PDE1

Phosphodiesterase PDE1 encodes Ca²⁺/calmodulin-regulated cyclic nucleotide phosphodiesterases that connect Ca²⁺ signaling with cAMP and cGMP degradation in the brain, heart, and vasculature^[1]. Mechanistically, Ca²⁺/calmodulin binding activates PDE1 by preventing an inhibitory domain from blocking the catalytic site, thereby controlling cyclic nucleotide signaling amplitude and compartmentation^[1]. In cardiovascular disease models, PDE1A is induced in activated cardiac myofibroblasts after Ang II or TGF-β stimulation and regulates extracellular matrix synthesis through cAMP-Epac-Rap1 and cGMP-PKG signaling^[2]. In human arterial smooth muscle cells, PDE1C is highly expressed in proliferating primary cultures and severe atherosclerotic lesions, but not in quiescent intact human aorta^[3]. Compared with related isoforms, human, monkey, and rat smooth muscle cells show different PDE1 patterns, with human cells expressing PDE1C, monkey cells expressing PDE1B, and rat cells expressing PDE1A^[3]. In sperm models, PDE1A localizes to the equatorial sperm head and flagellum, and mouse PDE1A_v7 is a major mature sperm PDE1A variant regulating cyclic nucleotide hydrolysis^[4]^[5]. For experimental applications, KS-505a selectively inhibits Ca²⁺/calmodulin-activated PDE1 isoenzymes and distinguishes subfamily members in brain-region models^[6].

References:

[1]. Nielsen J, et al. The Molecular Mechanism of PDE1 Regulation. Cells. 2025 Nov 1;14(21):1722. [Content Brief]

[2]. Miller CL, et al. Cyclic nucleotide phosphodiesterase 1A: a key regulator of cardiac fibroblast activation and extracellular matrix remodeling in the heart. Basic Res Cardiol. 2011 Nov;106(6):1023-39. [Content Brief]

[3]. Rybalkin SD, et al. Calmodulin-stimulated cyclic nucleotide phosphodiesterase (PDE1C) is induced in human arterial smooth muscle cells of the synthetic, proliferative phenotype. J Clin Invest. 1997 Nov 15;100(10):2611-21. [Content Brief]

[4]. Lefièvre L, et al. Presence of cyclic nucleotide phosphodiesterases PDE1A, existing as a stable complex with calmodulin, and PDE3A in human spermatozoa. Biol Reprod. 2002 Aug;67(2):423-30. [Content Brief]

[5]. Vasta V, et al. Identification of a new variant of PDE1A calmodulin-stimulated cyclic nucleotide phosphodiesterase expressed in mouse sperm. Biol Reprod. 2005 Oct;73(4):598-609. [Content Brief]

[6]. Ichimura M, et al. KS-505a, an isoform-selective inhibitor of calmodulin-dependent cyclic nucleotide phosphodiesterase. Biochem J. 1996 May 15;316 ( Pt 1)(Pt 1):311-6. [Content Brief]

Productos relacionados con PDE1 (56):

By Type:	Pan (35) Selective (14)
By Effects:	Inhibitors (55) Substrate (1)

Cat. No.	Nombre del producto	Efecto	Pureza

HY-114672

MBCQ	Inhibitor	99.80%
MBCQ 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.

HY-169402

PDE1-IN-9	Inhibitor
PDE1-IN-9 (Compound 7a) is a selective inhibitor for phosphodiesterase 1 (PDE1), that inhibits PDE1C with an IC₅₀ of 11 nM. PDE1-IN-9 reduces mRNA expression of IL-1β, IL-6, TNF-α and iNOS, inhibits the production of nitric oxide (NO) and reactive oxygen species (ROS). PDE1-IN-9 exhibits good metabolic stability in rat liver microsomes.

HY-101490

PDE1-IN-2	Inhibitor	98.0%
PDE1-IN-2 is a PDE1 inhibitor extracted from patent WO2016/55618 A1, example 31. PDE1-IN-2 has IC₅₀ values of 6 nM, 140 nM and 164 nM for PDE1C, PDE1B and PDE1A, respectvely. PDE1-IN-2 is developed for the research of neurodegenerative disorders and psychiatric disorders.

HY-169402A

PDE1-IN-9 hydrochloride	Inhibitor
PDE1-IN-9 (Compound 7a) hydrochloride is a selective inhibitor for phosphodiesterase 1 (PDE1), that inhibits PDE1C with an IC₅₀ of 11 nM. PDE1-IN-9 hydrochloride reduces mRNA expression of IL-1β, IL-6, TNF-α and iNOS, inhibits the production of nitric oxide (NO) and reactive oxygen species (ROS). PDE1-IN-9 hydrochloride exhibits good metabolic stability in rat liver microsomes.

HY-108621

RS-25344 hydrochloride	Inhibitor	99.93%
RS-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.

HY-119611A

Thioquinapiperifil dihydrochloride	Inhibitor	99.22%
Thioquinapiperifil dihydrochloride (KF31327), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC₅₀ of 0.074 nM) inhibitor, is used for sexual enhancement study.

HY-105349

T-0156	Inhibitor
T-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.

HY-12501

ITI-214 free base	Inhibitor	98.0%
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (K_i of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with K_is of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions.

HY-120741

PF-04822163	Inhibitor
PF-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.

HY-B0442C

Vardenafil dihydrochloride	Inhibitor
Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC₅₀ of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC₅₀s of 180 nM, and 11 nM respectively, while IC₅₀s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes^-.

HY-18252A

Avanafil dibenzenesulfonate	Inhibitor
Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC₅₀ values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis.

HY-116808B

TPN729MA	Inhibitor	99.45%
TPN729MA (TPN729 maleate) is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC₅₀ value of 2.28 nM. TPN729MA affects erectile function and it can be used for the research of erectile dysfunction.

HY-116808

TPN729	Inhibitor
TPN729 is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC₅₀ value of 2.28 nM. TPN729 affects erectile function and it can be used for the research of erectile dysfunction.

HY-112631

OPC 33540	Inhibitor
OPC-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.

HY-119611

Thioquinapiperifil	Inhibitor
Thioquinapiperifil (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.

HY-170435

PDE5-IN-13	Inhibitor
PDE5-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.

HY-14841

Gisadenafil	Inhibitor
Gisadenafil (UK-369003) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC₅₀ of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP).

HY-111167

AN-2898	Inhibitor
AN-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.

HY-103024

ICI-63197	Inhibitor	99.14%
ICI-63197 is a phosphodiesterase 3 (PDE3) and PDE4 inhibitor with K_i values of 9 µM and 10 µM, respectively. ICI-63197 is selectivity against PDE1 and PDE2. ICI-63197 has antidepressant effects.

HY-N6256

Ilexsaponin B2	Inhibitor
Ilexsaponin B2 is a saponin isolated from the root of Ilex pubescens Hook. et Arn. Ilexsaponin B2 is a potent phosphodiesterase 5 (PDE5) and PDEI inhibitor with IC₅₀ values of 48.8 μM and 477.5 μM, respectively.

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