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Adenosine A3 Receptor Antagonist
MRS1097 is a potent antagonist of the human adenosine A3 receptor, exhibiting a Ki value of 100 nM. This compound effectively inhibits A3 receptor activity, making it a valuable tool for investigating adenosine signaling pathways and their implications in various physiological and pathological processes. MRS1097 is suitable for research applications focused on inflammation, cancer, and neuroprotection. -
Adenosine Receptor Agonist
Neladenoson dalanate hydrochloride is an orally active adenosine A1 receptor agonist precursor. This compound demonstrates significant biological activity as a partial agonist, making it a valuable tool in research related to chronic heart diseases. Its favorable pharmacokinetic properties and safety profile enhance its potential for therapeutic applications in cardiology. -
A3AR Agonist
MRS 5980 is a potent A3 adenosine receptor (A3AR) agonist with a Ki value of 0.7 nM, demonstrating high specificity for this receptor subtype. This compound exhibits notable oral bioavailability, making it suitable for in vivo studies. MRS 5980 is employed in research to investigate the physiological roles of A3AR in various biological processes and potential therapeutic applications in inflammation and cancer. -
A2AR Antagonist
A2A receptor antagonist 2 is a highly selective antagonist of the adenosine A2A receptor (A2AR) with an IC50 of 8.3 nM. This compound exhibits significant inhibitory activity, making it valuable for research into the modulation of adenosine signaling pathways. Its application spans various fields, including neurobiology and immunology, particularly in studies focused on inflammation and neurodegenerative diseases. -
A2aR Modulator
A2AR modulator-1 is a selective negative allosteric modulator of the adenosine A2a receptor (A2aR) with an IC50 value of 9 nM. This compound reduces the affinity of endogenous adenosine for A2aR and inhibits activation of the cAMP signaling pathway. A2AR modulator-1 effectively enhances pCREB phosphorylation in CD4+ T cells, counteracting immunosuppression in the tumor microenvironment. Its ability to suppress tumor growth and metastasis has been demonstrated in models of triple-negative breast cancer, highlighting its potential in cancer research. -
Adenosine Receptor Antagonist
MRS7799 is a selective antagonist of the A3 adenosine receptor, demonstrating high affinity with Kds of 0.55 nM for human, 3.74 nM for mouse, and 2.80 nM for rat A3AR. This compound is particularly valuable in research applications related to neurodegeneration, cancer, and ischemic conditions in the heart and brain, as well as autoimmune inflammatory diseases. MRS7799 allows for the exploration of adenosine signaling pathways and their implications in various pathological states. -
Vasodilator/A2A Adenosine Receptor Agonist
Regadenoson hydrate is a selective A2A adenosine receptor agonist and potent vasodilator. It enhances coronary blood flow, making it valuable for myocardial perfusion imaging studies. Additionally, regadenoson hydrate increases the permeability of the blood-brain barrier (BBB) in rodent models, facilitating research into the enhanced delivery of therapeutic agents to the central nervous system (CNS) in humans. -
A3AR Antagonist
A3AR Antagonist 1 is a highly selective antagonist of the human A3 adenosine receptor (A3AR), exhibiting a Ki of 4.63 nM. This compound demonstrates no affinity for the rat A3AR, even at elevated concentrations. It is suitable for research applications focusing on adenosine signaling pathways and their roles in various physiological and pathological processes. -
hA3AR Antagonist
A3AR antagonist 2 is a potent inhibitor of the human A3 adenosine receptor (hA3AR) with a Ki value of 4.54 nM. This compound functions through competitive blockade of receptor activity, making it a valuable tool for elucidating A3AR-mediated signaling pathways. It is suitable for research applications investigating the role of A3AR in various biological processes, including inflammation and cancer biology. -
Adenosine Receptor Agonist
Neladenoson dalanate is a selective agonist precursor of the Adenosine A1 Receptor. This compound exhibits notable pharmacokinetic properties and a favorable safety profile, making it suitable for research in chronic heart disease. Its biological activity contributes to the modulation of cardiac function, offering insights into potential therapeutic applications for cardiovascular disorders. -
A1-adenosine Agonist
SDZ-WAG994 is a selective and orally active agonist of the A1-adenosine receptor, exhibiting a KD of 23 nM. This compound is characterized by its stability and long action, making it suitable for research applications related to atrial fibrillation. Its specificity for the A1 receptor facilitates investigations into adenosine receptor signaling pathways and potential therapeutic interventions in cardiovascular diseases. -
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. -
Adenosine Analog
N6-Benzoyl-7'-O-DMT-morpholino adenine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits notable biological activities, including smooth muscle vasodilation and the potential inhibition of cancer progression. It is commonly utilized in research applications related to cardiovascular studies and cancer therapeutics, contributing valuable insights into adenosine signaling and its effects on physiological processes. -
Adenosine Analog
2-Cyanomethylthioadenosine is an adenosine analog that primarily targets adenosine receptors. This compound demonstrates potent vasodilatory effects on smooth muscle tissue and has shown potential in inhibiting cancer progression. It serves as a valuable tool in research applications focusing on vascular biology and cancer therapeutics. -
Adenosine Analog
3’-β-C-Ethynyladenosine is an adenosine analog that primarily targets adenosine receptors. It exhibits smooth muscle vasodilatory effects and has been implicated in the inhibition of cancer progression. Additionally, this compound serves as a click chemistry reagent, featuring an alkyne group that allows it to undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, facilitating bioconjugation applications in chemical biology and drug development. -
Adenosine Analog
7'-O-DMT-morpholino thymine is an adenosine analog primarily known for its role in modulating adenosine receptors. It exhibits biological activities such as smooth muscle vasodilation and may play a role in inhibiting cancer progression. This compound is valuable for research applications in cardiovascular studies and cancer biology, providing insights into cellular signaling pathways and therapeutic strategies. -
Adenosine Analog
N6,N6-Dimethyl-2’-β-C-methyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant vasodilatory effects on smooth muscle and has been implicated in inhibiting cancer progression. It serves as a valuable tool for research in cardiovascular studies and cancer biology, providing insights into the modulation of adenosine signaling pathways. -
Adenosine Analog
N6-(3-Methoxybenzyl)-2’-C-methyl adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant biological activity as a smooth muscle vasodilator and demonstrates potential anti-cancer properties. It is suitable for research applications focused on vascular biology and cancer therapeutics. -
Adenosine Analog
N6-Methyl-2’-β-C-methyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound has demonstrated vasodilatory effects on smooth muscle and exhibits potential in inhibiting cancer progression. Its unique structure allows for various research applications related to adenosine signaling pathways and therapeutic interventions. -
Adenosine Analog
5’-O-(4,4’-Dimethoxytrityl)-N6-phenoxyacetyl adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant smooth muscle vasodilatory effects and has been implicated in the inhibition of cancer progression. It is a valuable reagent for research focused on vascular biology, immunology, and oncology, facilitating investigations into the therapeutic potential of nucleotide derivatives. -
Adenosine Analog
5'-O-[Bis(4-methoxyphenyl)phenylmethyl]-adenosine is an adenosine analog that primarily acts as a smooth muscle vasodilator. This compound has demonstrated potential in inhibiting cancer progression, making it valuable for cancer research. It serves as a useful tool in studies focused on adenosine receptor modulation and vascular biology. -
Adenosine Analog
3’-O-Propargyladenosine is an adenosine analog that primarily targets adenosine receptors, acting as a vasodilator and exhibiting potential anti-cancer properties. It serves as a valuable tool in research applications involving click chemistry, due to its alkyne functional group, which facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. This compound is instrumental in the study of biochemical pathways and therapeutic interventions related to adenosine signaling and vascular biology. -
Adenosine Analog
N6-Bz-5'-O-DMTr-3'-deoxyadenosine-2'-O-CED-phosphoramidite is an adenosine analog that primarily targets adenosine receptors. It exhibits biological activities such as smooth muscle relaxation and has demonstrated potential in inhibiting cancer progression. This compound is useful in various research applications, particularly in the development of nucleic acid-based therapeutics and the study of adenosine receptor signaling pathways. -
Adenosine Analog
5’-O-(4,4’-Dimethoxytrityl)-2’-beta-C-methyl adenosine is an adenosine analog that primarily acts as a smooth muscle vasodilator. This compound exhibits significant biological activities, including the inhibition of cancer progression. It serves as a valuable tool in research applications related to cardiovascular research, cancer therapies, and the study of adenosine receptor signaling pathways. -
Adenosine Analog
N6-Benzoyl-2'-O-tert-butyldimethylsilyl-3'-O-DMT-adenosine is an adenosine analog that primarily targets adenosine receptors. It exhibits significant smooth muscle vasodilatory effects and has demonstrated potential in inhibiting cancer progression. This compound is valuable for research applications focusing on vascular biology, oncology, and the investigation of adenosine signaling pathways. -
Adenosine Analog
N-[[4-(Trifluoromethyl)phenyl]methyl]adenosine is an adenosine analog known for its smooth muscle vasodilatory effects. This compound has demonstrated potential in inhibiting cancer progression, making it valuable for research in oncology and cardiovascular studies. Its biological activity positions it as a key reagent for investigating adenosine receptor pathways and their implications in various therapeutic contexts. -
Adenosine Analog
8-Benzyloxyadenosine is an adenosine analog that primarily targets adenosine receptors to elicit biological responses. This compound exhibits significant smooth muscle vasodilatory effects and has demonstrated potential in inhibiting cancer progression. It serves as a valuable tool for research in cardiovascular biology and cancer therapeutics. -
Adenosine Analog
5-Methyl-4’-thiouridine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits significant vasodilatory effects, promoting smooth muscle relaxation, and has shown potential in inhibiting cancer progression. Its applications in research encompass studies on cardiovascular function and cancer therapeutics. -
Adenosine Analog
8-Bromo-5’-O-(4-cyanobenzyl)-2’,3’-di-O-isopropylidene adenosine is an adenosine analog that primarily targets adenosine receptors. This compound exhibits smooth muscle vasodilatory activity and has potential applications in cancer research due to its ability to inhibit cancer progression. Its structural modifications make it a valuable tool for studying adenosine signaling pathways in various biological systems. -
Adenosine Analog
2'-O-t-Butyldimethylsilyladenosine is an adenosine analog that primarily targets adenosine receptors. This compound functions as a smooth muscle vasodilator and has demonstrated potential in inhibiting cancer progression. It is valuable for research applications in vascular biology and oncology, contributing to studies on therapeutic pathways involving adenosine signaling. -
Adenosine Analog
2-Benzylthioadenosine is an adenosine analog that primarily acts on adenosine receptors. It is known for its vasodilatory effects on smooth muscle and has been investigated for its potential to inhibit cancer progression. This compound is valuable in research applications related to cardiovascular health and oncology, contributing to the understanding of adenosine signaling pathways. -
Biochemical Assay Reagent
Adenosine 2'-PEG-Biotin is a biochemical assay reagent that acts as a bioisostere of endogenous adenosine, allowing it to engage adenosine receptors effectively. This compound plays a crucial role in regulating various cell signaling pathways, facilitating research into its applications as a bioprobe, biosensor, or diagnostic reagent. Its incorporation of biotin also enhances its utility in various biochemical assays and detection methodologies. -
Adenosine Analog
N6-Benzoyl-2',3'-isopropylidene adenosine is an adenosine analog targeting adenosine receptors. This compound exhibits significant smooth muscle vasodilatory activity and has demonstrated potential in inhibiting cancer progression. Its applications in research include studying vascular physiology and cancer biology, making it a valuable tool in the investigation of therapeutic strategies involving adenosine modulation.

