Catalog No.
Product Name
Application
Product Information
Citations
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σ Receptor Agonist
threo-Ifenprodil hemitartrate is a sigma (σ) receptor agonist, exhibiting Kis of 59.1 nM and 2 nM for σ1 and σ2 receptors, respectively. This compound also acts as a NR2B subunit-selective NMDA receptor antagonist, with an IC50 of 0.22 μM, and demonstrates inhibition of the hERG potassium channel with an IC50 of 88 nM, indicating potential antiarrhythmic activity. threo-Ifenprodil hemitartrate serves as a valuable tool in neuropharmacology and cardiovascular research. -
IBAT Inhibitor
Elobixibat hydrate is an orally active inhibitor of the intestinal bile acid transporter (IBAT), demonstrating potent activity with IC50 values of 0.53 nM for human IBAT, 0.13 nM for mouse IBAT, and 5.8 nM for canine IBAT. This compound has been shown to effectively lower LDL cholesterol levels, enhance serum GLP-1 concentrations, and promote colonic motility. Elobixibat hydrate is valuable for research applications related to chronic idiopathic constipation (CIC), dyslipidemia, non-alcoholic fatty liver disease, and the study of liver tumors, particularly in elderly populations. -
P/Q Type Ca2+ Channel Blocker
ω-Agatoxin IVA is a highly selective blocker of P/Q type calcium channels (Cav2.1), with IC50 values of 2 nM and 90 nM. This compound effectively inhibits glutamate exocytosis and calcium influx triggered by elevated potassium levels. Additionally, ω-Agatoxin IVA suppresses capsaicin-induced CGRP release and associated vasodilation. It is valuable for investigations into neurological and cardiovascular diseases, contributing to the understanding of calcium channel modulation in these contexts. -
Racemate of NNC 55-0396
(Rac)-NNC 55-0396 is a racemic mixture that targets the dopamine D2 receptor. This compound is of significant interest in neurological research due to its potential role in modulating dopaminergic signaling pathways. It is commonly utilized in studies investigating the pharmacological effects of dopamine receptor antagonists in various neurological disorders. -
Cholecystokinin
Cholecystokinin-J is a cholecystokinin peptide that primarily targets the cholecystokinin receptor. It is known to stimulate Ca2+ release, playing a significant role in various physiological processes such as digestion and satiety. This reagent is valuable for research applications in gastrointestinal physiology and neurobiology, facilitating studies on CCK-related pathways and functions. -
Stable Isotope
O-Desmethyl carvedilol-d5 is a deuterium-labeled derivative of O-Desmethylcarvedilol, a potent active metabolite of the non-selective β-adrenergic receptor antagonist Carvedilol. This compound exhibits inhibitory effects on store-overload-induced calcium release in HEK293 cells expressing the RyR2 R4496C mutation, with an IC50 of 7.62 μM. Additionally, O-Desmethyl carvedilol-d5 contributes to cardiovascular research by attenuating heart rate increases and stabilizing diastolic blood pressure in response to Isoproterenol in conscious rabbit models, demonstrating ED50 values of 32 and 5 μg/kg, respectively. -
Lipid
DMG-PEG is a lipid compound that enhances the hydrophilicity and electrical neutrality of lPEI/DNA nanoparticles, facilitating improved transport and diffusivity in the gastrointestinal mucus layer. This pegylated lipid is pivotal in formulating liposomes for siRNA delivery, significantly increasing transfection efficiency. In vivo studies demonstrate that nucleic acid nanoparticles coated with DMG-PEG effectively maintain elevated levels of glucagon-like peptide-1 (GLP-1) expression in liver, lung, and intestinal tissues of type II diabetic mouse models, while also regulating blood glucose levels. Additionally, DMG-PEG serves as an effective component in the preparation of lipid nanoparticles for mRNA therapeutics. -
MAGL Inhibitor
OMDM169 is a selective inhibitor of monoacylglycerol lipase (MAGL), effectively increasing the levels of 2-arachidonoylglycerol (2-AG) in biological systems. This compound demonstrates significant analgesic properties through the indirect activation of cannabinoid receptors. OMDM169 exhibits an effective concentration of 0.13 μM, making it a valuable tool for research focused on pain modulation and cannabinoid receptor signaling pathways. -
HIF Inhibitor
Arylsulfonamide 64B is a potent inhibitor of hypoxia-inducible factor (HIF). This compound effectively suppresses hypoxia/HIF-mediated expression of key oncogenes such as c-Met and CXCR4, thereby demonstrating significant anti-tumor activity. Arylsulfonamide 64B is particularly relevant for research focused on uveal melanoma, as it has been shown to reduce primary tumor growth and metastasis in mouse models. -
Bile Acid Sequestrant
Colesevelam hydrochloride is a bile acid sequestrant that primarily acts by binding bile acids in the gastrointestinal tract, leading to the formation of nonabsorbable complexes. This action interrupts enterohepatic recirculation and enhances fecal bile acid elimination. In addition to lowering lipids, colesevelam modulates FXR, TGR5, and CYP7A1 activities, which in turn activates cAMP signaling and promotes GLP-1 release. Its applications in research include investigations into type 2 diabetes mellitus, hypercholesterolemia, and alcohol-related liver disease, while also influencing hepatic lipid and glucose metabolism. -
Platelet Aggregation Inhibitor
Myrianthic acid is a pentacyclic triterpenoid that functions as a platelet aggregation inhibitor. Isolated from the root wood of Myrianthus arboreus and the leaves of Campsis grandiflora, it effectively inhibits adrenaline-induced platelet aggregation, demonstrating an IC50 of 46.2 μM. This compound is valuable for research applications focused on thrombosis and related cardiovascular disorders. -
Endogenous Metabolite
9(R)-HODE is a monohydroxy fatty acid and an endogenous metabolite of linoleic acid, generated through the enzymatic actions of cyclooxygenase (COX) and lipoxygenase (LO). This compound is known to promote chemotaxis and elevate the expression of chemokine receptors CCR9 and CXCR4 in immune cells. Additionally, 9(R)-HODE effectively inhibits interleukin-6 (IL-6) release in primary human monocytes and suppresses CD3α- and CD28-induced proliferation in isolated human peripheral blood lymphocytes at a concentration of 25 μg/mL, making it a valuable tool for studying immune responses and inflammatory processes. -
2-arachidonoylglycerol derivative
1-Monoarachidin is a 2-arachidonoylglycerol derivative that primarily acts as a modulator of cannabinoid receptors. This fatty acid plays a crucial role in the endocannabinoid system, contributing to various biological processes such as inflammation and neuroprotection. It is utilized in research to investigate the physiological effects of endocannabinoids and their potential therapeutic applications in neurological and inflammatory disorders. -
O-Alkyl-N-acyloxy Homologues
Oxy-Arachidonoyl ethanolamide is an O-alkyl-N-acyl oxime derivative that acts on O-Alkyl-N-acyl homologues. This compound exhibits significant biological activity, particularly in the modulation of endocannabinoid systems. It is employed in research applications focusing on cannabinoid receptor signaling, lipid metabolism, and neuroprotective studies, illuminating potential therapeutic pathways for various neurological diseases. -
Endogenous Metabolite
N-Methylarachidonamide is an analog of the endogenous cannabinoid anandamide, primarily targeting the central cannabinoid receptor (CB1). This compound exhibits a binding affinity with a Ki value of 60 nM for CB1, influencing various physiological processes. Additionally, it effectively inhibits rat glial gap junction cell-cell communication by 100% at a concentration of 50 μM. As such, N-Methylarachidonamide is a valuable tool for research exploring cannabinoid receptor signaling and its implications in neurobiology and related fields. -
FAAH Inhibitor
3-Decyl-5,5'-diphenyl-2-thioxo-4-imidazolidinone is a potent inhibitor of fatty acid amide hydrolase (FAAH) with a pI50 of 5.89. This compound exhibits significant activity against endocannabinoids and lipid mediators, making it relevant for studies in pain management, inflammation, and cannabinoid signaling pathways. Its limited affinity for cannabinoid receptors CB(1) and CB(2) allows for targeted research into FAAH-related physiological processes without direct receptor modulation. -
NR4A1 Inhibitor
Glycerol kinase, microorganism functions as an NR4A1 inhibitor by directly binding to and inhibiting the transcription factor NR4A1, which plays a critical role in hepatic gluconeogenesis. This inhibition leads to reduced blood glucose levels and positively influences UCP1 expression through the β-adrenergic receptor-cAMP-CREB signaling pathway, promoting the browning of white adipose tissue and enhancing thermogenesis. Additionally, it modulates intracellular fatty acid composition and energy metabolism. Research using glycerol kinase in diabetic mouse models has demonstrated its ability to counteract NR4A1-induced hyperglycemia, indicating its potential applications in diabetes and obesity studies. -
Endogenous Metabolite
AZD-3199 is an ultra-long-acting beta2 adrenergic agonist primarily targeting the beta2 adrenergic receptor. It exhibits significant bronchodilator activity, making it a candidate for therapeutic use in asthma and chronic obstructive pulmonary disease (COPD) research. Its prolonged action facilitates investigations into novel treatment strategies for managing these respiratory conditions. -
Drug Derivative
Bmapn is a drug derivative with impactful interactions on dopamine signaling pathways. It exhibits rewarding and reinforcing properties by decreasing dopamine transporter levels and enhancing dopamine receptor D2 gene expression specifically in the striatum. This compound is valuable for research applications studying addiction, neuropharmacology, and the modulation of dopaminergic systems. -
Stable Isotope
Boc-Leu-OH·H2O-13C is a stable isotope-labeled derivative of N-Boc-L-leucine, featuring a carbon-13 (13C) label. This amino acid derivative, protected with a Boc group, serves as an essential building block for the synthesis of peptides, such as L-prolyl-L-leucyl-glycinamide, which exhibit modulatory activity on dopamine receptors. It is valuable for applications in peptide research, metabolic studies, and tracer experiments utilizing stable isotopes. -
Histamine N-methyltransferase
Histamine N-methyltransferase, rat is a biocatalyst that functions primarily by catalyzing the N-methylation of histamine. This enzyme plays a critical role in the metabolism of histamine, contributing to the regulation of physiological processes such as inflammatory responses and neurochemical signaling. Research applications include enzyme engineering aimed at optimizing reaction kinetics, enhancing substrate specificity, and improving enzyme stability under varying pH conditions, potentially facilitating dynamic control of enzymatic activity for various experimental needs. -
Activation Peptide
Enterostatin (rat) is an activation peptide of procolipase that plays a significant role in modulating fat intake. This peptide selectively reduces body fat consumption and lowers serum cholesterol levels through a cholecystokinin 1 (CCK1) receptor-dependent mechanism. It serves as a valuable tool for research on energy balance, appetite regulation, and metabolic disorders. -
N-acylserinol Compound
Myristoyl ethanolamide, an N-acylserinol compound, functions as a bioactive lipid signaling molecule. It is involved in modulating various biological processes, including inflammation and pain perception. Myristoyl ethanolamide serves as a valuable tool in research applications focused on lipid metabolism, neuromodulation, and the study of cannabinoid receptor interactions. This compound can enhance the understanding of endocannabinoid signaling pathways and their implications in physiological and pathological conditions. -
Blood Platelet Aggregation Inhibitor
Ent-8-Iso-15(S)-prostaglandin F2α is a potent inhibitor of blood platelet aggregation. This compound exhibits superior activity compared to its isomer, 8-Isoprostaglandin F2α, in whole blood assays, making it a valuable tool for studying platelet function and related cardiovascular research. Its mechanism of action can aid in the exploration of therapeutic strategies for conditions associated with abnormal platelet aggregation. -
Endogenous Metabolite
8-(3-Chlorostyryl)caffeine is a selective antagonist of the A2a adenosine receptor, demonstrating a significant 520-fold selectivity in radioligand binding assays conducted in rat brain. It effectively inhibits adenylylase with a 22-fold selectivity in rat chromaffin cells. Co-administration with the A1-selective antagonist CPX has been shown to enhance exercise activity. Additionally, 8-(3-Chlorostyryl)caffeine exhibits potent inhibitory activity against MAO-B in primate mitochondrial systems. This compound serves as a valuable tool for studying adenosine receptor signaling and its effects on physiological processes. -
Endogenous Metabolite
Palmitoleoyl ethanolamide (POEA) is an endogenous fatty amide that functions primarily as a signaling molecule through the activation of cannabinoid receptors. It has been shown to exhibit anti-inflammatory and analgesic properties, making it relevant for research in pain management and inflammatory disorders. POEA's involvement in metabolic processes also positions it as a valuable target for studies in obesity and metabolic syndrome. -
Endogenous Metabolite
5-OAHSA is an endogenous metabolite that functions as a lipid mediator. It is known to lower blood glucose levels, enhance glucose tolerance, and stimulate the secretion of glucagon-like peptide-1 (GLP-1) and insulin. 5-OAHSA is valuable for research applications focused on metabolic regulation and inflammation modulation. -
Endogenous Metabolite
Hydroxy bosentan is an endogenous metabolite derived from Bosentan, primarily processed by the cytochrome P450 system in the liver. This compound retains 10%-20% of Bosentan's pharmacological activity, serving as a significant contributor to the overall therapeutic effects of the parent compound. Hydroxy bosentan is useful in research focused on metabolic pathways and the pharmacokinetics of endothelin receptor antagonists. -
Histamine Methylated Product
3-Methylhistamine dihydrochloride is a methylated derivative of histamine that serves as a significant biomarker in the study of immune responses. This compound has been shown to be upregulated in vaccinated murine models, making it useful for research applications focused on immunological studies and histamine-related pathways. Its role in the modulation of immune activity positions it as a valuable reagent in exploring allergic reactions and other histamine-mediated processes. -
Ligand for Target Protein for PROTAC
Rimonabant carboxylic acid is a ligand used for the targeted protein degradation (PROTAC) approach by engaging with the target protein. This compound plays a crucial role in synthesizing PROTAC CB1R Degrader-1, facilitating the study of cannabinoid receptor biology and influencing metabolic processes. It serves as a valuable tool for researchers investigating innovative therapeutic strategies for conditions related to the endocannabinoid system. -
MAO-A And 5-HT-uptake Inhibitor
Sercloremine hydrochloride is a selective and reversible inhibitor of monoamine oxidase A (MAO-A) and serotonin (5-HT) uptake. This compound is primarily utilized in research related to depression, offering insights into the modulation of serotonin levels and its effects on mood regulation. Its dual mechanism of action makes it valuable for exploring therapeutic approaches in depressive disorders. -
5-HT Reuptake Inhibitor
Clomipramine is a potent 5-HT reuptake inhibitor with an IC50 value of 1.5 nM. As a tricyclic antidepressant, it is primarily utilized in research investigating the mechanisms of depression and obsessive-compulsive disorder (OCD). Its ability to influence serotonin levels makes it a valuable tool for studying various neuropsychiatric conditions. -
5-HT2A Antagonist
Glemanserin is a potent and selective antagonist for the serotonin receptor 5-HT2A, exhibiting nanomolar affinity in various species (Ki values of 2.89, 0.54, and 2.5 nM for rat, rabbit, and human 5-HT2A, respectively). This compound is primarily utilized in neuropharmacological research to study the role of 5-HT2A receptors in various physiological and pathological conditions. Its antagonistic activity contributes to investigations into mood disorders, anxiety, and other CNS-related ailments. -
5-HT/NE Reuptake Inhibitor
Dextromilnacipran is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor, derived from the enantiomeric form of milnacipran. This compound also functions as a human alpha-adrenergic receptor antagonist, exhibiting an IC50 value of 3.4 μM. Dextromilnacipran is primarily utilized in research applications targeting mood disorders and neuropharmacology, facilitating investigations into its psychiatric and physiological effects. -
5-HT Uptake Blocker
Indalpine, a selective 5-HT uptake blocker, demonstrates significant potency in inhibiting serotonin transport. With an IC50 value of 36 μM, it effectively displaces ^3H-5-HT bound to brain membranes. This compound may have applications in the study of antidepressant mechanisms and is valuable for research in neuropharmacology. -
Stable Isotope
Dextromilnacipran-d6 is a deuterium-labeled analog of Dextromilnacipran, a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor. This compound also acts as a human alpha-adrenergic receptor antagonist, exhibiting an IC50 of 3.4 μM. Dextromilnacipran-d6 is a valuable tool for metabolic and pharmacokinetic studies, providing insights into the behavior and efficacy of 5-HT/NE reuptake inhibitors in various research contexts. -
Noradrenaline And 5-HT Uptake Blocker
Clemeprol is an orally active noradrenaline and 5-HT uptake blocker. It effectively inhibits the depletion of brain noradrenaline induced by 6-Hydroxydopamine and demonstrates a dose-dependent inhibition of reserpine-induced hypothermia. Clemeprol is applicable in the investigation of depression and related neurochemical pathways. -
5-HT1 Agonist
2-Aminotetralin is a selective agonist of the serotonin 5-HT1 receptor subtypes, including 5-HT1A, 5-HT1B, and 5-HT1D. This compound demonstrates high affinity, with a Ki value of 25 nM or lower, and exhibits significant stereoselectivity, showing over a 50-fold preference for specific receptor configurations. 2-Aminotetralin is utilized in research exploring serotonin signaling pathways and their implications in neuropharmacology and mood disorders. -
5-HT Transporter Inhibitor
6-Nitroquipazine is a highly potent and selective inhibitor of the serotonin transporter (5-HT transporter), exhibiting a Ki value of 0.17 nM. This compound significantly impacts serotonin reuptake, making it a valuable tool for investigating the pathophysiology and treatment of psychiatric disorders, including depression. Its ability to modulate serotonin levels can be instrumental in research aimed at understanding mood regulation and therapeutic interventions in related conditions. -
σ-Receptor Ligand
Igmesine hydrochloride is a potent σ-receptor ligand that exhibits the ability to inhibit colonic electromechanical activity stimulated by emotional stress. This compound effectively counteracts the enhancement of colonic motility induced by dopamine and centrally injected D1 or D2 receptor agonists. Additionally, Igmesine hydrochloride disrupts the colonic motility responses prompted by corticotropin-releasing factor (CRF), likely through mechanisms involving central cholecystokinin (CCK) release or activation of supraspinal CCK pathways, making it a valuable tool for studying gastrointestinal responses to stress and neurotransmitter signaling. -
Anticholinergic
Piperilate is an anticholinergic agent that functions primarily as a PAF antagonist through its hetrazepine derivatives. This compound exhibits significant biological activity in the treatment of bronchial asthma and demonstrates hypotensive effects. Additionally, Piperilate has been shown to effectively rescue mice from organophosphate poisoning, making it a valuable reagent for research into respiratory conditions and toxicology. -
DA/NE/5-HT Inhibitor
Tesofensine is a triple monoamine reuptake inhibitor targeting dopamine (DA), norepinephrine (NE), and serotonin (5-HT). It effectively inhibits the reuptake of these neurotransmitters in the synaptic cleft, exhibiting IC50 values of 6.5 nM for DA, 1.7 nM for NE, and 11 nM for 5-HT. Tesofensine is primarily studied for its potential as an anti-obesity agent and may be useful in related central nervous system research applications. -
PN-1 Agonist
Serpinin is an agonist of the protease inhibitor Nexin-1 (PN-1), promoting its expression through the cAMP-PKA-Sp1 signaling pathway, which enhances granule biogenesis in endocrine cells. This compound is instrumental in studying the regulation of secretory functions and demonstrates selectivity for β-adrenergic receptors. By interacting with β1-adrenergic receptors, Serpinin activates the AC-cAMP-PKA pathway, crucial for regulating myocardial systolic and diastolic function. Additionally, pGlu-serpinin has been shown to upregulate Bcl2 mRNA transcription, contributing to its neuroprotective effects. -
Anti-platelet Aggregation Agent
Antiplatelet agent 3 is a potent anti-platelet aggregation agent that inhibits platelet aggregation induced by ADP, AA, and COL, with IC50 values of 2.55, 3.22, and 2.09 mg/mL, respectively. This compound demonstrates significant biological activity advantageous for elucidating mechanisms involved in thrombosis and other cardiovascular conditions. Antiplatelet agent 3 is suitable for use in cardiovascular disease research, providing insights into therapeutic strategies for managing platelet-related disorders. -
β-Glucuronidase Inhibitor
β-Glucuronidase-IN-5 is a selective inhibitor of β-glucuronidase with an IC50 value of 39.8 μM. This compound demonstrates low cytotoxicity in PC-3 cells, with an IC50 greater than 30 μM, and shows no affinity for adenosine receptors A₁ and A₂A. β-Glucuronidase-IN-5 is useful for investigating diseases associated with overexpression of β-glucuronidase, including colon cancer, arthritis, and complications related to AIDS. -
PAF C-16 Precursor/Metabolite
Lyso-PAF C-16 is a key precursor and metabolite of 1-O-hexadecyl-2-acetyl-sn-glycero-3-phosphocholine (PAF C-16). It serves as a substrate in the remodeling pathway for the formation of PAF C-16 and is also involved in the selective acylation with arachidonic acid through a CoA-independent transacylase. This compound is beneficial for research into lipid metabolism and the roles of bioactive lipids in various biological processes. -
PAFAH1b2/1b3 Inhibitor
P11 is a selective inhibitor of platelet-activating factor acetylhydrolases (PAFAHs) 1b2 and 1b3, demonstrating significant impairment of cancer cell survival. With IC50 values of approximately 40 nM for PAFAH1b2 and 900 nM for PAFAH1b3, P11 is a valuable tool for investigating the role of these enzymes in cancer biology and related research applications, including studies focused on cell proliferation and apoptosis. -
PROTAC Linker
2-[4-(Aminomethyl)triazol-1-yl]ethanamine is a specialized PROTAC linker that serves as a crucial component in targeted protein degradation strategies. This compound facilitates the synthesis of PROTAC CB1R Degrader-1, enabling the effective modulation of cannabinoid receptor 1 (CB1R) levels. Its application in research supports investigations into protein homeostasis and therapeutic approaches for various diseases. -
H3 Agonist
Immepip dihydrobromide acts as a selective agonist for the H3 histamine receptor. It is known to attenuate cortical histamine release, thereby influencing neurotransmitter dynamics. This compound is applicable in the study of neurological disorders, providing insights into histaminergic system modulation and its potential therapeutic effects. -
ARα2c Inhibitor
BAY-2925976 is an α2C adrenergic receptor (ARα2C) inhibitor that selectively blocks receptor activity. This compound is primarily utilized in research related to obstructive sleep apnea (OSA), providing insights into its underlying mechanisms and potential therapeutic approaches. BAY-2925976 aids in elucidating the role of ARα2C in respiratory regulation and sleep disorders.
