PDE7
PDE7 is a cAMP-specific phosphodiesterase family that terminates biological functions of cAMP, a major intracellular regulator[1]. Mechanistically, cAMP affects cell functions through the canonical PKA pathway and non-canonical EPAC pathway, placing PDE7 within cAMP-dependent signaling control[1]. In immune biology, PDE7 is present in many immune cells, including T lymphocytes, and both PDE7A and PDE7B are expressed in T cells, where PDE7A1 is the predominant splice variant[1]. Disease-oriented studies therefore use PDE7 to examine T-cell activity, inflammation, and neurodegenerative models, including dopaminergic neuron injury[2][3]. Compared with related isoforms, PDE7 is distinguished from PDE4 by rolipram insensitivity, while PDE7A-deficient mice retain T-cell proliferation and Th1/Th2 cytokine production after CD3/CD28 costimulation[1][4]. For experimental applications, BRL 50481 competitively inhibits human recombinant PDE7A1 with a Ki of 180 nM and shows acceptable selectivity for in vitro studies in monocytes, lung macrophages, and CD8+ T lymphocytes[5]. PDE7 inhibitors also protect dopaminergic neurons against different insults, supporting their use in Parkinson disease-related experimental designs[3].
References:
- [1]. Szczypka M. Role of Phosphodiesterase 7 (PDE7) in T Cell Activity. Effects of Selective PDE7 Inhibitors and Dual PDE4/7 Inhibitors on T Cell Functions. Int J Mol Sci. 2020 Aug 25;21(17):6118. doi: 10.3390/ijms21176118. PMID: 32854348; PMCID: PMC7504236. et al. Role of Phosphodiesterase 7 (PDE7) in T Cell Activity. Effects of Selective PDE7 Inhibitors and Dual PDE4/7 Inhibitors on T Cell Functions. Int J Mol Sci. 2020 Aug 25;21(17):6118. [Content Brief]
- [2]. Zorn A, et al. Phosphodiesterase 7 as a therapeutic target - Where are we now? Cell Signal. 2023 Aug;108:110689. [Content Brief]
- [3]. Morales-Garcia JA, et al. Phosphodiesterase 7 inhibition preserves dopaminergic neurons in cellular and rodent models of Parkinson disease. PLoS One. 2011 Feb 24;6(2):e17240. [Content Brief]
- [4]. Yang G, et al. Phosphodiesterase 7A-deficient mice have functional T cells. J Immunol. 2003 Dec 15;171(12):6414-20. [Content Brief]
- [5]. Smith SJ, et al. Discovery of BRL 50481 [3-(N,N-dimethylsulfonamido)-4-methyl-nitrobenzene], a selective inhibitor of phosphodiesterase 7: in vitro studies in human monocytes, lung macrophages, and CD8+ T-lymphocytes. Mol Pharmacol. 2004 Dec;66(6):1679-89. [Content Brief]
All Product Categories
-
PDE7 Related Products (28)
Related Products (28)
- 1
- 2
-
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.
-
PDE4B/7A-IN-1
0 ImagesPDE4B/7A-IN-1 is a dual PDE4B/PDE7A inhibitor. PDE4B/7A-IN-1 shows IC50 values of 69.0 μM for PDE4B and 57.0 μM for PDE7A, as well as Ki values of 539 nM for 5-HT1A and 328 nM for 5-HT7. PDE4B/7A-IN-1 shows favorable membrane permeability. PDE4B/7A-IN-1 can be used for the study of cognitive impairment and depression.
-
PDE4B/7A-IN-2
0 ImagesCat. No.: HY-146202CAS No.: 2511632-55-45-HT1A/5-HT7 receptor antagonist (5-HT1A Ki = 8 nM, Kb = 0.04 nM; 5-HT7 Ki = 451 nM, Kb = 460 nM) with PDE4B/PDE7A inhibitory activity (PDE4B IC50 = 80.4 μM; PDE7A IC50 = 151.3 μM) , its antidepressant like effect is stronger than that of escitalopram as a reference agent.
-
BC-54
0 ImagesCat. No.: HY-124635CAS No.: 534579-04-9
-
P7-2104
0 ImagesP7-2104 is a blood-brain barrier-permeable, selective PDE7A inhibitor with an IC50 of 31 nM. P7-2104 shows selectivity for hERG channels and most CYP450 subtypes. P7-2104 can be used for PDE7-targeted PET neuroimaging studies and research related to neurodegenerative diseases, when labeled with 11C or 18F.
-
BC12
0 ImagesCat. No.: HY-119514CAS No.: 423744-89-2BC12 is a barbituric acid derivative and a phosphodiesterase 7 (PDE7) inhibitor, with an IC50 of 0.77 μM against human targets. BC12 inhibits the enzymatic activity of PDE7, but this activity is not the driver of its immunomodulatory effects on T lymphocytes. BC12 blocks the upregulation of IL-2 transcription in activated T cells. BC12 modulates the transcriptional response of T cells upon stimulation, exerting anti-inflammatory and pro-stress effects. BC12 inhibits the proliferation of primary mouse T cells and the IL-2 secretion of human peripheral blood T lymphocytes. BC12 exerts immunosuppressive and immunomodulatory effects on T lymphocyte function. BC12 can be used in research related to T lymphocyte-mediated diseases.
-
ASB16165
0 ImagesCat. No.: HY-165553CAS No.: 873541-45-8ASB16165 is a selective and potent PDE7A inhibitor with an IC50 of 15 nM against human PDE7A. ASB16165 inhibits IL-12-induced IFN-γ production via a cAMP/PKA-dependent mechanism, reduces cutaneous TNF-α production, and suppresses keratinocyte proliferation. ASB16165 can be used in research on skin diseases such as psoriasis.
- 1
- 2
