms.[4][5] For experimental applications, selective PDE2 inhibitors such as BAY 60-7550 are widely used to investigate cyclic nucleotide compartmentalization, neuroplasticity, cardiovascular signaling, and mitochondrial regulatory mechanisms.[7]
References:
- [1]. Uniprotkb.
- [2]. Sciencedirect.topics.
- [3]. Zaccolo M, et al. cAMP and cGMP signaling cross-talk: role of phosphodiesterases and implications for cardiac pathophysiology. Circ Res. 2007;100(11):1569-1578.
- [4]. Acin-Perez R, et al. A phosphodiesterase 2A isoform localized to mitochondria regulates respiration[J]. Journal of Biological Chemistry, 2011, 286(35): 30423-30432.
- [5]. Baliga RS, et al. Phosphodiesterase 2 inhibition preferentially promotes NO/guanylyl cyclase/cGMP signaling to reverse the development of heart failure. Proc Natl Acad Sci U S A. 2018 Jul 31;115(31):E7428-E7437. [Content Brief]
- [6]. Bubb KJ, et al. Inhibition of phosphodiesterase 2 augments cGMP and cAMP signaling to ameliorate pulmonary hypertension. Circulation. 2014 Aug 5;130(6):496-507. [Content Brief]
- [7]. Ruan L, et al. Phosphodiesterase-2 Inhibitor Bay 60-7550 Ameliorates Aβ-Induced Cognitive and Memory Impairment via Regulation of the HPA Axis. Front Cell Neurosci. 2019 Oct 2;13:432. [Content Brief]
All Product Categories
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PDE2 Related Products (51)
Related Products (51)
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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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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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Girisopam
0 ImagesCat. No.: HY-187129CAS No.: 82230-53-3Girisopam is a PDE inhibitor with IC50 values of 3.2, 4.0, and 12.5 μM against PDE4, PDE2, and PDE5, respectively. Girisopam exhibits anxiolytic, antidepressant, anti-aggressive, and antipsychotic activities. The binding sites of Girisopam are enriched exclusively in the basal ganglia of rat brains, and depletion of these sites is associated with damage to the striatonigral pathway. Girisopam enhances the potency of μ-opioid receptor agonists, attenuates the antagonistic effect of low-dose Naloxone (HY-17417A), and synergistically potentiates the anti-fighting effect of Chlorpromazine (HY-12708). Girisopam can be used in studies related to psychiatric disorders such as anxiety and depression.
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BML-288
0 ImagesCat. No.: HY-114023CAS No.: 851681-89-5BML-288 (compound Oxindole 1) is a potent PDE2 inhibitor with an IC50 value of 40 nM. BML-288 has the potential for the research of osteoarthritis pain.
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Olprinone Hydrochloride (Standard)
0 ImagesSynonyms: Loprinone Hydrochloride (Standard)Olprinone (Loprinone) Hydrochloride Standard is the analytical standard of Olprinone (Hydrochloride) (HY-14254). This product is intended for research and analytical applications. Olprinone (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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PF-06815189
0 ImagesCat. No.: HY-124173CAS No.: 2218484-75-2PF-06815189 is a phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 0.4 nM.
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Olprinone (Standard)
0 ImagesCat. No.: HY-14254ARCAS No.: 106730-54-5Synonyms: Loprinone (Standard)Olprinone (Loprinone) Standard is the analytical standard of Olprinone (HY-14254A). This product is intended for research and analytical applications. Olprinone (Loprinone) 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 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 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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JNJ-10258859
0 ImagesCat. No.: HY-123145CAS No.: 374927-03-4JNJ-10258859 is a potent and selective phosphodiesterase type 5 inhibitor, with a Ki of 0.23 nM. JNJ-10258859 can be used for erectile dysfunction research.
