Catalog No.
Product Name
Application
Product Information
Citations
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COMT Inhibitor
Nitecapone is an orally active and short-acting catechol-O-methyltransferase (COMT) inhibitor. It exhibits notable gastroprotective and antioxidant properties by scavenging reactive oxygen and nitrogen species, thereby preventing lipid peroxidation. Nitecapone is valuable in research applications focusing on neurodegenerative diseases and other conditions where COMT modulation may play a therapeutic role. -
COMT
3-O-Methyldopa monohydrate is a notable metabolite of L-DOPA, primarily interacting with catechol O-methyltransferase (COMT). It does not function as a substrate or inhibitor of L-amino acid decarboxylase, distinguishing it from its precursor. The inhibition of COMT by this compound may enhance the therapeutic effects of L-DOPA in Parkinson's disease, making it a valuable tool in neurological research and studies on Parkinson's treatments. -
hMAO-B/MB-COMT Inhibitor
hMAO-B/MB-COMT-IN-1 is a dual inhibitor of human monoamine oxidase B (hMAO-B) and membrane-bound catechol-O-methyltransferase (MB-COMT), exhibiting IC50 values of 2.5 µM and 3.84 µM, respectively. This compound is effective in protecting cells from oxidative damage, making it a valuable tool for studying neurodegenerative diseases, including Parkinson's Disease. Its dual inhibition profile provides insights into the molecular mechanisms underlying these conditions and aids in the development of potential therapeutic strategies. -
COMT Inhibitor
S-Adenosylhomocysteine sulfoxide is a potent inhibitor of catechol-O-methyltransferase (COMT) with an IC50 value of 860 μM. This compound is utilized in research to investigate the modulation of methylation reactions, providing valuable insights into biochemical pathways involving methyltransferases. Its inhibitory properties make it a significant tool for studies related to neurotransmitter metabolism and epigenetic regulation. -
Stable Isotope
Entacapone-d10 is a deuterium-labeled version of Entacapone, a potent, reversible inhibitor of catechol-O-methyltransferase (COMT). This compound selectively inhibits COMT with IC50 values of 10 nM in rat brain, 20 nM in erythrocytes, and 160 nM in liver, demonstrating minimal interaction with other catecholamine metabolizing enzymes. Entacapone-d10 is utilized primarily in research related to Parkinson's disease and metabolic disorders, serving as an FTO demethylation inhibitor with an IC50 of 3.5 μM. -
COMT Inhibitor
U-0521 is a selective inhibitor of catechol-O-methyltransferase (COMT), an enzyme involved in the metabolism of catecholamines. This compound exhibits significant biological activity by modulating neurotransmitter levels, which is crucial for investigations into Parkinson's disease and related disorders. U-0521 is valuable for research focused on understanding the role of COMT in neurodegenerative conditions and for exploring potential therapeutic strategies targeting this pathway. -
COMT Inhibitor
(Z)-Entacapone is a selective inhibitor of catechol-O-methyltransferase (COMT), crucial for catecholamine metabolism. This compound serves as a valuable tool in studying COMT's role in neurological disorders and drug metabolism. Additionally, it may appear as a potential impurity in commercial Entacapone preparations or as a degradation product due to UV light exposure, providing further relevance in quality control and biological research applications. -
Hydroxycinnamic Acid
(E)-5-Hydroxyferulic acid is an isomer of the hydroxycinnamic acid class, functioning as a key intermediate in the phenylpropanoid pathway. It plays a crucial role as a precursor in the biosynthesis of sinapic acid and serves as a non-esterified substrate for catechol-O-methyltransferase (COMT). This compound is important for studying metabolic pathways and the functions of phenolic compounds in various biological systems. -
hMAO-B/MB-COMT Inhibitor
hMAO-B/MB-COMT-IN-2 is a potent dual inhibitor of hMAO-B and MB-COMT, exhibiting IC50 values of 4.27 μM and 2.69 μM, respectively. This compound effectively protects cells from oxidative damage, making it valuable for studies related to neurodegenerative diseases. hMAO-B/MB-COMT-IN-2 is particularly relevant in the research of conditions such as Parkinson’s Disease, offering insights into potential therapeutic strategies. -
COMT Inhibitor
COMT-IN-1 is a potent catechol-O-methyltransferase (COMT) inhibitor, demonstrating an IC50 of 0.37 μM for COMT activity. This nitrophenolic analogue effectively inhibits monoamine oxidase A (MAO-A) and MAO-B with IC50 values of 95.58 μM and 58.82 μM, respectively. With good blood-brain barrier permeability, COMT-IN-1 enhances dopamine levels and alleviates symptoms associated with MPTP-induced Parkinson's disease in murine models, making it a valuable tool for research into Parkinson's disease and dopamine metabolism. -
COMT Inhibitor
CGP 28014 is a potent inhibitor of catechol-O-methyltransferase (COMT), an enzyme involved in the metabolism of catecholamines. This compound has been shown to lower homovanillic acid (HVA) levels and increase dihydroxyphenylacetic acid (DOPAC) levels in the striatum of rat models. CGP 28014 is valuable in research focused on the pathophysiology and potential treatment strategies for Parkinson's disease, providing insights into dopaminergic signaling and neurotransmitter dynamics. -
COMT Inhibitor
BIA 3-335 is a potent inhibitor of catechol-O-methyltransferase (COMT), an enzyme involved in the metabolism of catecholamines. Its primary mechanism disrupts the methylation of catechols, leading to increased levels of dopamine, which may be beneficial in the study of Parkinson's disease and related neurological disorders. This compound is widely used in research settings to explore therapeutic strategies aimed at enhancing dopaminergic signaling. -
COMT Inhibitor
Methylspinazarin is a potent inhibitor of catechol O-methyltransferase (COMT), exhibiting an IC50 of 0.8 μg/ml. Isolated from the actinobacterium Streptomyces, Methylspinazarin demonstrates selectivity for COMT compared to tyrosine hydroxylase. This compound is valuable for research applications focused on neurotransmitter metabolism and the pharmacological modulation of catecholamine pathways. -
Stable Isotope
Dibucaine-d9 hydrochloride is a deuterium-labeled derivative of Dibucaine hydrochloride, primarily functioning as a sodium channel inhibitor. This compound exhibits strong inhibition of serum cholinesterase (SChE) activity, making it valuable in pharmacological studies related to analgesia and local anesthesia. Its stable isotope labeling facilitates advanced metabolic research and provides insights into drug metabolism and distribution. -
ACOX1 Inhibitor
10,12-Tricosadiynoic acid is a selective and potent inhibitor of acyl-CoA oxidase-1 (ACOX1). It demonstrates significant potential in addressing metabolic disorders induced by high-fat diets or obesity by enhancing mitochondrial lipid metabolism and modulating reactive oxygen species (ROS) levels. Additionally, this compound serves as a versatile click chemistry reagent, featuring an alkyne group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it valuable for various biochemical applications. -
Cholinesterase (ChE) Inhibitor
Sinapine hydroxide is an acetylcholinesterase (AChE) inhibitor with significant potential in the investigation of neurodegenerative disorders such as Alzheimer's disease, myasthenia gravis, ataxia, and Parkinson's disease. This alkaloid, derived from cruciferous seeds, exhibits a range of biological activities including anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic, and radioprotective effects. Its ability to modulate cholinergic pathways makes it a valuable tool for studying cholinergic dysfunction and related therapeutic strategies. -
P2X4 Antagonist
PSB-12054 is a selective antagonist of the P2X4 receptor, exhibiting an IC50 of 0.189 μM in human P2X4 assays. This compound has significant potential for studying neuropathic pain mechanisms and exploring therapeutic strategies for neurodegenerative diseases. Its specificity for P2X4 makes it a valuable tool for researchers investigating purinergic signaling pathways. -
P2X Receptor Inhibitor
PSFL2915 is a selective inhibitor of the P2X receptor family, exhibiting an IC50 of 0.319 μM for human P2X3 and 0.261 μM for rat P2X2/3, with approximately 42-fold selectivity for human P2X3 over human P2X2. This compound inhibits human P2X3 activation by disrupting the allosteric tightening of the inner pocket necessary for channel opening, with dependency on magnesium for its inhibitory effect. Additionally, PSFL2915 demonstrates inhibitory activity against rat P2X2/3 and human P2X2 receptors, while showing minimal effects on human P2X1, P2X4, and P2X7 receptors. It is applicable in chronic cough research. -
P2X4 Receptor Antagonist
5-BDBD is a selective antagonist of the P2X4 receptor, demonstrating potent inhibition of rP2X4R-mediated currents with an IC50 of 0.75 μM. This compound effectively interferes with both basal and acute hyperalgesia induced by nitroglycerin (NTG). 5-BDBD is valuable for studying pain mechanisms and the role of purinergic signaling in nociception. -
P2X3/P2X7 Receptor Ligand
α,β-Methylene-ATP trisodium is a potent agonist of P2X3 and P2X7 receptors, which facilitates significant biological responses through purinergic receptor activation. This compound is capable of traversing the blood-brain barrier, thereby influencing both peripheral and central nervous system pathways. It is instrumental in studying reflex cardiovascular responses and antinociceptive mechanisms mediated by noradrenergic neurons in the locus coeruleus. Researchers utilize α,β-Methylene-ATP trisodium for insights into neuropathic pain mechanisms and cardiovascular reflex regulation. -
P2X4 Antagonist
BAY-1797 is a selective antagonist of the P2X4 receptor, demonstrating a potent inhibition with an IC50 of 211 nM in human P2X4 assays. This compound exhibits minimal activity toward other P2X ion channels, allowing for targeted research applications. BAY-1797 has been shown to provide anti-nociceptive and anti-inflammatory effects, making it a valuable tool for studies into pain modulation and inflammatory processes. -
P2X Receptor Inhibitor
AZD9056 hydrochloride is a selective oral inhibitor of the P2X7 receptor, which is implicated in various inflammatory and pain-related conditions. By blocking P2X7 activity, this compound demonstrates potential in modulating inflammatory responses, making it a valuable tool for research in pain management and inflammatory disease pathways. Its application in preclinical studies may help elucidate the role of purinergic signaling in various biological processes. -
P2X7 Antagonist
JNJ-47965567 is a high-affinity, selective antagonist of the P2X7 receptor, exhibiting centrally permeable properties with pKis of 7.9 for human P2X7 and 8.7 for rat P2X7. This compound is instrumental in investigating the role of central P2X7 in rodent models, providing insights into its involvement in various CNS pathophysiological conditions. JNJ-47965567 is valuable for studies aimed at elucidating the molecular mechanisms underlying neurological disorders. -
P2X3 Antagonist
Camlipixant is a potent, selective, non-competitive antagonist of the P2X3 receptor, exhibiting an IC50 of 25 nM against human P2X3 homotrimers. This compound demonstrates significant anti-tussive activity without causing taste alterations. Camlipixant is primarily utilized in research focused on unexplained and refractory chronic cough. -
P2X7 Antagonist
JNJ-55308942 is a selective P2X7 antagonist with high affinity and significant brain penetration. It effectively inhibits the P2X7 receptor, demonstrating IC50 values of 10 nM for human and 15 nM for rat P2X7, along with corresponding Ki values of 7.1 nM and 2.9 nM. This compound is orally bioavailable and has been shown to block the release of IL-1β from adult rodent brain tissue, making it a valuable tool for investigating neuroinflammatory processes and related therapeutic applications. -
P2X1 Receptor Antagonist
NF023 hexasodium is a selective and competitive antagonist of the P2X1 receptor, demonstrating an IC50 value of 0.21 μM. While showing significantly higher IC50 values of 28.9 μM, > 50 μM, and > 100 μM for human P2X3, P2X2, and P2X4 receptor-mediated responses respectively, it provides a robust tool for investigating P2X1 receptor functions. This reagent is valuable in pharmacological research and studies exploring the role of purinergic signaling in various physiological and pathological processes. -
P2X4 Inhibitor
NP-1815-PX sodium is a selective inhibitor targeting the P2X4 receptor, exhibiting an IC50 of 0.26 μM against human P2X4 receptors. This compound effectively inhibits ATP-mediated prostaglandin production and attenuates TP receptor-induced calcium elevation, as well as NLRP3 inflammasome signaling. Notably, NP-1815-PX sodium demonstrates anti-allodynic effects in vivo and alleviates DNBS-induced colitis symptoms, including weight loss and tissue damage, through the downregulation of IL-1β levels and Caspase-1 activity. This reagent is applicable in research areas such as asthma and inflammatory bowel disease. -
P2X Receptor Antagonist
TNP-ATP triethylammonium is a selective antagonist of the P2X receptor, primarily involved in purinergic signaling. This compound exhibits significant antinociceptive effects in preclinical models, making it a valuable tool for investigating pain mechanisms. TNP-ATP triethylammonium can be utilized in research focused on pain modulation and the role of purinergic receptors in various physiological processes. -
P2X3 Antagonist
Eliapixant is a potent and selective antagonist of the P2X3 receptor, exhibiting an IC50 of 8 nM. It is primarily utilized in research related to refractory chronic cough, offering valuable insights into the mechanisms underlying this condition. The compound's specificity towards the P2X3 receptor makes it a valuable tool for studying purinergic signaling in respiratory pathways. -
P2X3 Receptor Antagonist
Sivopixant is a selective antagonist of the P2X3 receptor, exhibiting a potent inhibitory activity with an IC50 of 4.2 nM for P2X3 and 1100 nM for P2X2/3. This compound demonstrates significant analgesic properties, making it valuable for research focused on pain pathways and therapeutic applications in pain management. Sivopixant can be utilized in studies investigating the role of purinergic signaling in nociception and related disorders. -
P2X3 Antagonist
P2X3 antagonist 34 is a selective and orally active antagonist targeting the P2X3 homotrimeric receptor, demonstrating IC50 values of 25 nM, 92 nM, and 126 nM for human, rat, and guinea pig P2X3 receptors, respectively. This compound exhibits reduced activity against P2X2/3 heterotrimeric receptors, indicating a favorable selectivity profile. Its significant anti-tussive properties make P2X3 antagonist 34 a valuable tool for research in pain and respiratory conditions. -
P2X7 Receptor Antagonist
P2X7 receptor antagonist-2 is a selective antagonist of the P2X7 receptor, exhibiting a pIC50 value between 6.5 and 7.5. This compound demonstrates significant efficacy in reducing neuroinflammation, making it a valuable tool for research in neurodegenerative diseases and inflammatory conditions. Its ability to modulate P2X7 receptor activity positions it as a promising candidate for investigating therapeutic strategies targeting neuroinflammatory pathways. -
P2X3 Antagonist
Gefapixant citrate is a potent antagonist of the purinergic P2X3 receptor, exhibiting IC50 values of approximately 30 nM against recombinant human P2X3 homotrimers and 100-250 nM at human P2X2/3 heterotrimeric receptors. This compound is valuable for research related to chronic cough and knee osteoarthritis, providing insights into the modulation of nociceptive signaling pathways associated with these conditions. Its oral bioavailability further enhances its applicability in in vivo studies. -
P2X7 Receptor Antagonist
Lu AF27139 is a selective antagonist of the P2X7 receptor, exhibiting potent inhibitory activity with IC50 values of 12 nM and 2.4 nM for human and rat receptors, respectively. Additionally, it demonstrates effective inhibition in mouse, human, and rat models with Kis of 22, 54, and 13 nM. Due to its favorable pharmacokinetic profile, including oral activity and CNS penetration, Lu AF27139 is a valuable tool for investigating central nervous system diseases. -
P2X4 Receptor Inhibitor
Taspine is a natural product that functionally inhibits the P2X4 receptor, primarily through the inhibition of the PI3K signaling pathway. This compound exhibits notable anti-inflammatory activity by suppressing pro-inflammatory signaling in macrophages. Taspine is valuable for research applications focused on inflammation and immune responses, as well as studying the role of purinergic receptors in various pathological conditions. -
P2X7 Antagonist
JNJ-42253432 is a high-affinity orally active antagonist of the P2X7 receptor, exhibiting significant CNS penetration. With pKi values of 9.1 for rat and 7.9 for human P2X7 channels, it effectively modulates purinergic signaling. This compound is valuable for research on neuroinflammation, pain pathways, and other P2X7-related biological processes. -
P2X3 Receptor Antagonist
NF110 is a P2X3 receptor antagonist with a Ki of 36 nM, demonstrating selectivity as it is inactive toward stably expressed P2Y receptors (IC50s > 10 µM). It effectively inhibits alpha, beta-methylene-ATP-induced currents in rat dorsal root ganglia neurons, with an IC50 value of 527 nM. This compound is valuable for researching pain pathways and receptor signaling in nociceptive responses. -
P2-Receptor Agonist
2-Methylthio-ATP tetrasodium is a non-specific P2-receptor agonist that modulates purinergic signaling pathways. It has been shown to cause noncompetitive inhibition of ADP-induced aggregation in human platelets. This reagent is valuable for studies investigating platelet function, receptor signaling, and related cardiovascular research applications. -
P2X3 Receptor Antagonist
(E/Z)-Sivopixant is a selective antagonist of the P2X3 receptor, exhibiting an IC50 value of 4 nM. This compound demonstrates significant biological activity in modulating pain signals and neurogenic inflammation. It is primarily employed in research related to respiratory diseases, providing insights into potential therapeutic strategies for conditions associated with P2X3 receptor activation. -
P2X3 Receptor Inhibitor
P2X3-IN-1 is a selective inhibitor of the P2X3 receptor, which plays a crucial role in mediating pain and other neurogenic responses. This compound demonstrates significant biological activity in modulating P2X3 receptor signaling, making it valuable for research into neurogenic diseases and pain pathways. Researchers can utilize P2X3-IN-1 to explore therapeutic strategies for conditions associated with P2X3 receptor dysfunction. -
P2X3/P2X2/3 Receptor Antagonist
RO-3 is a potent orally active antagonist of the P2X3 and P2X2/3 receptors, exhibiting pIC50 values of 5.9 and 7.0 for human homomultimeric P2X3 and heteromultimeric P2X2/3 receptors, respectively. This compound demonstrates selectivity for P2X3 and P2X2/3, with IC50 values exceeding 10 μM against all other functional P2X receptor homomultimers, including P2X1, P2X2, P2X4, P2X5, and P2X7. RO-3 is valuable for research focused on pain pathways and chronic pain conditions due to its specific receptor interactions. -
P2X Agonist
BzATP triethylammonium is a potent P2X receptor agonist that exhibits varying pEC50 values across multiple P2X receptor subtypes, including 8.74 for P2X1, 5.26 for P2X2, 7.10 for P2X3, 7.50 for P2X2/3, 6.19 for P2X4, and 6.31 for P2X7. It demonstrates significant activity at P2X7 receptors, with EC50 values of 3.6 μM for rat P2X7 and 285 μM for mouse P2X7. BzATP triethylammonium is valuable for research investigating purinergic signaling pathways and receptor pharmacology. -
P2X4 Inhibitor
P2X4 antagonist-1 is a potent inhibitor of the P2X4 receptor, exhibiting an IC50 of 15 nM. This compound effectively modulates P2X4 signaling, making it valuable for research involving pain modulation, neuroinflammation, and cardiovascular regulation. Its specificity towards P2X4 supports studies aimed at understanding its role in various pathophysiological conditions. -
P2X1 receptor antagonist
Ro 0437626 is a selective antagonist of the purinergic P2X1 receptor, exhibiting an IC50 value of 3 μM. It demonstrates low affinity for P2X2, P2X3, and P2X2/3 receptors, with IC50 values exceeding 100 μM. This compound is valuable for research applications involving the modulation of P2X1 receptor signaling pathways, contributing to studies in cardiovascular and pain research. -
P2X7 Receptor Antagonists
AZ 11645373 is a selective antagonist of the human P2X7 receptor, demonstrating significant potency without affecting the rat variant. It effectively inhibits ATP-induced release of IL-1β from lipopolysaccharide-activated THP-1 cells, with an IC50 value of 90 nM. This compound is valuable for studies focused on inflammatory processes and purinergic signaling pathways. -
P2X4 Receptor Antagonist
MRS4719 is a potent antagonist of the P2X4 receptor, exhibiting an IC50 value of 0.503 μM in human P2X4 receptor assays. This compound demonstrates neuroprotective effects by reducing infarct volume and promoting neurorehabilitation in models of ischemic stroke. Additionally, MRS4719 effectively decreases ATP-induced intracellular calcium influx in primary human monocyte-derived macrophages, making it a valuable reagent for studying ischemic stroke and related neuroinflammatory processes. -
P2X Receptor Antagonist
AF-353 hydrochloride is a potent and selective antagonist of the P2X3 and P2X2/3 receptors, exhibiting a pIC50 of 8.0 for both human and rat P2X3 and a pIC50 of 7.3 for human P2X2/3. This compound is notable for its oral bioavailability, making it suitable for in vivo studies. AF-353 hydrochloride is primarily utilized in research applications focused on pain modulation and the study of purinergic signaling pathways. -
P2X3 Antagonist
P2X3 antagonist 38 is a potent oral antagonist of the P2X3 receptor, demonstrating IC50 values of 0.132 µM for human P2X3, 0.165 µM for rat P2X3, and 0.421 µM for guinea pig P2X3. This compound is valuable in studies focused on pain modulation and respiratory disorders, positioning it as a significant tool for researching the role of P2X3 in various biological processes. Its high selectivity and efficacy make it suitable for in vivo applications in pharmacological investigations. -
P2X3 Receptor Inhibitor
Purotoxin 1 is a selective P2X3 receptor inhibitor. It exhibits significant antinociceptive effects in animal models of inflammatory pain, making it a valuable tool for pain research. Isolated from the venom of the wolf spider Geolycosa sp., Purotoxin 1 can be utilized in studies aimed at understanding pain mechanisms and developing new analgesic therapies. -
P2X7 Antagonist
(S)-JNJ-54166060 is a selective P2X7 antagonist, exhibiting potent inhibitory activity against the P2X7 receptor. This compound is useful in research related to chronic inflammatory diseases, neurodegeneration, and pain pathways, as well as studying the role of P2X7 in immune responses. Its specificity and efficacy make it a valuable tool for investigating the therapeutic potential of modulating P2X7 signaling.
