Catalog No.
Product Name
Application
Product Information
Citations
-
P2X4 Receptor Antagonist
BX430 is a potent noncompetitive allosteric antagonist of the human P2X4 receptor, exhibiting an IC50 value of 0.54 μM. This compound demonstrates selectivity and species specificity, making it a valuable tool for investigating the role of P2X4 receptors in various biological processes. BX430 is primarily utilized in research applications related to chronic pain and cardiovascular diseases, providing insight into therapeutic potential in these areas. -
Stable Isotope
Acetylcholine-d9 chloride is a deuterium-labeled form of acetylcholine chloride, a potent cholinergic agonist that effectively crosses the blood-brain barrier. This compound modulates dopaminergic neuronal activity by stimulating nicotinic acetylcholine receptors (nAChRs). Additionally, it has been shown to inhibit p53 mutant peptide aggregation in vitro, making it valuable for research focused on neurobiology, receptor pharmacology, and protein aggregation studies. -
Neuroprotective Compound
REM127 is a neuroprotective small molecule that modulates calcium homeostasis in cells. It effectively restores calcium balance in cellular models affected by the pathological accumulation of tau protein, demonstrating potential to mitigate synaptic and cognitive deficits in Alzheimer's disease models. REM127 is capable of crossing the blood-brain barrier and may slow the progression of amyloid-beta and tau protein pathologies. This compound is suitable for research applications in neurodegenerative diseases. -
NMDA Receptor Inhibitor
Bupivacaine-d9 is a deuterium-labeled analog of Bupivacaine, primarily targeting NMDA receptors. This compound exhibits inhibitory effects on sodium, L-calcium, and potassium channels, with a notable potency against SCN5A channels, characterized by an IC50 value of 69.5 μM. Bupivacaine-d9 is utilized in research related to chronic pain mechanisms and the modulation of excitatory neurotransmission, offering valuable insights into therapeutic applications in pain management. -
Calcium Channel
2-Chloro-ATP sodium is an analog of ATP that acts as an antagonist of the purinergic P2Y1 receptor, inhibiting intracellular calcium mobilization induced by ADP in Jurkat cells with a Ki of 2.3 μM. Additionally, it serves as an agonist for the purinergic P2X receptor, generating inward currents in HEK293 cells with varying affinities (EC50 of 0.5 and 2.5 μM). This compound also induces concentration-dependent relaxation of precontracted guinea pig cecal strips. Furthermore, 2-Chloro-ATP sodium is utilized to investigate substrate specificity among cyclic nucleotide-dependent protein kinases, including protein kinase A (PKA) and PKG. -
α7 nAChR Allosteric Modulator
PAM-2 is a selective positive allosteric modulator of the α7 nicotinic acetylcholine receptor (nAChR). Exhibiting potent anti-nociceptive and anti-inflammatory properties, PAM-2 enhances receptor activity, demonstrating efficacy in animal models of neuropathic pain induced by Streptozotocin and Oxaliplatin. It shows selectivity for α7 nAChR over α9α10 nAChR and CaV2.2 channels, making it a valuable tool for research into pain mechanisms and potential therapeutic applications in neuropathic pain. -
Calcium Antagonist
Phenchlobenpyrrone is a selective neuronal calcium antagonist that effectively crosses the blood-brain barrier. This compound demonstrates the capability to mildly inhibit acetylcholinesterase (AChE) activity, along with inhibiting amyloid-beta (Aβ) aggregation and promoting the clearance of Aβ oligomers. Additionally, Phenchlobenpyrrone reduces abnormal phosphorylation of Tau protein. This agent is valuable for research applications focused on Alzheimer's disease and related neurodegenerative conditions. -
α9α10 nAChR/CaV2.2 Antagonist
GeX-2 is a truncated analogue of αO-conotoxin that serves as an antagonist of the α9α10 nicotinic acetylcholine receptor (nAChR) and CaV2.2 channels. This compound demonstrates significant analgesic properties, effectively alleviating pain in rat models exhibiting chronic constriction injury. GeX-2 is valuable in research focusing on pain mechanisms and the modulation of excitatory neurotransmission through its interactions with nAChR and calcium channels. -
α-Amylase Inhibitor
α-Amylase-IN-3 is a potent inhibitor of α-Amylase, exhibiting an IC50 of 18.04 μM, and also targets acetylcholinesterase (AChE) with IC50s of 21.04 μM and 22.2 μM, respectively. This compound demonstrates antioxidant activity, making it valuable for studies related to diabetes and diseases associated with oxidative stress. Its biochemical properties make α-Amylase-IN-3 a useful tool for researchers investigating metabolic disorders and neuroprotective mechanisms. -
α-glucosidase/α-amylase enzyme Dual Inhibitor
α-Amylase/α-Glucosidase-IN-7 is a competitive dual inhibitor targeting α-glucosidase and α-amylase, demonstrating IC50 values of 18.52 µM and 20.25 µM, respectively. Additionally, this compound effectively inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), with IC50 values of 9.25 µM and 10.06 µM. α-Amylase/α-Glucosidase-IN-7 is valuable for research applications related to diabetes and Alzheimer’s disease. -
CES Inhibitor
Dibromsalicil is a selective inhibitor of carboxylesterases (CES), exhibiting inhibitory activity with IC50 values of 72.7 nM against human intestinal carboxylesterase (hiCE) and 53.5 nM against rabbit liver carboxylesterase (rCE). This compound demonstrates minimal activity against human liver carboxylesterase (hCE1) and cholinesterase, making it a valuable tool for research applications focused on drug metabolism and enzymatic activity modulation. Its specificity for hiCE and rCE positions Dibromsalicil as an important reagent for studying carboxylesterase-related pathways. -
AChE/CES Inhibitor
Heptenophos is a potent inhibitor of acetylcholinesterase (AChE) and plasma carboxylesterase (CES). By obstructing AChE activity, Heptenophos leads to the accumulation of acetylcholine at cholinergic synapses, which can result in symptoms characteristic of organophosphate poisoning. Its rapid toxicity in animal models, such as male albino mice, allows for the investigation of detoxification strategies, particularly in conjunction with agents like obidoxime and Memantine. This compound is widely utilized in research exploring the mechanisms underlying organophosphate effects and potential antidotal treatments. -
COMT Inhibitor
Neluxicapone is a potent inhibitor of catechol-O-methyltransferase (COMT), primarily utilized in the research of Parkinson's disease (PD). By inhibiting COMT, this compound enhances dopamine levels in the brain, which may alleviate motor symptoms associated with PD. Researchers can use neluxicapone to investigate its pharmacological effects and potential therapeutic benefits in neurodegenerative conditions. -
Hydroxycinnamic Acid
5-Hydroxyferulic acid is a hydroxycinnamic acid derived from the phenylpropanoid pathway. It serves as a key precursor in the biosynthesis of sinapic acid and acts as a non-esterified substrate for catechol-O-methyltransferase (COMT). This compound is utilized in various research applications focused on studying phenolic compounds and their roles in plant metabolism and health benefits. -
COMT Inhibitor
Ro 41-0960 is a selective inhibitor of catechol-O-methyltransferase (COMT), which plays a crucial role in the metabolism of catecholamines. By inhibiting COMT, this compound enhances the levels of neurotransmitters such as dopamine, norepinephrine, and epinephrine. It is widely used in research to investigate the biochemical pathways of neurotransmission and to explore potential therapeutic applications in conditions such as Parkinson's disease and other neuropsychiatric disorders. -
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. -
CaMKK2 Inhibitor
CaMKK2-IN-1 is a selective inhibitor of calcium/calmodulin-dependent protein kinase kinase 2 (CaMKK2) with an IC50 of 7 nM. This compound displays high ligand efficiency, making it a valuable tool for investigating the role of CaMKK2 in cellular signaling pathways. Its application in research includes studies on metabolism, cancer, and neurological disorders where the modulation of CaMKK2 activity may provide insights into therapeutic interventions. -
CAMKK2 Inhibitor
SGC-CAMKK2-1 is a selective inhibitor of calcium/calmodulin-dependent protein kinase kinase 2 (CAMKK2), exhibiting an IC50 of 30 nM. This compound effectively inhibits AMPK phosphorylation in C4-2 cells with an IC50 of 1.6 μM. SGC-CAMKK2-1 serves as a valuable chemical probe for investigating the role of CAMKK2 in various biological processes and pathways related to cellular energy regulation and metabolism. -
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. -
OGT Inhibitor
ST045849 is a small-molecule inhibitor targeting O-GlcNAc transferase (OGT) with an IC50 of 30 μM against the soluble form of OGT (sOGT) and 53 μM against the nuclear/cytoplasmic form (ncOGT). This compound is valuable for studying the role of OGT in metabolism-related diseases, providing insights into regulatory mechanisms involving O-GlcNAcylation. Its application aids in understanding the biological implications of OGT inhibition in various pathological conditions. -
OGT Inhibitor
OSMI-2 is a selective inhibitor of O-linked N-acetylglucosamine transferase (OGT), designed for cellular permeability. This compound has been shown to enhance the splicing of retained introns in various cell types, making it a valuable tool for studying the regulation of alternative splicing and OGT's role in cellular processes. OSMI-2 is applicable in various research fields, including cancer biology and neurodegenerative disorders, where OGT activity is implicated. -
Racemate of OSMI-1
(Rac)-OSMI-1 is a racemic mixture of OSMI-1, a potent inhibitor of O-GlcNAc transferase (OGT) that exhibits an IC50 value of 2.7 μM. This compound effectively inhibits O-linked N-acetylglucosamine (O-GlcNAcylation) in various mammalian cell lines, while not significantly affecting cell surface N- or O-linked glycans. Its application spans diverse studies in cellular signaling and glycosylation modifications, making it a valuable tool for research into OGT-related biological processes. -
OGT Inhibitor
OSMI-3 is a selective inhibitor of O-linked N-acetylglucosamine transferase (OGT), characterized by its potent and cell-permeable properties. This compound effectively modulates OGT activity, leading to the enhancement of retained intron splicing in cellular contexts. OSMI-3 is valuable in research investigating the role of OGT in cellular processes and its implications in various disease states. -
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.
