Catalog No.
Product Name
Application
Product Information
Citations
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Stable Isotope
(R)-3-O-Methyldopa-d3 is a deuterated form of the R-enantiomer of 3-O-Methyldopa, which acts as a metabolite of L-DOPA. The compound exerts its biological activity by competitively inhibiting catechol-O-methyltransferase (COMT), thus influencing the pharmacological effects of both L-DOPA and dopamine. This stable isotope is essential for research applications involving metabolic pathways and neurological studies. -
P2Y1 receptor/[35S]GTPγS binding/β-arrestin 2 recruitment Agonist
MRS2365 is a highly potent and selective agonist of the P2Y1 receptor, exhibiting an EC50 of 0.4 nM for [35S]GTPγS binding and β-arrestin 2 recruitment. This compound effectively alleviates mechanical allodynia and enhances mechanical sensitivity, making it valuable for pain research. Notably, MRS2365 demonstrates minimal activity at P2Y12 and P2Y13 receptors, highlighting its specificity for P2Y1. -
BChE Inhibitor/CB2R Agonist
hBChE-IN-2 is a potent butyrylcholinesterase (BChE) inhibitor with an IC50 of 0.62 μM and functions as an agonist for cannabinoid receptor 2 (CB2R). This compound exhibits significant neuroprotective activities, making it a valuable tool in the study of neurodegenerative diseases and cannabinoid signaling pathways. Its dual action positions hBChE-IN-2 as an important reagent for research applications targeting cholinergic regulation and endocannabinoid modulation. -
Alkaloid
Aposcopolamine is an alkaloid isolated from Datura ferox, known for its ability to bind closely with acetylcholinesterase (ACHE), adrenergic receptor alpha-2A (ADRA2A), and muscarinic receptor subtype 2 (CHRM2). This compound is of significant interest in Alzheimer's disease research due to its potential effects on cholinergic signaling pathways. Aposcopolamine serves as a valuable tool in investigating neurodegenerative mechanisms and developing therapeutic strategies. -
M3 mAChR Antagonist
p-F-HHSiD hydrochloride is a potent and selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound also demonstrates antagonistic properties towards other mAChR subtypes and the alpha1-adrenoceptor. p-F-HHSiD hydrochloride is useful for research applications involving cancer, metabolic disorders, neurological conditions, and cardiovascular diseases, including colon cancer, Alzheimer’s disease, and diabetes. -
mAChR Antagonist
Batefenterol Succinate is an inhaled bifunctional bronchodilator that acts as a muscarinic acetylcholine receptor (mAChR) antagonist and a beta2-adrenoceptor agonist. This dual mechanism results in effective smooth muscle relaxation, enhancing respiratory function. Batefenterol Succinate is primarily utilized in research focused on chronic obstructive pulmonary disease (COPD) and other respiratory conditions, providing insights into therapeutic strategies for airway obstruction. -
mAChR/Adrenergic Receptor Antagonist
Muscarinic toxin 3 (MT3) is a selective and non-competitive antagonist of muscarinic acetylcholine receptors (mAChRs) and adrenergic receptors. It exhibits high potency with pIC50 values of 6.71, 8.79, 8.86, 7.57, 8.13, and 8.49 against M1, M4, α1A, α1B, α1D, α2A, α2B, and α2C receptors, respectively, highlighting its prominent adrenoceptor activity. This compound is valuable in studying receptor signaling pathways and has potential applications in pharmacological research focused on nervous system disorders and cardiovascular diseases. -
M3 mAChR Antagonist
p-F-HHSiD (p-Fluorohexahydrosiladifenidol) functions as a selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound exhibits antagonistic activity against various muscarinic receptor subtypes as well as the alpha-1 adrenergic receptor. p-F-HHSiD is valuable for research in cancer, metabolic disorders, neurological pathologies, and cardiovascular diseases, including colon cancer, Alzheimer's disease, and diabetes. -
P2Y14R Antagonist
MK-852 is a potent P2Y14 receptor antagonist that plays a crucial role in modulating platelet aggregation. This compound effectively inhibits the binding of fibrinogen to platelets in vitro, making it a valuable tool for studying thrombotic processes. Research applications include investigations into platelet function and the development of antithrombotic therapies. -
Topoisomerase I Inhibitor
RPR121056 is a topoisomerase I inhibitor that functions as a metabolite of the chemotherapy agent Irinotecan (CPT-11), produced by the enzyme CYP3A4. This compound induces cell death by disrupting DNA replication, making it relevant for cancer research, particularly in the context of colorectal cancer treatment. Additionally, RPR121056 demonstrates direct inhibition of acetylcholinesterase (AChE), further expanding its potential applications in pharmacological studies. -
Stable Isotope
RPR121056-d3 is a deuterated analog of RPR121056, a metabolite of the anticancer drug Irinotecan. It primarily targets and inhibits topoisomerase type I, leading to apoptosis in cancer cells. RPR121056-d3 is utilized in research applications focused on understanding the metabolic pathways and pharmacokinetics of Irinotecan, particularly in the context of colorectal cancer therapy. Additionally, it may also provide insights into the inhibition of acetylcholinesterase (AChE). -
Integrated Stress Response Pathway Modulator
Comtifator is an integrated stress response pathway modulator that influences cellular responses to various stressors. This compound is essential for studying the role of the integrated stress response in diseases such as neurodegeneration and cancer. Its ability to alter stress signaling makes it a valuable tool for research investigating therapeutic interventions and mechanisms underlying stress-related disorders. -
Alkaloid
Circumdatin C is an alkaloid that demonstrates inhibitory effects on lipopolysaccharide (LPS)-stimulated nitric oxide production. Additionally, it inhibits acetylcholinesterase (AChE) activity with an IC50 value of 13.9 μM. This compound is valuable for research into neurodegenerative diseases, particularly Alzheimer's disease, by exploring mechanisms related to neurotransmitter regulation and neuroinflammation. -
Antioxidant Agent
4-Hydroxyisophthalic acid functions primarily as an antioxidant agent, activating crucial antioxidant enzymes such as catalase (CAT) and superoxide dismutase (SOD). Its ability to scavenge free radicals contributes to its protective effects on neuronal function, as it enhances the activity of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). In research applications, 4-Hydroxyisophthalic acid has demonstrated potential in improving cognitive defects and alleviating circadian rhythm disorders in model organisms, such as fruit flies. -
Stable Isotope
Imidazole-15N2 is a stable isotope-labeled derivative of imidazole, a heterocyclic aromatic compound. It serves as a valuable tool in metabolic studies and tracing experiments due to its nitrogen-15 labeling. Imidazole and its derivatives exhibit a wide range of biological activities, including inhibition of acetylcholinesterase and xanthine oxidase, as well as properties such as antifungal, antituberculosis, anti-inflammatory, and antioxidant effects. Additionally, imidazole derivatives have shown promise in the inhibition of SARS-CoV-2 3CLPro enzyme, highlighting their potential applications in research related to Alzheimer's disease, gout, COVID-19, and thromboembolic disorders. -
COX Inhibitor
SC57666 is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 26 nM. This compound exhibits anti-inflammatory activity by specifically blocking COX-2, thereby reducing prostaglandin synthesis. SC57666 is valuable for research applications focused on understanding inflammation and pain mechanisms, as well as for screening in drug discovery efforts targeting COX-2 related conditions. -
COX Inhibitor
FR-188582 is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 value of 17 nM. This compound exhibits potent anti-inflammatory activity, making it a valuable tool for studies related to pain and inflammation pathways. Its specificity for COX-2 allows for the exploration of therapeutic applications in conditions such as arthritis and other inflammatory diseases. -
COX Inhibitor
Nitroflurbiprofen is a cyclooxygenase (COX) inhibitor known for its nitric oxide (NO)-donating properties. It effectively modulates increased intrahepatic vascular tone, making it a valuable tool in studying portal hypertension and liver diseases. This compound is utilized in research contexts focused on the therapeutic mechanisms of COX inhibition and its impact on hepatic vascular dynamics. -
COX Inhibitor
RWJ 63556 is an orally active inhibitor of cyclooxygenase-2 (COX-2) and a 5-lipoxygenase inhibitor, exhibiting significant anti-inflammatory properties. This compound is utilized in research to explore its potential therapeutic effects in conditions characterized by inflammation, such as arthritis and other inflammatory diseases. Its selective inhibition may provide insights into the role of COX-2 and lipoxygenase pathways in various biological processes. -
COX Inhibitor
COX-2-IN-6 is a selective cyclooxygenase-2 (COX-2) inhibitor, specifically designed for oral administration and exhibiting gut-restricted properties. With an IC50 value of 0.84 μM and a Ki of 69 nM, COX-2-IN-6 effectively targets COX-2, inhibiting COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM. This compound is utilized in research focused on colorectal cancer chemoprevention, offering valuable insights into inflammatory processes and therapeutic strategies. -
COX-2 Inhibitor
COX-2-IN-28 is a potent and selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 of 0.054 µM for COX-2, while demonstrating significantly lower inhibitory activity against 15-lipoxygenase (2.14 µM) and cyclooxygenase-1 (13.21 µM). This selective inhibition positions COX-2-IN-28 as a valuable tool for investigating the role of COX-2 in inflammation and pain pathways. It is suitable for research applications focused on inflammatory diseases and therapeutic development targeting COX-2 pathways. -
COX Inhibitor
Tolmetin sodium is a potent inhibitor of cyclooxygenase (COX), demonstrating IC50 values of 0.35 μM for human COX-1 and 0.82 μM for COX-2. As a non-steroidal anti-inflammatory drug (NSAID), it is primarily used for its analgesic and anti-inflammatory properties. Tolmetin sodium is valuable in research applications focused on pain management, inflammation, and associated disorders. -
COX-2 Inhibitor
SD 8381 is a potent and selective inhibitor of cyclooxygenase-2 (COX-2). It demonstrates an IC50 value of 0.0098 μM against human COX-2 and 0.69 μM against human COX-1, indicating a high degree of selectivity. This compound is valuable for research applications focused on inflammation and pain management, as well as studies examining the role of COX-2 in various disease states. -
COX2 Inhibitor
COX-2-IN-56 is a selective inhibitor of cyclooxygenase-2 (COX-2), demonstrating minimal inhibition of cyclooxygenase-1 (COX-1). This compound is valuable for investigating COX-2-dependent disorders, particularly in the context of inflammatory processes. Its specificity makes it suitable for research applications focused on understanding the role of COX-2 in various pathological conditions. -
COX Inhibitor
Benzoylgomisin O is a selective inhibitor of cyclooxygenase enzymes COX-1 and COX-2, as well as 15-lipoxygenase (15-LOX). This compound, isolated from Schisandra rubriflora, exhibits significant anti-inflammatory activity, making it a valuable reagent for research into inflammatory diseases and related pathways. Its ability to modulate lipid mediators positions it as a potential tool in the study of pathophysiological conditions where COX and LOX pathways are implicated. -
COX-1 inhibitor
COX-1-IN-1 is a selective inhibitor of cyclooxygenase-1 (COX-1) with an IC50 value of 0.23 μM, demonstrating a high degree of selectivity over COX-2 (IC50 > 50 μM), resulting in a selectivity index of 217. This compound effectively inhibits platelet aggregation, making it a useful tool in the study of inflammatory processes and cardiovascular research applications. COX-1-IN-1 can aid in understanding the role of COX-1 in various physiological and pathological conditions. -
COX-2 Inhibitor
Desmethyl etoricoxib is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 1 μM in whole blood, demonstrating significant potential in modulating inflammatory responses. It exhibits a lower affinity for COX-1, with an IC50 of 16 μM in U937 cells, highlighting its selectivity. This compound is valuable for research applications targeting inflammatory pathways and exploring therapeutic effects in various inflammatory conditions. -
COX1/2 Inhibitor
COX-1/2-IN-2 is a selective inhibitor of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), demonstrating potent activity with IC50 values of 9.7 ± 0.09 µM for COX-1 and 4.6 ± 1.45 µM for COX-2. This compound is useful in research applications involving inflammation and pain modulation, as it effectively reduces the synthesis of pro-inflammatory prostaglandins. Its utility in pharmacological studies makes it a valuable reagent for exploring COX-related pathways. -
COX-2 Inhibitor
Cassiatannin A is a proanthocyanidin tetramer that acts as a selective COX-2 inhibitor. It has demonstrated significant inhibition rates of 38%, 52%, and 97% at concentrations of 10, 100, and 1000 μg/mL, respectively. This compound is valuable for research into inflammatory processes and the molecular pathways associated with COX-2-mediated responses. -
COX-2 Inhibitor
COX-2-IN-21 is a selective, orally active inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 0.039 μM. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for research into inflammatory diseases and pain management. Its selectivity for COX-2 over COX-1 enhances its therapeutic potential while minimizing side effects associated with non-selective NSAIDs. -
iNOS/COX-2 Inhibitor
Longiferone B is a daucane sesquiterpene derived from the rhizomes of Boesenbergia longiflora, acting as an inhibitor of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). It exhibits significant anti-inflammatory properties, effectively reducing nitric oxide production with an IC50 value of 21.0 μM. Longiferone B also suppresses the mRNA expression of iNOS and COX-2, making it a valuable compound for research in inflammation-related studies. -
COX-2 Inhibitor
COX-2-IN-27 is a potent and selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 of 0.045 µM against COX-2, while demonstrating significantly higher IC50 values of 13.22 µM for COX-1 and 1.67 µM for 15-lipoxygenase (15-LOX). This compound exhibits notable anti-inflammatory activity, making it a valuable tool for research in inflammation-related pathways and the study of COX-2 mediated processes. Its selectivity enables detailed investigations into the role of COX-2 in disease and therapeutic applications. -
COX-1 Inhibitor
VU0487836 is a selective inhibitor of cyclooxygenase-1 (COX-1), exhibiting an IC50 value of 0.36 μM against ovine-derived COX-1. This compound is being investigated as a prototype for developing radiological imaging agents aimed at COX-1 in ovarian cancer. VU0487836 is relevant for research focused on ovarian cancer and may provide insights into therapeutic strategies targeting COX-1 pathways. -
COX-2 Inhibitor
LM-4108 (N-(2-Phenylethyl)-indomethacin amide) is a selective and orally active inhibitor of COX-2, demonstrating an IC50 of 0.06 μM against purified human COX-2. This compound exhibits significant anti-inflammatory properties and has potential applications in cancer prevention. The metabolic stability of LM-4108 varies across species, with half-lives of 11 minutes in rat, 21 minutes in human, and 51 minutes in mouse liver microsomes. -
COX-2 Inhibitor
COX-2-IN-5 is a selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 value of 0.65 µM. This compound is primarily utilized in research focused on inflammation and related pathways. Its potent inhibitory activity makes it an invaluable tool for studying COX-2 mediated processes in various biological contexts. -
COX-2/5-LOX Inhibitor
COX-2/5-LOX-IN-2 is a potent dual inhibitor of cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LOX). This benzothiophen-2-yl pyrazole carboxylic acid derivative demonstrates significant analgesic and anti-inflammatory properties, exhibiting COX-2 inhibitory activity with an IC50 of 0.01 μM and 5-LOX inhibitory activity with an IC50 of 1.78 μM. COX-2/5-LOX-IN-2 is a valuable tool for research applications aimed at understanding and modulating inflammatory pathways. -
COX Inhibitor
Plantanone A is a selective cyclooxygenase (COX) inhibitor, demonstrating an IC50 of 33.37 μM for ovine COX-1 and 46.16 μM for ovine COX-2. This compound exhibits limited DPPH radical scavenging activity with an IC50 of 467.7 μM. Plantanone A serves as a valuable tool for investigating inflammation-related diseases and their underlying mechanisms. -
COX-2 Inhibitor
COX-2-IN-17 is a potent inhibitor of cyclooxygenase-2 (COX-2) with a remarkable ability to penetrate the blood-brain barrier (BBB), exhibiting an IC50 of 0.02 μM. This compound demonstrates significant anti-inflammatory and analgesic properties, effectively reducing hyperalgesia during both the neurogenic and inflammatory phases. COX-2-IN-17 is suitable for research applications aimed at understanding pain mechanisms and exploring potential therapeutic interventions for inflammatory conditions. -
COX-1/2 Inhibitor
N-Acetyl-2-carboxybenzenesulfonamide is a potent inhibitor of COX-1 and COX-2, exhibiting IC50 values of 0.06 μM and 0.25 μM, respectively. This compound demonstrates significant anti-inflammatory activity, making it a valuable tool for the study of inflammatory pathways and the development of anti-inflammatory therapies. Its ability to selectively inhibit cyclooxygenase enzymes positions it as a useful agent in pharmacological research. -
COX-2 Inhibitor
COX-2-IN-51 is a selective COX-2 inhibitor exhibiting an IC50 of 70.7 nM. It effectively reduces LPS-induced release of nitric oxide (NO) and prostaglandin E2 (PGE2), as well as the expression of COX-2 and inducible nitric oxide synthase (iNOS), and inhibits the NF-κB signaling pathway. This compound demonstrates anti-inflammatory and analgesic properties in various murine models by targeting the NF-κB cascade, while presenting a lower risk of gastrointestinal side effects compared to traditional nonsteroidal anti-inflammatory drugs. -
COX-I Inhibitor
2,5-Dimethoxy-3-glucopyranosylcinnamic alcohol is a selective inhibitor of the cyclooxygenase-1 (COX-I) enzyme. This compound exhibits notable anti-inflammatory properties, making it a valuable tool for research in inflammation-related pathways. It is isolated from the plant species P. crocatum and Dirca palustris and can be utilized in studies investigating the modulation of inflammatory responses and related signaling mechanisms. -
COX Inhibitor
Pemedolac is a selective inhibitor of cyclooxygenase (COX), demonstrating potent analgesic activity while minimizing anti-inflammatory effects. This compound exhibits significant efficacy in alleviating chemically induced and inflammatory pain in preclinical models, with effective pain relief achieved at lower doses than those typically associated with anti-inflammatory or gastric irritant effects. Pemedolac has a reduced ulcerogenic potential, suggesting a safer profile compared to standard nonsteroidal anti-inflammatory drugs (NSAIDs), making it a valuable candidate in the treatment of neurological, dermatological, and musculoskeletal disorders. -
COX-1 Inhibitor
COX-1-IN-4 is a selective inhibitor of cyclooxygenase-1 (COX-1), demonstrating an IC50 of 0.09 μM for COX-1 and 2.49 μM for COX-2. This compound effectively reduces nitric oxide production and decreases the expression of the inducible nitric oxide synthase (iNOS) protein. COX-1-IN-4 is valuable for exploring mechanisms associated with neuroinflammation in research settings. -
COX-2 Inhibitor
COX-2-IN-47 is a selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 value of 0.03 μM. This compound demonstrates notable anti-edema activity, making it valuable for research in inflammation and pain management studies. COX-2-IN-47 can be utilized to explore pathways involving COX-2 modulation in various biological contexts. -
COX1/2 Inhibitor
COX-1/2-IN-1 is a selective inhibitor of cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2), exhibiting significant anti-inflammatory properties. It demonstrates IC50 values of 13.9 ± 3.21 µM for COX-1 and 6.4 ± 0.74 µM for COX-2, effectively modulating prostaglandin synthesis. This compound is valuable for research related to pain, inflammation, and cardiovascular disorders. -
COX-2 Inhibitor
Clematomandshurica saponin B is a selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting significant inhibitory activity with an IC50 of 2.58 mM. This compound's ability to modulate COX-2 activity makes it valuable for studying inflammatory processes and analgesic pathways in various biological systems. It can serve as a tool for research applications focused on understanding pain mechanisms and developing anti-inflammatory therapies. -
COX-2 Inhibitor
Vitacoxib is a selective COX-2 inhibitor, functioning primarily through the blockade of cyclooxygenase-2 enzyme activity. This compound exhibits significant anti-inflammatory properties, making it a valuable tool for studying inflammatory diseases. Vitacoxib can also be employed in pain and fever research applications, contributing to a deeper understanding of these conditions. -
COX-2/sEH Inhibitor
COX-2/sEH-IN-1 is a dual inhibitor targeting cyclooxygenase-2 (COX-2) and soluble epoxide hydrolase (sEH), with IC50 values of 1.24 µM and 0.40 nM, respectively. This compound exhibits enhanced anti-inflammatory properties and significantly lowers cardiovascular risks. COX-2/sEH-IN-1 is suitable for research applications aimed at understanding inflammatory pathways and developing therapeutic strategies for cardiovascular diseases. -
COX-2 Inhibitor
COX-2-IN-13 is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 0.98 μM. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for research into inflammation and pain pathways. Additionally, COX-2-IN-13 demonstrates a favorable safety profile in in vivo acute toxicity studies, supporting its potential use in therapeutic applications. -
COX-2 Inhibitor
COX-2-IN-11 is a potent and selective inhibitor of cyclooxygenase-2 (COX-2), involved in the inflammatory response. This compound exhibits significant anti-inflammatory activity, making it valuable for studies on inflammation-related diseases. Research applications may include investigating the role of COX-2 in various pathological conditions and exploring therapeutic strategies for inflammatory disorders.
