Catalog No.
Product Name
Application
Product Information
Citations
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Phosphodiesterase (PDE) Control
Sildenafil chlorosulfonyl functions as a synthetic intermediate in the production of sildenafil, a selective phosphodiesterase 5 (PDE5) inhibitor. This compound plays a crucial role in the regulation of cGMP levels, presenting significant implications for research into erectile dysfunction and pulmonary arterial hypertension. Its application in various biochemical pathways makes it a valuable reagent for studies involving PDE inhibition and the modulation of nitric oxide signaling. -
PDE-5 Inhibitor
Aildenafil, also known as Methisosildenafil, is a potent inhibitor of phosphodiesterase type 5 (PDE-5), which facilitates vasodilation by elevating nitric oxide (NO) levels. This compound is primarily utilized in research exploring cardiovascular effects and conditions related to erectile dysfunction. Its ability to enhance blood flow through the modulation of cyclic guanosine monophosphate (cGMP) levels makes it a valuable tool for studying vascular physiology and pharmacology. -
PDE4 Inhibitor
PF-07038124 is a potent phosphodiesterase 4 (PDE4) inhibitor, exhibiting an IC50 of 0.5 nM for the PDE4B2 isoform. It demonstrates significant inhibitory activity against pro-inflammatory cytokines, including IL-13 (IC50 = 125 nM), IL-4 (IC50 = 4.1 nM), and IFN-γ (IC50 = 1.06 nM). This compound is valuable for research applications related to atopic dermatitis and plaque psoriasis, offering insights into therapeutic strategies for managing these inflammatory conditions. -
PDE4 Inhibitor
LASSBio-1632 is a selective phosphodiesterase 4 (PDE4) inhibitor, specifically targeting the PDE4A and PDE4D isoenzymes. This compound demonstrates significant anti-asthmatic properties by attenuating airway hyper-reactivity and inhibiting TNF-α production in lung tissue. Additionally, LASSBio-1632 exhibits high permeability across the blood-brain barrier, facilitating its potential use in various research applications related to respiratory conditions. -
PDE1 Inhibitor
PF-04822163 is a selective phosphodiesterase 1 (PDE1) inhibitor that effectively crosses the blood-brain barrier, exhibiting IC50 values of 2 nM for PDE1A, 2.4 nM for PDE1B, and 7 nM for PDE1C. This compound demonstrates significant potential for modulating intracellular signaling pathways, making it valuable in the study of neurological disorders such as attention deficit hyperactivity disorder and Parkinson's disease. Its potency and selectivity support its use in preclinical research efforts aimed at elucidating the role of PDE1 in these conditions. -
PDE5 Inhibitor
Vardenafil dihydrochloride is a selective inhibitor of phosphodiesterase-5 (PDE5), demonstrating a potent inhibitory effect with an IC50 of 0.7 nM. It also exhibits inhibition of PDE1 and PDE6 with IC50 values of 180 nM and 11 nM, respectively, while showing minimal activity against PDE3 and PDE4. By competitively inhibiting the hydrolysis of cyclic guanosine monophosphate (cGMP), Vardenafil dihydrochloride elevates cGMP levels, making it a valuable tool for studying conditions such as erectile dysfunction, hepatitis, and diabetes. -
PDE-5 Inhibitor
Avanafil dibenzenesulfonate is a selective phosphodiesterase-5 (PDE-5) inhibitor with a potent IC50 of 5.2 nM for PDE-5, demonstrating significant selectivity against other PDE isoforms. This compound activates the NO/cGMP/PKG signaling pathway, ultimately leading to reduced bone mineral density loss, alleviation of bone atrophy, and decreased oxidative stress. Avanafil dibenzenesulfonate is suitable for research applications related to erectile dysfunction and osteoporosis, where modulation of cGMP levels is crucial. -
TbrPDEB1 Inhibitor
NPD-1335 is an inhibitor of Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1), demonstrating submicromolar efficacy against T. brucei parasites. This compound enhances intracellular cAMP levels, leading to cell cycle disruption and apoptosis in the target cells. Additionally, NPD-1335 features an alkyne moiety, enabling its use as a click chemistry reagent for copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, thus expanding its utility in various research applications. -
PDE5 Inhibitor
TPN729MA is a selective phosphodiesterase type 5 (PDE5) inhibitor with an IC50 value of 2.28 nM. This compound plays a critical role in regulating erectile function and is suitable for research applications related to erectile dysfunction. Its potent inhibitory effect on PDE5 makes it a valuable tool for studying the underlying mechanisms of this condition. -
PDE5 Inhibitor
TPN729 is a selective inhibitor of phosphodiesterase type 5 (PDE5), exhibiting an IC50 value of 2.28 nM. This compound is primarily involved in modulating erectile function and serves as a valuable tool in the research of erectile dysfunction. Its high potency and specificity make it suitable for investigating PDE5's role in various physiological and pathological processes. -
PDE Inhibitor
Autotaxin-IN-4 is a potent inhibitor of autotaxin, targeting the enzyme responsible for lysophosphatidic acid production. This compound exhibits promising biological activity in the modulation of fibrosis processes, making it a candidate for research in conditions such as idiopathic pulmonary fibrosis. It serves as a valuable tool for studies aimed at understanding the role of autotaxin in fibrotic diseases and exploring therapeutic interventions. -
PDE Inhibitor
PDE1-IN-3 is a selective inhibitor of human phosphodiesterase 1 (PDE1), known for its potential to modulate intracellular cyclic nucleotide levels. This compound also demonstrates inhibitory activity against PDE4D and PDE6AB, with IC50 values of 23.99 μM and 10 μM, respectively. PDE1-IN-3 is suitable for research applications focused on cardiovascular diseases, neuroprotection, and other conditions where cyclic nucleotide signaling plays a critical role. -
PDE III Inhibitor
WIN-63291 is a selective and orally active phosphodiesterase III (PDE III) inhibitor. It effectively increases intracellular cyclic AMP levels, which plays a critical role in cardiovascular function. This compound is primarily utilized in research applications aimed at investigating cardiovascular diseases and their associated pathways. -
AR Antagonist/PDE5 Inhibitor
ID11916 is an orally active antagonist of the androgen receptor (AR) and a phosphodiesterase 5 (PDE5) inhibitor. It effectively inhibits androgen binding to AR, prevents nuclear translocation, and suppresses androgen-dependent transcriptional activity. Additionally, ID11916 elevates intracellular cGMP levels and activates protein kinase G (PKG) through its inhibitory effects. This compound demonstrates significant anti-cancer activity against prostate cancer cell lines VCaP and 22Rv1, as well as in AR-positive breast cancer cell lines such as SK-BR-3, making it a valuable tool for cancer research. -
PDE Inhibitor
Menabitan dihydrochloride is a selective inhibitor of phosphodiesterase 9 (PDE 9), demonstrating potential as a non-opioid analgesic agent. This compound has been shown to effectively reduce intraocular pressure in rabbit models, making it valuable for research in ocular health and pain management. Its specificity for PDE 9 positions it as an important tool for studies investigating the role of cyclic nucleotides in various physiological processes. -
PDE4 Inhibitor
Davalomilast is a selective phosphodiesterase 4 (PDE4) inhibitor known for its anti-inflammatory properties. This compound is of particular interest in research on autoimmune diseases and dermatological conditions, where it may modulate inflammatory responses and provide therapeutic insights. Its mechanism suggests potential applications in alleviating symptoms associated with various inflammatory disorders. -
PDE3 Inhibitor
OPC-33540 is a highly selective and competitive inhibitor of phosphodiesterase 3 (PDE3), exhibiting IC50 values of 0.32 nM for PDE3A and 1.5 nM for PDE3B. This compound demonstrates significantly reduced activity against other phosphodiesterases, with IC50 values ranging from 42.9 μM to 100.8 μM for PDE1, PDE2, PDE4, PDE5, and PDE7. OPC-33540 effectively increases cAMP levels in platelets and inhibits thrombin-induced platelet aggregation, making it a valuable tool for antithrombotic research applications. -
PDE 10 Inhibitor
Gemlapodect is a potent inhibitor of phosphodiesterase 10A (PDE10A). This compound has been shown to modulate intracellular signaling pathways and is primarily used in researching schizophrenia. Its ability to prevent the degradation of cyclic nucleotides makes it a valuable tool for studying neuropsychiatric disorders and potential therapeutic interventions. -
PDE11 Inhibitor
PDE11-IN-1 is a selective inhibitor of phosphodiesterase 11 (PDE11), a key enzyme involved in the regulation of cyclic nucleotide signaling. This compound plays a crucial role in adrenal insufficiency research by modulating intracellular cAMP and cGMP levels, which can impact adrenal hormone synthesis and secretion. PDE11-IN-1 is a valuable tool for investigating the physiological and pathophysiological processes associated with adrenal function and related disorders. -
PDE Inhibitor
5,7-Diacetoxy-8-methoxyflavone is a potent phosphodiesterase (PDE) inhibitor with a mechanism of action targeting cAMP metabolism. This compound exhibits significant biological activity by enhancing cAMP levels, thereby influencing various cellular processes. It is primarily utilized in research applications focused on cell signaling, inflammation, and potential therapeutic interventions related to PDE modulation. -
PDE Inhibitor
ER21355 hydrochloride is a potent phosphodiesterase (PDE) inhibitor that enhances levels of cyclic AMP (cAMP) and cyclic GMP (cGMP) within cells. This action facilitates the relaxation of smooth muscle cells, making it a valuable candidate for research into therapeutic strategies for benign prostatic hyperplasia (BPH) and related conditions. ER21355 hydrochloride provides a useful tool for studies focused on the modulation of smooth muscle relaxation and its implications in prostatic disorders. -
Phosphodiesterase (PDE)
Nor-Acetildenafil is a derivative of Acetildenafil and functions as a phosphodiesterase (PDE) inhibitor. This compound demonstrates biological activity that may enhance blood flow by promoting vasodilation. It is used in research applications focused on cardiovascular health and erectile dysfunction therapies, providing insights into mechanisms of action of PDE inhibitors. -
PDE-III Inhibitor
Meribendan is a potent phosphodiesterase III (PDE-III) inhibitor. It enhances intracellular cyclic adenosine monophosphate (cAMP) levels, promoting cardiac contractility and vasodilation. This compound is primarily used in cardiovascular research, providing insights into heart failure mechanisms and potential therapeutic strategies. -
PDE8B Inhibitor
PDE8B-IN-1 hydrochloride is a potent and selective inhibitor of phosphodiesterase type 8B (PDE8B) with an IC50 value of 1.5 nM. This compound is valuable for research focused on the modulation of intracellular cAMP levels, which is relevant in the study of diabetes and related metabolic disorders. PDE8B-IN-1 hydrochloride provides a useful tool for investigating the role of PDE8B in cellular signaling pathways and potential therapeutic strategies. -
PDE5 Inhibitor
Thioquinapiperifil is a potent, selective, and non-competitive inhibitor of phosphodiesterase-5 (PDE-5), with an IC50 of 0.074 nM. This compound is primarily utilized in research focusing on sexual enhancement and the modulation of erectile function. Its high specificity and efficacy make it a valuable tool for investigating PDE5-related pathways and potential therapeutic applications in sexual health. -
PDEδ Inhibitor
Deltazinone 1 is a selective phosphodiesterase δ (PDEδ) inhibitor with a KD value of 8 nM, targeting the PDEδ-Ras interaction. It demonstrates a dose-dependent inhibitory effect on the proliferation of oncogenic KRas-dependent cell lines, making it a valuable compound for studying KRas signaling pathways and potential therapeutic interventions in cancer research. -
PDE4 Inhibitor
PDE4-IN-34 is a selective phosphodiesterase 4 (PDE4) inhibitor, demonstrating IC50 values of 19 pM and 14 pM for PDE4B1 and PDE4D2, respectively. This compound shows weak inhibitory activity against PDE8A1 (IC50 of 4.092 μM) and exhibits significant selectivity over other PDE subtypes (IC50 > 10 μM). PDE4-IN-34 effectively improves pulmonary function, reduces inflammatory responses, and mitigates lung tissue damage in rat models of chronic obstructive pulmonary disease induced by cigarette smoke and LPS. It serves as a valuable tool for research into PDE4-related pathways in pulmonary disorders. -
PDE11A4 Inhibitor
PDE11A4-IN-1 is a selective inhibitor of the phosphodiesterase 11A4 (PDE11A4) enzyme, exhibiting an IC50 of 12 nM. This compound demonstrates strong selectivity for PDE11A4 compared to other phosphodiesterases including PDE1, PDE2, PDE7, PDE8, and PDE9. It is suitable for studies investigating the role of PDE11A4 in various biological processes and potential therapeutic applications in conditions influenced by cyclic nucleotide signaling. -
PDE3/4 Inhibitor
PDE3/4-IN-3 is a potent dual inhibitor of phosphodiesterase 3 and 4, exhibiting IC50 values of 0.17 nM for PDE3A and ≤50 nM for PDE4B2. This compound effectively reduces methacholine-induced bronchoconstriction in guinea pigs, demonstrating its potential in respiratory research. PDE3/4-IN-3 is valuable for investigating therapeutic strategies in chronic obstructive pulmonary disease (COPD) and asthma. -
Phosphodiesterase (PDE) Inhibitor
RA642 is a selective phosphodiesterase (PDE) inhibitor that enhances arterial blood pressure and promotes vasodilation. This compound demonstrates significant biological activity by improving cerebral blood flow and reducing both cerebrovascular and peripheral resistance. It exhibits a relaxant effect on smooth muscle, akin to that of papaverine, making it a valuable tool for studying cardiovascular dynamics and smooth muscle physiology in research settings. -
Phosphodiesterase (PDE) Inhibitor
ATX inhibitor 7 is a selective inhibitor of autotaxin, a lysophospholipase that catalyzes the production of lysophosphatidic acid (LPA) from lysophosphatidylcholine. This compound demonstrates significant oral bioavailability, making it a valuable tool for investigations into the role of LPA signaling in various physiological and pathological processes. ATX inhibitor 7 is suitable for research applications related to cancer, fibrosis, and neurodegenerative diseases, where modulation of autotaxin activity may offer therapeutic benefits. -
PDE5 Inhibitor
T-1032 free base is a highly selective phosphodiesterase 5 (PDE5) inhibitor, exhibiting an IC50 value of 1.0 nM. It demonstrates a significant relaxant effect on isolated rabbit corpus cavernosum. T-1032 free base is primarily utilized in research focused on erectile dysfunction and related vascular disorders. -
PDE Inhibitor
Imazodan hydrochloride is a selective phosphodiesterase III (PDE III) inhibitor that enhances myocardial contractility by preventing the degradation of cyclic adenosine monophosphate (cAMP). This compound improves cardiac contractile function and serves as a peripheral vasodilator. Imazodan hydrochloride is relevant for research applications involving cardiovascular conditions and the modulation of heart function. -
PDE Inhibitor
Isopedicin is a potent phosphodiesterase (PDE) inhibitor that effectively reduces superoxide anion (O2•-) production in formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP)-activated cells. By inhibiting PDE activity, Isopedicin enhances cyclic AMP (cAMP) formation and promotes protein kinase A (PKA) activity, thereby influencing various intracellular signaling pathways. This compound is suitable for research applications investigating oxidative stress and signaling mechanisms in immune responses. -
PDE2A Inhibitor
PDE2A-IN-2 is a selective inhibitor of phosphodiesterase type 2A (PDE2A) with a Ki value of 5.49 nM, demonstrating over 100-fold selectivity against other PDE isoforms. This compound serves as a radiolabeled PET tracer, facilitating brain imaging in patients with neurodegenerative diseases by eliciting a signal specifically in PDE2A-rich regions. Its application in neurodegenerative disease research highlights its potential in studying PDE2A's role in pathophysiology. -
PDE5 Inhibitor
(R)-Xanthoanthrafil is a selective phosphodiesterase-5 (PDE5) inhibitor. By increasing cyclic guanosine monophosphate (cGMP) levels, it promotes smooth muscle relaxation, facilitating penile erection. This compound is valuable for research applications related to erectile dysfunction and the physiological mechanisms governing this condition. -
PDE4 Inhibitor
Z21090 is a selective inhibitor of phosphodiesterase-4 (PDE4), exhibiting an IC50 value of 37.4 nM and demonstrating oral bioavailability. This compound is significant for studies related to alcohol-related diseases and offers potential therapeutic insights into inflammatory processes and neurodegenerative conditions associated with PDE4 activity. Researchers may utilize Z21090 to explore its effects on cyclic AMP signaling pathways and related biological mechanisms. -
PDE4 Inhibitor
LT-104A is a selective phosphodiesterase 4 (PDE4) inhibitor that effectively elevates intracellular cyclic AMP (cAMP) levels, exhibiting an EC50 of 1.9 μM and inhibiting PDE4D3 activity with an IC50 of 9.3 μM. By activating the cAMP-PKA-CREB anti-inflammatory signaling pathway, LT-104A suppresses expression of NF-κB-related genes such as Il1b and Nos2. This compound is valuable for research focused on inflammation-related diseases and therapeutic interventions aimed at modulating inflammatory responses. -
Phosphodiesterase (PDE)
JNJ-42259152 is a selective phosphodiesterase 10A (PDE10A) positron emission tomography (PET) tracer designed to assess PDE10A activity in vivo. This compound demonstrates reliable binding potential across critical brain regions, including the lentiform nucleus, caudate nucleus, and ventral striatum, making it a valuable tool in the exploration of neuropsychiatric disorders. With an average blood half-life of 90 minutes, JNJ-42259152 enables detailed kinetic analysis in healthy subjects, supporting research into the underlying mechanisms of various central nervous system conditions. -
PDE Inhibitor
Menabitan is a selective inhibitor of phosphodiesterase 9 (PDE 9), exhibiting non-opioid analgesic properties. This compound has demonstrated efficacy in lowering intraocular pressure in rabbit models, making it a valuable tool for research in ophthalmology and pain management. Its inhibition of PDE 9 underlines its potential in developing therapeutic strategies for conditions associated with elevated intraocular pressure. -
PDE5 Inhibitor
BMS-341400 is a potent, orally active selective phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 0.3 nM. By inhibiting PDE5, BMS-341400 effectively prevents the breakdown of cyclic guanosine monophosphate (cGMP), facilitating nitric oxide (NO)-induced smooth muscle relaxation in the corpus cavernosum, which promotes erectile function. This compound is primarily utilized in the study of erectile dysfunction and related pathways in sexual health research. -
PDE III Inhibitor
CK-2289 is a selective inhibitor of type III cyclic 3',5'-adenosine monophosphate phosphodiesterase (PDE III). This compound demonstrates significant efficacy in inhibiting platelet aggregation and lowering mean arterial blood pressure, making it a valuable tool in cardiovascular research. CK-2289 is particularly relevant for studies focused on cardiovascular diseases, including congestive heart failure. -
Ligand of PDEδ
PDEδ-IN-1 is a selective ligand of phosphodiesterase delta (PDEδ), primarily involved in regulating intracellular signaling pathways. This compound is utilized in research focused on PDEδ-related cellular processes and can be employed to synthesize PDEδ autophagic degrader 1. Its ability to modulate PDEδ function makes it a valuable tool for elucidating the role of this enzyme in various biological contexts. -
Phosphodiesterase (PDE) Inhibitor
Parogrelil hydrochloride is a selective phosphodiesterase (PDE) inhibitor, primarily targeting PDE3. It demonstrates significant biological activity by inhibiting human platelet aggregation in vitro and reducing aortic contraction in rat models. Research indicates that Parogrelil hydrochloride effectively improves walking distance and increases plantar surface temperature in the rat femoral artery ligation model, exhibiting superior efficacy compared to cilostazol. This compound is valuable for studies focused on cardiovascular health and peripheral artery disease. -
PDE10A Tracer
AMG-7980 is a selective phosphodiesterase 10A (PDE10A) tracer with a high affinity characterized by a KD of 0.94 nM. When labeled with a radioactive isotope, AMG-7980 serves as a valuable tool for in vivo imaging studies and pharmacological research involving PDE10A. Its precise targeting makes it suitable for investigating the role of PDE10A in various neurological and psychiatric disorders. -
PDE6δ-KRas Inhibitor
Deltasonamide 1 TFA is a potent inhibitor of the PDE6δ-KRas interaction, exhibiting a binding affinity with a KD of 203 pM. This compound is valuable in research focused on cancer biology, particularly in the study of tumor progression and metastasis. Its ability to disrupt the PDE6δ-KRas axis makes it a useful tool for investigating the underlying mechanisms of KRas-driven malignancies. -
PDE5A Inhibitor
PF-03049423 free base is a selective inhibitor of phosphodiesterase-5A (PDE5A), exhibiting an IC50 of approximately 0.2 nM in both rat and human platelet enzymes. This compound demonstrates significant potential for research applications focused on acute ischemic stroke, where modulation of PDE5A activity may impact downstream signaling pathways and cellular responses. Researchers can utilize PF-03049423 to explore its effects on vascular function and neuroprotection in ischemic conditions. -
PDE4 Inhibitor
PDE4-IN-12 is a potent pan-PDE4 inhibitor that demonstrates IC50 values of 3.5 nM for PDE4 and 15 nM for PDE7, with selectivity indices of 2.71 and 4.27, respectively. This compound is well-tolerated and is suitable for research applications in the study of inflammatory bowel diseases (IBDs) and related inflammatory conditions. Its strong inhibitory activity on phosphodiesterase enzymes makes it a valuable tool for investigating therapeutic strategies in inflammatory disorders. -
Phosphodiesterase (PDE) Inhibitor
Reproterol hydrochloride is a selective phosphodiesterase (PDE) inhibitor that also acts as a dual-acting beta2-adrenoceptor agonist. It effectively stimulates cyclic AMP (cAMP) production in human monocytes, demonstrating potential for enhanced airway function. Additionally, Reproterol hydrochloride exhibits significant inhibition of leukotriene B4 (LTB4) production, suggesting anti-inflammatory properties that may be beneficial in treating respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD). -
PDE V Inhibitor
FR-229934 is a phosphodiesterase type V (PDE V) inhibitor that demonstrates potential therapeutic effects in the treatment of pulmonary arterial hypertension and erectile dysfunction. By inhibiting PDE V, FR-229934 increases intracellular cAMP levels, leading to vasodilation and improved blood flow. This compound is valuable for research applications focused on cardiovascular diseases and sexual health disorders.
