Catalog No.
Product Name
Application
Product Information
Citations
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A2A Receptor Agonist
GW 328267 is an A2A receptor agonist that plays a pivotal role in modulating inflammatory responses. Its activation of the A2A receptor has potential applications in the study of asthma, chronic obstructive pulmonary disease (COPD), and upper respiratory inflammatory diseases. This compound serves as a valuable tool for researchers investigating the therapeutic implications of A2A receptor pathways in inflammatory conditions. -
Adenosine Receptor Antagonist
XCC is a 1,3,8-substituted xanthine derivative that functions as an adenosine receptor antagonist, exhibiting a Ki of 1.905 μM. This compound is valuable for studying adenosine receptor signaling pathways and their implications in various physiological processes and disease states. Research applications include pharmacological studies related to neuroprotection, inflammation, and cancer. -
Fluorinated Detergent
FLAC6 is a potent fluorinated detergent designed for the solubilization of membrane proteins, including the native adenosine receptor A2AR and two transporters, AcrB and BmrA. This reagent effectively preserves the structural and functional integrity of various membrane proteins, making it valuable for applications in structural biology and biophysical characterization. FLAC6 facilitates the study of GPCRs and transporters, enabling advancements in drug discovery and biochemical research. -
A2A Adenosine Receptor Agonist
2-Hexynyl-5′-N-ethylcarboxamidoadenosine is a selective agonist of the A2A adenosine receptor. It enhances intracellular cAMP levels and suppresses TNFα-induced MMP-3 release, indicating its anti-inflammatory potential. Furthermore, 2-Hexynyl-5′-N-ethylcarboxamidoadenosine promotes Aβ42 production in SH-SY5Y cells, making it a valuable tool for research on neurodegenerative diseases and receptor signaling pathways. -
Adenosine A2A Antagonist
ST4206 is a potent adenosine A2A receptor antagonist, exhibiting inhibitory constants (Kis) of 12 nM for the A2A receptor and 197 nM for the A1 receptor. This compound demonstrates significant biological activity, making it a valuable tool in the study of neurodegenerative disorders. ST4206 holds potential for advancing research in Parkinson's disease, providing insights into adenosine-mediated signaling pathways. -
Adenosine Receptor Antagonist
A2B receptor antagonist 1 is a selective antagonist of the A2B adenosine receptor. This compound demonstrates significant inhibition of adenosine-mediated signaling pathways, making it valuable in the investigation of adenosine receptor functions and their roles in various physiological and pathological conditions. A2B receptor antagonist 1 is applicable in research areas such as immunology, cancer biology, and neurobiology. -
Adenosine Receptor Antagonist
Sch412348 is a highly potent competitive antagonist of the human adenosine A2A receptor, exhibiting a Ki value of 0.6 nM and demonstrating over 1000-fold selectivity against other adenosine receptor subtypes. This selectivity makes Sch412348 a valuable tool for studying adenosine signaling pathways. It is particularly relevant in research focusing on neurological disorders, cardiovascular conditions, and cancer, where modulation of adenosine receptors may provide therapeutic insights. -
Adenosine Receptor Inhibitor
KF21213 is a selective adenosine A2A receptor inhibitor, demonstrating a high affinity with a Ki value of 3.0 nM. This compound is essential for research involving central nervous system (CNS) functions and disorders, providing valuable insights into adenosine receptor signaling pathways. Its precision in targeting A2A receptors makes it a suitable tool for studying their role in neuropharmacology and related therapeutic applications. -
Adenosine Receptor Agonist
UP202-56 is an adenosine receptor agonist that selectively activates adenosinergic signaling pathways. Its primary mechanism involves mimicking endogenous adenosine, leading to enhanced receptor-mediated cellular responses. This compound is essential for research applications focused on exploring adenosine-related physiological processes and the potential therapeutic implications in various diseases. -
Adenosine Receptor Antagonist
N-0861 racemate is a selective antagonist of the adenosine A1 receptor. It exhibits notable activity in modulating adenosine signaling pathways, making it valuable for research in neurology and cardiology. This compound is essential for investigating the physiological roles of adenosine receptors and their implications in various biological processes. -
CRFR Antagonist
DMP 904 is a noncompetitive antagonist of the corticotropin-releasing factor receptor (CRFR), effectively inhibiting CRF-stimulated adenylate cyclase activity and adrenocorticotropic hormone (ACTH) release. This compound demonstrates significant antidepressant and anxiolytic properties, making it a valuable tool for research in stress-related disorders and neuropsychiatric conditions. Its mechanism of action can provide insights into the therapeutic potential for anxiety and depression treatments. -
CGRP Agnalogue
[Tyr22] Calcitonin Gene Related Peptide, (22-37), rat is a CGRP analogue that targets the CGRP receptor and modulates adenylate cyclase activity. This peptide fragment, derived from the rat CGRP sequence, exhibits key biological activities associated with pain modulation and vasodilation. It is suitable for research applications studying neurogenic inflammation, cardiovascular regulation, and the pathophysiology of migraine headaches. -
Adenylate Cyclase Inhibitor
KUM 32 is a potent inhibitor of adenylate cyclase that functions by antagonizing epinephrine-induced platelet aggregation. By selectively binding to the alpha-2 adrenergic receptor on human platelets, KUM 32 modulates platelet activation and aggregation pathways. This compound is utilized in research focused on cardiovascular disease and hemostasis, providing insights into the mechanisms of platelet function. -
GCGR Antagonist
Glucagon receptor antagonist-7 is a potent inhibitor of the human glucagon receptor (hGCGR), demonstrating an IC50 of 181 nM for blocking the binding of 125I-labeled glucagon. With a KDB of 81 nM, it inhibits glucagon-stimulated adenylyl cyclase activity in CHO cells. This compound effectively reduces glucagon-mediated glycogenolysis in human hepatocytes and has been shown to lower blood glucose levels, making it a valuable tool for research in glucose metabolism and diabetes therapeutic strategies. -
sst2/sst5 Receptor Partial Agonist
Angiopeptin is a cyclic octapeptide analogue of somatostatin that acts as a partial agonist at the sst2 and sst5 receptors, exhibiting IC50 values of 0.26 nM and 6.92 nM, respectively. This compound effectively inhibits growth hormone secretion and reduces insulin-like growth factor-1 (IGF-1) production. Angiopeptin also modulates cellular signaling by inhibiting adenylate cyclase and stimulating extracellular acidification. Its unique properties make it a valuable tool for research into coronary atherosclerosis and related metabolic disorders. -
Adrenergic Receptor Agonist
Phenylephrine is a selective α1-adrenoceptor agonist that primarily functions as a decongestant. It exerts its biological activity by inducing vasoconstriction, leading to decreased nasal congestion. This compound is widely utilized in research applications related to cardiovascular studies, nasal physiology, and adrenergic receptor signaling pathways. -
Analgesic
α2AR agonist 2 is a selective agonist for the α2B adrenergic receptor, demonstrating an IC50 of 1.2 µM. This compound is primarily utilized in research focused on analgesic effects, particularly in the contexts of inflammatory and neuropathic pain. Its selective action makes it a valuable tool for studying pain modulation pathways and developing novel therapeutic strategies. -
β-Adrenoceptor Agonist
(-)-Isoproterenol hydrochloride is a potent β-adrenoceptor agonist. It primarily acts on β1 and β2 adrenergic receptors, resulting in increased heart rate and myocardial contractility. This compound is widely used in research related to cardiac function and ventricular remodeling, making it essential for studies exploring cardiovascular physiology and related therapeutic interventions. -
β3-AR Antagonist
SR59230A is a potent and selective antagonist of the β3-adrenergic receptor, demonstrating IC50 values of 40 nM, 408 nM, and 648 nM for β3, β1, and β2 receptors, respectively. Its ability to penetrate the blood-brain barrier makes it a valuable tool for exploring the physiological roles of β3-AR in the central nervous system. This compound is primarily utilized in research related to metabolic disorders, obesity, and cardiovascular diseases, providing insight into the therapeutic potential of β3-AR modulation. -
α1/β-adrenergic Receptors Antagonist
Labetalol is a competitive antagonist of α1-adrenergic and non-selective β-adrenergic receptors. This antihypertensive agent is orally bioavailable and effectively addresses hypertension by reducing peripheral vascular resistance with minimal impact on cardiac output. Labetalol is particularly relevant for research on cardiovascular diseases, including hypertension during pregnancy, and its ability to partially traverse the blood-brain barrier also makes it a candidate for neurological studies of vascular conditions. -
β3 Adrenergic Receptor Antagonist
L748337 is a selective β3-adrenergic receptor antagonist with a high affinity for the β3 receptor (Ki = 4.0 nM) compared to β1 (Ki = 390 nM) and β2 receptors (Ki = 204 nM). This compound predominantly couples to Gi proteins, leading to the activation of MAPK signaling pathways, which subsequently enhances the phosphorylation of Erk1/2 with a pEC50 value of 11.6. L748337 is applicable in research focused on cancer, nonalcoholic fatty liver disease (NAFLD), and various cardiovascular disorders. -
CXCR7 Antagonist
CXCR7 antagonist-1 functions as a CXCR7 antagonist by inhibiting the binding of the SDF-1 (CXCL12) and I-TAC (CXCL11) chemokines to the CXCR7 receptor. This inhibition plays a critical role in suppressing tumor cell proliferation and tumor growth, thereby providing potential therapeutic applications in cancer treatment. Additionally, CXCR7 antagonist-1 may be beneficial in the study and management of various inflammatory diseases and other pathologies associated with the CXCR7 pathway. -
β2-Adrenergic Receptor Blocker
Butaxamine hydrochloride is a specific antagonist of the β2-adrenergic receptor. This compound effectively inhibits the reduction of urine volume in ethanol-anesthetized, water-diuretic rats, demonstrating its role in regulating diuresis. Butaxamine hydrochloride is valuable for studying β2-adrenergic receptor signaling and its implications in renal function and fluid regulation. -
β/α-1 Blocker
(S)-Carvedilol is a non-selective β/α-1 blocker that primarily targets adrenergic receptors. This compound demonstrates protective effects against the vascular and cardiac toxicity induced by Doxorubicin (DOX). It is utilized in research related to cardioprotection and the mitigation of chemotherapy-related side effects. -
α Blocker
(R)-Carvedilol primarily targets alpha (α) adrenergic receptors, acting as an α-blocker while exhibiting no β-receptor activity. This compound is noted for its ability to inhibit spontaneous Ca2+ waves, thereby contributing to its cardioprotective effects. Research applications for (R)-Carvedilol include the study of stress-induced ventricular tachycardia and the potential inhibition of UV-induced skin tumor development, suggesting its utility in cancer research and cardiovascular studies. -
α2A Agonist
Guanfacine functions as a selective α2A adrenergic receptor agonist, exhibiting potent noradrenergic activity. Its mechanism leads to reduced sympathetic outflow, resulting in hypotension and sedation. Guanfacine is utilized in research related to prefrontal cortex cognitive disorders, including Tourette’s syndrome and attention deficit hyperactivity disorder (ADHD), making it valuable for understanding the pharmacological modulation of these conditions. -
β1-AR Agonist
Dobutamine is a synthetic catecholamine that acts primarily as a selective agonist of the β1-adrenergic receptor (β1-AR). It is known to enhance cardiac output and improve conditions of hypoperfusion by elevating heart rate and contractility. Dobutamine is utilized in various research applications, including studies on cardiac function, mechanisms of heart failure, and other cardiovascular disorders. -
Adrenergic Receptor Agonist
Xamoterol hemifumarate is a selective and potent agonist of the beta-1 adrenergic receptor. It has significant potential for studying arrhythmogenesis and elucidating the relationship between β1-adrenergic stimulation and the potassium ion channel IKr. This compound is valuable for research applications focused on cardiac function and the mechanisms underlying arrhythmic conditions. -
A2B Receptor Antagonist
PSB-603 is a potent and highly selective antagonist of the A2B adenosine receptor, exhibiting a Ki value of 0.553 nM. This compound demonstrates minimal affinity for human and rat A1, A2A, and human A3 receptors at concentrations up to 10 μM. PSB-603 is primarily utilized in research exploring adenosine receptor signaling pathways and their implications in various physiological and pathological processes. -
Adenosine A3 Receptor Antagonist
MRS 1523 is a selective antagonist of the adenosine A3 receptor, demonstrating Ki values of 18.9 nM and 113 nM for human and rat A3 receptors, respectively. It exhibits significant selectivity with 140-fold and 18-fold greater affinity for the A3 receptor over A1 and A2A receptors in rat models. MRS 1523 has been shown to produce an antihyperalgesic effect by blocking N-type calcium channels and inhibiting action potentials in isolated rat dorsal root ganglion (DRG) neurons, making it valuable for research in pain mechanisms and receptor activity. -
A2B Adenosine Receptor Antagonist
PSB-1115 is a selective antagonist of the A2B adenosine receptor, providing a valuable tool for investigating adenosine signaling pathways. It effectively inhibits the contraction induced by 2,4,6-trinitrobenzenesulfonic acid (TNBS) in response to acetylcholine (ACh). This compound is relevant for research in inflammation, smooth muscle function, and potential therapeutic interventions targeting adenosine receptors. -
A3 Adenosine Receptor Antagonist
DPTN dihydrochloride is a potent and selective antagonist of the A3 adenosine receptor (A3AR), exhibiting Ki values of 1.65 nM for human, 9.61 nM for mouse, and 8.53 nM for rat receptors. This compound is valuable for research applications investigating the physiological roles of A3AR in various biological processes, including immunomodulation and tumor growth regulation. DPTN's selectivity makes it an important tool for studies aimed at elucidating the therapeutic potential of A3AR modulation in human and animal models. -
A3 Receptor Antagonist
MRS1220 is a highly potent and selective antagonist of the human A3 adenosine receptor (hA3AR), exhibiting a Ki value of 0.59 nM. This compound is of significant interest for research related to diseases of the central nervous system and has demonstrated the ability to reduce glioblastoma tumor size and inhibit angiogenesis in vivo. Its distinct action on the A3 receptor makes it a valuable tool for studying mechanisms associated with neuroprotection and tumor biology. -
GPCRs/Adenosine Modulator
SCH-202676 hydrobromide is an allosteric modulator targeting G protein-coupled receptors (GPCRs), specifically the adenosine receptor. This compound demonstrates notable antiviral activity and effectively inhibits the 3CLpro enzyme in a time-dependent manner, with an IC50 value of 0.655 μM. Its unique mechanism makes it a valuable reagent for research applications focused on GPCR modulation and antiviral studies. -
Adenosine Receptor Activator
Adenosine-2'-monophosphate (2'-AMP) functions primarily as an adenosine receptor activator. This compound is metabolized to extracellular adenosine through the extracellular 2’,3’-cAMP-adenosine pathway, playing a crucial role in modulating immune responses. Research indicates that 2'-AMP inhibits lipopolysaccharide (LPS)-induced production of TNF-α and CXCL10 via activation of the A2A receptor, making it a valuable tool in studies of inflammation and immune regulation. -
Adenosine Receptor Antagonist
7-Methylxanthine is a non-selective adenosine receptor antagonist that serves as an orally active methyl derivative of xanthine. This compound has demonstrated key biological activities, including anti-myopia effects, making it valuable for research in visual function and ocular health. Additionally, 7-Methylxanthine is a component of human urinary calculi, highlighting its relevance in studies related to purine metabolism and urolithiasis. -
A2A Receptor Antagonist
Inupadenant is a potent and selective antagonist of the A2A adenosine receptor, primarily utilized for its immunomodulatory effects. This compound enhances the humoral immune response and exhibits promising anti-tumor activity, making it a valuable tool in cancer research and immune response studies. Notably, Inupadenant does not penetrate the blood-brain barrier, which may limit its central nervous system effects. -
A2A Inverse Agonist
Sipagladenant is an orally active inverse agonist of the adenosine A2A receptor. It is primarily utilized in research related to frontal lobe dysfunction, offering insights into the modulation of adenosine signaling pathways. This compound may be useful in elucidating the role of A2A receptors in various neurological conditions. -
A1 Adenosine Receptor Antagonist
PSB36 is a selective antagonist of the A1 adenosine receptor, exhibiting a Ki of 0.12 nM and Kd of 0.7 nM. This compound has demonstrated efficacy in reducing formalin- and carrageenan-induced edema in murine models, alongside a decrease in pain-related behaviors without causing local paw effects. Furthermore, PSB36 prolongs the action potential duration (APD90) of rat and human atria, enhances frequency-dependent atrial effective refractory period (ERP), raises diastolic thresholds, and mitigates the duration of atrial fibrillation episodes. PSB36 is applicable in research investigating inflammatory pain, hyperalgesia, edema, and atrial fibrillation. -
Adenosine A2A Receptor Antagonist
(E)-8-(3-Chlorostyryl)caffeine is a selective antagonist of the adenosine A2A receptor, which plays a significant role in neuronal signaling. In addition to its primary action, this compound also inhibits monoamine oxidase B (MAO-B) with a Ki value of 70 nM through a mechanism independent of its effects on the A2A receptor. Due to its dual activity, (E)-8-(3-Chlorostyryl)caffeine is of particular interest in research related to Parkinson's disease and other neurological disorders. -
A2AAR Agonist
UK-432097 is a highly potent and selective agonist of the A2A adenosine receptor (A2AAR), exhibiting a pKi of 8.4 for human A2AAR. This compound demonstrates significant anti-inflammatory and anti-aggregatory properties, making it a valuable tool for studying inflammatory pathways. UK-432097 is particularly relevant for research applications related to chronic obstructive pulmonary disease (COPD) and other conditions influenced by A2A receptor signaling. -
A2BAR Antagonist
ISAM-140 is a potent and selective antagonist of the A2B adenosine receptor, exhibiting a Ki of 3.49 nM. This compound is valuable for research applications focused on adenosine signaling pathways and their role in various physiological processes. Its high specificity makes it an essential tool for studying the therapeutic potential of A2B receptor modulation in disease models. -
Adenosine Receptor Agonist
(-)-N6-Phenylisopropyl adenosine is a selective agonist for the A1 adenosine receptor. This compound effectively inhibits K+-induced Ca2+ uptake with an IC50 of 0.5 µM. It has been shown to protect against ischemia-induced ventricular arrhythmias and atrial fibrillation, while also exacerbating symptoms associated with ethanol withdrawal. Additionally, (-)-N6-phenylisopropyl adenosine exhibits notable analgesic properties, making it a valuable tool for research in cardiovascular and pain-related studies. -
A3 Adenosine Receptor Antagonist
MRS-1191 is a selective antagonist of the A3 adenosine receptor, exhibiting a KB value of 92 nM and a Ki value of 31.4 nM for the human A3 receptor. This compound demonstrates an IC50 of 120 nM in CHO cells, making it an effective tool for investigating A3 receptor-related biological pathways. Additionally, MRS-1191 features an alkyne group, enabling its use as a click chemistry reagent through copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
Adenosine A2A Receptor Antagonist
ANR94 is a potent and selective antagonist of the adenosine A2A receptor (AA2AR), exhibiting a Ki value of 46 nM for human AA2AR. This compound demonstrates strong biological activity that makes it a significant tool for studying the role of AA2AR in various physiological processes. ANR94 is particularly relevant for research focused on Parkinson's disease and related neurodegenerative disorders. -
AR Inhibitor
Adenosine receptor inhibitor 1 is a highly selective antagonist of adenosine receptors, demonstrating Ki values of >1000 nM for A1AR, A2BAR, and A3AR, and 68.5 nM for A2AAR. This compound exhibits significant antinociceptive and anti-inflammatory properties, contributing to its potential as a peripheral analgesic. Research applications include the investigation of mechanisms underlying cancer and neurodegenerative diseases, making it a valuable tool for advancing scientific understanding in these areas. -
Adenosine Receptor Antagonist
Xanthine amine congener hydrochloride is a non-selective adenosine receptor antagonist. It exhibits significant biological activity, inducing convulsions in murine models, which may be useful for studying the role of adenosine receptors in neurological disorders. This reagent serves as a valuable tool for researchers investigating adenosine receptor signaling pathways and their implications in various physiological and pathological conditions. -
Adenosine Receptors Antagonist
9-Ethyladenine acts as a competitive antagonist of adenosine receptors, specifically targeting A1, A2A, and A3 subtypes. This compound demonstrates high affinity for these receptors, with Ki values of 27 nM, 46 nM, and 86 nM respectively. Importantly, 9-Ethyladenine exhibits no significant inhibitory effect on adenine phosphoribosyltransferase (APRT), making it suitable for studies involving adenosine receptor-related disorders, including nervous system diseases. Researchers can utilize this compound to further investigate the roles of adenosine receptors in various biological contexts. -
Adenosine Receptor Antagonist
VUF-5574 is a selective antagonist of the adenosine A3 receptor, exhibiting a Ki value of 4.03 nM for the recombinant human receptor. This compound is beneficial for studies investigating adenosine signaling pathways and their implications in various physiological processes. Its use as an antagonist makes it a valuable tool for elucidating the role of adenosine receptors in disease models and therapeutic research. -
Adenosine Receptor Antagonist
MRS-3777 hemioxalate is a selective antagonist of the adenosine A3 receptor, known for its role in various physiological processes. This compound inhibits adenosine signaling, making it a valuable tool for investigating the functions of adenosine receptors in cellular systems. It has potential applications in researching inflammatory responses, cancer biology, and cardiovascular diseases.
