Catalog No.
Product Name
Application
Product Information
Citations
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Adenosine Receptor Agonist
MRS8028 is a selective agonist for the A3 adenosine receptor (A3AR), demonstrating a binding affinity with a Ki of 2.44 nM. This compound exhibits potential therapeutic effects in the modulation of ischemia and inflammatory diseases, making it a valuable tool for researchers investigating adenosine signaling pathways in pathological conditions. Its efficacy in targeting A3AR may provide insights into novel treatment approaches for related diseases. -
A₂B Adenosine Receptor Antagonist
SYAF080 is a selective antagonist of the human A₂B adenosine receptor (hA₂B AdoR), exhibiting a binding affinity with a Ki of 23.6 nM and a KB of 25.2 nM. This compound does not exhibit inhibition of human CYP450 cytochromes, making it suitable for pharmacological studies. SYAF080 is valuable for research focused on inflammation, metabolic disorders, and cardiovascular diseases, providing insights into the therapeutic potential of A₂B receptor modulation. -
A1AR Antagonist
A1AR Antagonist 1 is a selective antagonist of the A1 adenosine receptor, exhibiting Ki values of 2.08 nM for human A1, 6.91 nM for human A2A, and 31.2 nM for human A2B receptors. This compound demonstrates significant biological activity in modulating adenosine signaling pathways, making it valuable for research applications related to cardiovascular diseases, neuroprotection, and cancer progression. Its potency and selectivity provide a useful tool for studying the role of A1AR in various biological processes. -
A1-Adenosine Antagonist
Naxifylline is a potent and selective A1-adenosine antagonist, exhibiting Ki values of 0.67 nM for rat A1 receptors and 0.45 nM for cloned human A1 receptors. This compound serves as a potassium-sparing diuretic, making it useful for investigating edema related to congestive heart failure. Naxifylline's mechanism of action provides critical insights into adenosine receptor signaling and its implications in cardiovascular research. -
Hypnotic Agent
YGZ-331 is a hypnotic agent that primarily targets adenosine receptors A1R and A2aR. It enhances GABA levels and exerts a sedative-hypnotic effect by inhibiting the phosphorylation of CaMKII (pCaMKII). This compound has demonstrated the ability to reduce spontaneous motor activity in mice, making it a valuable tool for research into sedative mechanisms and sleep-related studies. -
A2A/A3 AR Antagonist
A2A/A3 AR antagonist-1 is a dual antagonist of the human A2A and A3 adenosine receptors, exhibiting dissociation constants (Kis) of 90 nM and 31.8 nM for hA2A AR and hA3 AR, respectively. This compound serves as a fluorescent ligand, facilitating the study of adenosine receptor signaling pathways. Its biological activity makes it a valuable tool for research applications in pharmacology, receptor biology, and the development of therapies targeting adenosine-related disorders. -
Adenosine A1 Receptor Antagonist
NPC 200 is a potent and selective antagonist of the Adenosine A1 receptor. It effectively reverses NECA-induced left and right atrial depression, demonstrating EC50 values of 1.08 and 2.03 μM, respectively. This compound is valuable for research into cardiovascular function and the role of adenosine receptors in various physiological processes. -
Adenosine Receptor Agonist
Adenosine Receptor Agonist 2 is a potent adenosine A2B receptor (A2BR) agonist with an EC50 of 0.38 nM. This compound effectively inhibits the accumulation of cyclic AMP (cAMP) and calcium, demonstrating its role in modulating intracellular signaling pathways. Adenosine Receptor Agonist 2 is suitable for research applications focused on cardioprotection and related cardiovascular studies. -
A1/A3 Antagonist
A1/A3 AR antagonist 1 is a potent dual antagonist of the adenosine A1 and A3 receptors, exhibiting affinity constants (Kis) of 36.7 nM for human A1, 25.4 nM for human A3, and 1.47 nM for rat A1. This compound is valuable for investigating various biological processes, particularly in the context of kidney failure, inflammatory pulmonary diseases, and Alzheimer's disease. Its dual receptor targeting makes it a useful tool for exploring the roles of adenosine receptors in these conditions. -
Adenosine Receptor Antagonist
Xanthine amine congener dihydrochloride is a potent antagonist of adenosine A1 and A2 receptors, exhibiting IC50 values of 1.8 nM and 114 nM, respectively. This compound has demonstrated convulsant activity in murine models, making it a valuable tool for studying adenosine receptor involvement in neurological research and potential therapeutic applications. Its selectivity and potency make it suitable for investigations into the modulation of adenosine signaling and its implications in various physiological processes. -
A1 Adenosine Receptor Antagonist
IRFI-165 is a potent and selective antagonist of the A1 adenosine receptor, exhibiting a Ki value of 7.9 nM for the rat A1 adenosine receptor. This compound shows a high degree of selectivity over A2A and A3 receptors. IRFI-165 has demonstrated antidepressant activity in vivo, making it a valuable tool for studying psychiatric and neurological disorders in research applications. -
A1AR Antagonist
FSCPX is a potent and selective irreversible antagonist of the A1 adenosine receptor (A1AR), exhibiting low nanomolar affinity for this target. By effectively reducing interstitial adenosine levels, FSCPX can alter the impact of nucleoside transport inhibitors such as NBTI in cardiac tissue. This compound is valuable for research applications focused on cardiovascular pharmacology and adenosine signaling pathways. -
Adenosine Receptor Antagonist
Adenosine receptor antagonist 1 is a selective antagonist for the A2A adenosine receptor, exhibiting an IC50 of 0.29 nM. This compound demonstrates a 14-fold greater selectivity for A2A receptors compared to A2B receptors. It is widely used in research to investigate the modulatory effects of adenosine signaling in various physiological and pathological processes. -
Adenosine Receptor antagonist
N-0861 is a selective antagonist of the A1 adenosine receptor. It effectively inhibits the negative conduction effects associated with adenosine, such as prolonged AH interval and chest pain, without significantly affecting the increase in coronary blood flow velocity induced by adenosine. This specificity makes N-0861 a valuable tool for research in cardiovascular physiology and the exploration of adenosine receptor signaling pathways. -
Adenosine Analog
8-Methoxyadenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits smooth muscle vasodilatory effects and possesses potential anti-cancer properties by inhibiting tumor progression. It is valuable for research applications in cardiovascular studies and cancer biology, providing insights into adenosine's role in these processes. -
mGlu5 Agonist
VU0424465 is a potent partial agonist and positive allosteric modulator (PAM) of the metabotropic glutamate receptor subtype 5 (mGlu5), primarily targeting intracellular calcium (iCa2+) mobilization. With a Ki value of 11.8 nM, VU0424465 demonstrates high affinity at the MPEP allosteric binding site. This compound also facilitates the activation of pERK1/2 in cortical neurons, making it a valuable tool for research into neurological disorders and signaling pathways associated with mGlu5 activation. -
D3R PAM-Antagonist
MLS6357, a D3 dopamine receptor (D3R)-selective positive allosteric modulator and antagonist, demonstrates significant antagonist activity in D3R-mediated assays, including BRET-based β-arrestin recruitment and Go-BRET assays, with IC50 values of 13 μM, 14 μM, and 17 μM respectively. It shows selectivity for D3R, with no notable activity on other dopamine receptor subtypes (D1R, D2R, D4R, D5R) at concentrations above 100 μM. MLS6357 serves as a valuable tool for investigating neuropsychiatric disorders, particularly in the context of substance use disorders. -
A2 Agonist
CI-936 is an orally active A2 adenosine receptor agonist exhibiting an affinity of 25 nM. This compound demonstrates significant and selective activities in preclinical models associated with antipsychotic efficacy. Notably, CI-936 effectively inhibits exploratory behavior in mice, making it a valuable tool for understanding the neuropharmacological pathways linked to psychotropic effects. -
Exenatide Impurity
(D-Asn28)-Exenatide is an impurity of Exenatide, which functions as a long-acting agonist of the glucagon-like peptide-1 receptor. This compound may be used in research applications focusing on peptide synthesis, quality control, and pharmacological studies involving GLP-1 receptor pathways. Its significance lies in understanding the properties and effects of Exenatide-related compounds. -
RGS Protein Inhibitor
CCG 203769 is a selective inhibitor of the regulator of G protein signaling (RGS4), effectively disrupting the RGS4-Gαo protein-protein interaction with an IC50 of 17 nM. This compound is instrumental for research applications focused on G protein-coupled signaling pathways and the modulation of G protein activity. CCG 203769 may be utilized in studies exploring the role of RGS proteins in various physiological processes and disease states. -
RGS Agonist
BMS-192364 is a selective RGS (Regulator of G Protein Signaling) agonist that targets the Gα-RGS interaction, promoting the formation of an inactive Gα-RGS complex. This compound has been shown to reduce urinary bladder contraction and enhance the activity of GTPase-activating proteins (GAPs) on Gq proteins. Additionally, BMS-192364 inhibits calcium flux, making it a valuable tool for studying signaling pathways involved in bladder function and related physiological processes. -
RGS10 Modulator
RGS10 modulator-1 functions as a potent modulator of the RGS10 protein, exhibiting significant biological activity by reversing interferon-gamma (IFNγ)-induced expression of RGS10 protein and mRNA. Additionally, this compound effectively reduces the levels of COX-2 mRNA and inducible nitric oxide synthase (iNOS) expression that are stimulated by IFNγ. RGS10 modulator-1 is a valuable tool for research exploring the regulatory mechanisms of RGS10 in inflammatory responses and related signaling pathways. -
RGS14 Inhibitor
Z55660043 is a selective inhibitor of Regulator of G protein Signaling-14 (RGS14) with an IC50 of 2.3 μM. This compound acts by non-covalently inhibiting the GTPase-accelerating protein (GAP) activity of RGS14, demonstrating a favorable safety profile without significant cytotoxic effects. Z55660043 is suitable for research focused on central nervous system and metabolic disorders, contributing to the understanding of RGS14's role in these biological processes. -
RGS4 Inhibitor
CCG-2046 is a selective inhibitor of the regulator of G-protein signaling 4 (RGS4), demonstrating an IC50 value of 4.3 μM for inhibiting the RGS4-Gαo interaction. This compound modulates G-protein signaling pathways, making it a valuable tool for studying their role in various physiological processes. CCG-2046 is suitable for research applications focused on neurobiology, cardiac function, and potential therapeutic interventions for related disorders. -
RGS Protein Inhibitor
CCG-4986 is a selective RGS protein inhibitor that covalently modifies the Cys-132 residue of RGS4, thereby inhibiting its activity. This compound is valuable for studying the implications of altered G protein-coupled receptor (GPCR) signaling in various pathological conditions, including Parkinson's disease and opioid addiction. CCG-4986 is a useful tool for researchers investigating the role of RGS proteins in cellular signaling pathways. -
RXFP1 Modulator
AZD5462 is an RXFP1 modulator that targets the relaxin receptor, which is part of the GPCR family. This compound exhibits anti-fibrotic and anti-inflammatory properties, making it a valuable tool for research into heart failure and related cardiovascular diseases. Its application in studies of RXFP1 signaling pathways can provide insights into potential therapeutic strategies for heart dysfunction. -
RXFP2 Agonist
RXFP2 Agonist 2 is a selective allosteric agonist of the RXFP2 receptor, exhibiting an EC50 of 0.38 μM. This compound promotes osteoblast mineralization and enhances bone formation in female mice. RXFP2 Agonist 2 is valuable for research studies focused on osteoporosis and bone health. -
RXFP3/4 Agonist
RXFP3/4 Agonist 2 is a potent nonpeptide dual agonist targeting RXFP3 and RXFP4, with EC50 values of 3.1 nM and 2.7 nM, respectively. This compound effectively promotes the interaction between RXFP3 and β-arrestin-2, displaying EC50 values ranging from 10 to 22 nM. RXFP3/4 Agonist 2 is valuable for investigating receptor signaling pathways and exploring potential therapeutic applications related to metabolic and cardiovascular diseases. -
RXFP4 Agonist
A13:B7-24-GG is a selective RXFP4 agonist that acts through its high-affinity binding (Ki = 2.29 nM) to the RXFP4 receptor, while demonstrating minimal interaction with RXFP3 (Ki = 602.56 nM). This compound effectively inhibits cAMP production with an EC50 of 1.17 nM and facilitates the recruitment of β-Arrestin2, showing an EC50 of 22.39 nM. A13:B7-24-GG is primarily utilized in research focused on chronic constipation and related gastrointestinal disorders. -
RXFP1 Agonist
AZ7976 is a highly selective agonist for the Relaxin Family Peptide Receptor 1 (RXFP1), displaying a pEC50 value greater than 10.5. This compound enhances cAMP signaling through an allosteric mechanism, resulting in a physiological increase in heart rate. AZ7976 is suitable for investigations in cardiovascular disease research and related studies focusing on RXFP1-mediated pathways. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-6 is a potent agonist of the RXFP1 receptor, effectively stimulating cAMP production in HEK293 cells that stably express the human RXFP1. With an EC50 value of 12 nM, this compound is valuable for research applications focused on understanding RXFP1 signaling pathways and their implications in various physiological processes. -
RXFP2 Agonist
RXFP2 Agonist 1 selectively targets the relaxin family peptide receptor 2 (RXFP2) and demonstrates potent agonistic activity with an EC50 of 0.06 µM. This compound plays a significant role in cellular signaling pathways associated with bone metabolism and has potential applications in osteoporosis research. Its ability to modulate RXFP2 activity makes it a valuable tool for studies focused on therapeutic strategies aimed at bone health and regeneration. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-10 is a potent RXFP1 receptor agonist with an EC50 value of 0.5 nM. This compound exhibits significant biological activity, making it a valuable tool for studying the physiological roles of the RXFP1 receptor. Its utility in research extends to investigations related to heart failure, providing insights into the potential therapeutic mechanisms involving RXFP1 modulation. -
RXFP1 Activator
Efadirelaxin alfa is a selective agonist of the relaxin/insulin-like family peptide receptor RXFP1, exhibiting a prolonged terminal half-life following subcutaneous administration. It demonstrates significant anti-cardiac hypertrophy and anti-fibrotic properties by modulating the TGF-β1/Smad2 and AKT/eNOS signaling pathways. Efadirelaxin alfa effectively reverses cardiac hypertrophy and collagen deposition while improving cardiac systolic function, all without affecting blood pressure or heart rate. This compound is primarily utilized in research focused on heart failure mechanisms and therapies. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-8 is a selective agonist for the RXFP1 receptor, which plays a crucial role in the modulation of cellular signaling pathways. This compound effectively stimulates cAMP production in HEK293 cells that stably express human RXFP1, exhibiting an EC50 value of 1.8 nM. It is valuable for research applications investigating RXFP1-mediated signaling and its physiological implications. -
RXFP3 Agonist
RXFP3 Agonist 1 is a nonpeptide compound that selectively activates the RXFP3 receptor with an EC50 value of 6937 nM. This reagent is valuable for investigating the physiological roles of RXFP3 in various biological processes, including mood regulation and reproductive functions. Its application extends to studies exploring potential therapeutic targets for diseases associated with RXFP3 signaling pathways. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-4 is a selective agonist for the RXFP1 receptor. It effectively stimulates cyclic AMP (cAMP) production in HEK293 cells that stably express the human RXFP1 receptor, demonstrating an EC50 value of 4.9 nM. This compound is valuable for research applications related to the RXFP1 signaling pathway and its role in various physiological processes. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-1 selectively targets the RXFP1 receptor, leading to the activation of downstream signaling pathways. This compound effectively stimulates cyclic AMP (cAMP) production in HEK293 cells that stably express human RXFP1, demonstrating an EC50 value of 300 nM. It serves as a valuable tool for research into receptor signaling mechanisms and the physiological implications of RXFP1 activation. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-5 is a selective agonist for the RXFP1 receptor, a key regulator of various physiological processes. This compound effectively stimulates cAMP production in HEK293 cells that stably express the human RXFP1 receptor, demonstrating an EC50 value of 1.3 nM. It is an invaluable tool for research applications involving signal transduction, reproductive biology, and cardiovascular studies. -
Relaxin Receptor Agonist
Efranarelaxin alfa acts as a relaxin receptor agonist, primarily influencing cardiovascular health and tissue regeneration pathways. This compound has potential applications in research focused on cardiovascular diseases and promoting tissue repair mechanisms, offering a valuable tool for exploring therapeutic strategies in these areas. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-3 is a selective agonist for the RXFP1 receptor, known to enhance the production of cyclic AMP (cAMP) in HEK293 cells that stably express the human RXFP1. With an effective concentration (EC50) of 2 nM, RXFP1 receptor agonist-3 serves as a valuable tool for studying the biological functions and signaling pathways associated with RXFP1, facilitating research in areas such as cardiovascular biology and neurobiology. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-2 is a potent agonist of the RXFP1 receptor, demonstrating the ability to stimulate cAMP production in HEK293 cells stably expressing human RXFP1, with an EC50 value of 1 nM. This compound is useful for investigating the role of the RXFP1 receptor in various physiological processes and cellular signaling pathways. It serves as a valuable tool in pharmacological research focused on receptor function and related biological activities. -
RXFP1 Receptor Agonist
RXFP1 receptor agonist-7 is a selective agonist of the RXFP1 receptor, facilitating significant increases in cAMP production. This compound has demonstrated an EC50 value of 4.2 nM in HEK293 cells stably expressing human RXFP1, indicating potent activity. RXFP1 receptor agonist-7 is suitable for research applications focusing on signal transduction, neurobiology, and cardiovascular studies involving the RXFP1 pathway. -
RXFP3/4 Agonist
RXFP3/4 Agonist 1 is a selective agonist of the relaxin family peptide 3/4 receptors (RXFP3/4), exhibiting EC50 values of 82 nM for RXFP3 and 2 nM for RXFP4. This compound has been shown to enhance food intake in rat models, making it a valuable tool for studying appetite regulation and metabolic processes. Its potency and specificity make it suitable for research focusing on the roles of RXFP3/4 in energy homeostasis and related signaling pathways. -
RXFP1 Agonist
RXFP1 receptor agonist-9 is a selective agonist for the RXFP1 receptor, displaying an EC50 of 2.5 μM and a maximum response (Ymax) of 65%. This compound demonstrates excellent microsomal stability along with favorable pharmacokinetic properties, making it suitable for in vivo studies. RXFP1 receptor agonist-9 is primarily utilized in the investigation of heart failure and related cardiovascular conditions. -
sst1 Agonist
L-797591 hydrochloride is a selective somatostatin receptor 1 (sst1) agonist. It effectively mimics the action of somatotropin release inhibiting factor (SRIF) analogs, SRIF-14 and SRIF-28, by potently inhibiting cAMP accumulation stimulated by Forskolin or corticotropin-releasing hormone (CRH). This compound is useful for studies focused on somatostatin receptor signaling and its implications in neuroendocrine regulation. -
SSTR4 Agonist
SSTR4 Agonist 6 is a selective agonist for the somatostatin receptor subtype 4 (SSTR4), which plays a crucial role in modulating neuroendocrine functions and pain pathways. This compound has demonstrated significant biological activity in preclinical models, making it a valuable tool for investigating the mechanisms of pain and potential therapeutic applications in pain management research. -
MMP Inhibitor
Sucrose octasulfate is a matrix metalloproteinase (MMP) inhibitor that modulates cellular activities by regulating the extracellular matrix. It promotes the release of somatostatin-like immunoreactivity from gastric D cells, facilitating ulcer healing through increased endogenous somatostatin levels. This compound has demonstrated efficacy in improving wound closure in diabetic foot ulcers and venous leg ulcers, making it pertinent for research in chronic wound healing and gastrointestinal disorders. Additionally, sucrose octasulfate serves as a valuable pharmaceutical excipient in various therapeutic applications. -
SST4 Receptor Agonist
J-2156 TFA is a potent and selective agonist of the somatostatin receptor type 4 (SST4), exhibiting IC50 values of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. This compound demonstrates significant anti-inflammatory activity and is utilized in research focused on alleviating mechanical allodynia and mechanical hyperalgesia in rodent models. Its specificity for the SST4 receptor makes it an essential tool in studies related to pain mechanisms and somatostatin signaling pathways. -
SSTR4 Agonist
Mazisotine is a potent agonist of somatostatin receptor 4 (SSTR4) with an EC50 of 4.7 nM. This orally active compound demonstrates significant analgesic properties in models of nociceptive and neuropathic pain, including inflammatory and osteoarthritic conditions. Mazisotine serves as a valuable tool for pain research applications, facilitating the exploration of SSTR4-mediated pathways in pain modulation.
