Catalog No.
Product Name
Application
Product Information
Citations
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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. -
β-adrenergic Antagonist
Pronethalol is a non-selective β-adrenergic antagonist that effectively inhibits β-adrenergic receptor activity. It has been shown to potently inhibit Sox2 expression and demonstrates protective effects against digitalis-induced ventricular arrhythmias. Additionally, Pronethalol limits the formation of cerebral arteriovenous malformations (AVMs), making it a valuable reagent for research into cardiovascular and neurological conditions. -
Adrenergic Receptor Agonist
A-61603 is a selective α1A-adrenergic receptor agonist that enhances adrenergic signaling. This compound increases the frequency of spontaneous calcium (Ca2+) transients in rat ventricular myocytes in vitro, indicating its potential role in cardiac research. A-61603 is valuable for studies investigating adrenergic receptor functions and cardiovascular physiology. -
β-AR Modulator
Lubabegron is a potent modulator of β-adrenergic receptors (β-AR). It exhibits antagonistic activity at the β1 and β2 receptor subtypes while acting as an agonist for the β3 receptor subtype in cattle. This compound is effective in reducing ammonia gas emissions from livestock and their waste, making it relevant for environmental and agricultural research applications. Lubabegron holds potential for studies focusing on animal physiology and sustainable farming practices. -
α-adrenoceptors Agonist
Levonordefrin is an α-adrenergic receptor agonist known for its role in blood pressure regulation. This compound exerts hypotensive effects through the stimulation of central α-adrenergic receptors in the nucleus tractus solitarius of the medulla oblongata, leading to centrally mediated hypotension and bradycardia. When administered intravenously, Levonordefrin demonstrates a dose-dependent increase in mean arterial blood pressure. This reagent is particularly useful for investigating the pathophysiology of hypertension and studying drug metabolism. -
Stable Isotope
Atenolol-d7 is a deuterium-labeled variant of Atenolol, a cardioselective β1-adrenergic receptor blocker that exhibits a Ki value of 697 nM at the β1-adrenoceptor in guinea pig left ventricle membranes. This stable isotope is instrumental in pharmacokinetic studies and metabolic research related to hypertension and angina pectoris. Its unique properties facilitate the investigation of drug metabolism and disposition in biological systems. -
Adrenergic Receptor Antagonist
Vatinoxan hydrochloride is a selective peripheral α2 adrenergic receptor antagonist. It demonstrates significant biological activity in modulating adrenergic signaling pathways and has been widely utilized in research exploring the effects of α2 receptor inhibition on cardiovascular function and neuropharmacology. This compound serves as a valuable tool for studies aimed at understanding the therapeutic potential of adrenergic modulation in various disease models. -
Gαi Inhibitor
0990CL is a selective inhibitor of the heterotrimeric Gαi subunit, functioning through direct interaction with Gαi. This compound effectively inhibits α2 adrenergic receptor-mediated regulation of cyclic AMP (cAMP), making it a valuable tool for studying Gαi signaling pathways. It is particularly useful in research related to neurotransmission and cardiovascular physiology, aiding in the exploration of GPCR-mediated processes. -
Alpha-Adrenergic Agonist
Norfenefrine hydrochloride is an orally active alpha-adrenergic agonist that primarily targets adrenergic receptors. It is utilized in research to investigate mechanisms underlying female stress incontinence and to explore therapeutic strategies for managing this condition. Its role as an endogenous compound also contributes to studies of adrenergic signaling pathways. -
β-adrenergic Receptor Antagonist
Metipranolol is a nonselective β-adrenergic receptor antagonist that exerts its effects primarily through the inhibition of β-receptor signaling. It has demonstrated efficacy in modulating cardiovascular function and intraocular pressure, making it valuable for research related to hypertension and glaucoma. This compound serves as a key tool for studying adrenergic pharmacology and its implications in various physiological and pathological conditions. -
β3-Adrenergic Receptor Agonist
BRL-37344 is a selective β3-adrenergic receptor agonist known for its role in modulating metabolic processes. It has been demonstrated to significantly reduce body weight in obese mouse models, highlighting its potential in obesity research and metabolic disorders. This compound serves as a valuable tool for investigating the therapeutic effects of β3-adrenergic activation in various preclinical studies. -
β-adrenoceptor Agonist
Isoprenaline is a non-selective β-adrenergic receptor agonist known for its potent peripheral vasodilator, bronchodilator, and cardiac stimulating effects. This compound is utilized extensively in research focused on conditions such as bradycardia and bronchial asthma, providing valuable insights into cardiovascular and respiratory therapeutic strategies. Isoprenaline’s diverse biological activity makes it a critical tool for understanding β-adrenoceptor modulation in various physiological and pathological contexts. -
Alkaloid
Aposcopolamine is an alkaloid isolated from Datura ferox, known for its ability to bind closely with acetylcholinesterase (ACHE), adrenergic receptor alpha-2A (ADRA2A), and muscarinic receptor subtype 2 (CHRM2). This compound is of significant interest in Alzheimer's disease research due to its potential effects on cholinergic signaling pathways. Aposcopolamine serves as a valuable tool in investigating neurodegenerative mechanisms and developing therapeutic strategies. -
CXCR7 Antagonist
CXCR7 antagonist-1 hydrochloride functions as an antagonist to the CXCR7 receptor, effectively inhibiting the binding of the SDF-1 chemokine (CXCL12) and I-TAC (CXCL11). This compound demonstrates significant potential in research related to tumor cell proliferation and formation, as well as in inflammatory diseases and other pathologies associated with CXCR7 signaling. Its ability to modulate chemokine receptor activity makes it a valuable tool for exploring therapeutic strategies in cancer and inflammation. -
β2 Agonist
Salmeterol-d3 is a deuterated form of Salmeterol, acting as a selective agonist for the human β2 adrenergic receptor. This compound effectively stimulates cyclic AMP (cAMP) accumulation in Chinese Hamster Ovary (CHO) cells expressing human β2 adrenergic receptors, demonstrating a pEC50 of 9.6, along with lower activity at β1 and β3 adrenergic receptors (pEC50 values of 6.1 and 5.9, respectively). Salmeterol-d3 is valuable for research applications focused on respiratory diseases, drug metabolism studies, and the pharmacological profiling of β2 agonists. -
Adrenergic Receptor
FFN270 hydrochloride is a fluorescent tracer that specifically targets adrenergic receptors, functioning as a substrate for norepinephrine and vesicular monoamine transporters. This compound displays distinct absorption and excitation maxima at either 320 nm or 365 nm depending on the solvent pH, with an emission wavelength of 475 nm. FFN270 hydrochloride is valuable in research applications that involve monitoring norepinephrine dynamics and can also serve as a ratiometric pH sensor for various biological studies. -
Adrenergic Receptor Agonist
Lofexidine hydrochloride is a selective α2-adrenergic receptor agonist, primarily utilized to mitigate the physical symptoms associated with opioid withdrawal, including heroin dependence. Its mechanism involves reducing norepinephrine release, thereby diminishing withdrawal-related discomfort. This compound is valuable in research focusing on addiction treatment and the physiological responses to opioid cessation. -
Adrenergic Receptor Agonist
Methyldopate is an ethyl ester proagent of α-Methyldopa, functioning primarily as an α-adrenergic receptor agonist with selectivity for α2-adrenergic receptors. This compound is of significant interest in the study of severe hypertension due to its potential to modulate adrenergic signaling pathways. Research applications include investigating the mechanisms of blood pressure regulation and the pharmacology of antihypertensive therapies. -
Adrenergic Receptor Antagonist
Medroxalol is an orally active adrenergic receptor antagonist that targets both α- and β-adrenergic receptors. This compound exhibits antihypertensive properties as well as vasodilatory effects, making it valuable in studies related to cardiovascular health. Its mechanism of action and biological activity are significant for researching hypertension and related cardiovascular conditions. -
Adrenergic Receptor Antagonist
(±)-N-Methylcoclaurine is a selective α2-adrenoceptor antagonist. This compound demonstrates potential to modulate adrenergic signaling pathways, making it a valuable tool in studies of cardiovascular function and neurobiology. Its ability to inhibit α2-adrenergic receptors positions it as a candidate for investigating therapeutic strategies in conditions related to adrenergic dysregulation. -
Adrenergic Receptor Agonist
Dopexamine hydrochloride is a selective β2 adrenergic receptor agonist. It exhibits positive inotropic and vasodilatory effects, making it valuable in the treatment of heart failure and shock. Additionally, its ability to enhance cardiac output and tissue perfusion underpins its application in cardiovascular research and studies investigating adrenergic signaling pathways. -
β3-adrenergic Receptor Inhibitor
Vemtoberant is a selective β3-adrenergic receptor inhibitor with a human Ki of 8.2 nM, demonstrating a significant selectivity of 400- to 600-fold over the human β1- and β2-adrenergic receptors. This compound effectively attenuates β3-AR-mediated cardiac inhibition, making it a valuable tool for studying mechanisms underlying systolic heart failure. Researchers can utilize Vemtoberant to investigate therapeutic strategies aimed at modulating β3-adrenergic signaling in cardiac contexts. -
Stable Isotope
Propranolol-d7 is a stable isotope-labeled form of Propranolol, a nonselective β-adrenergic receptor (βAR) antagonist. It exhibits high affinity for β1AR and β2AR, with inhibition constants (Ki) of 1.8 nM and 0.8 nM, respectively. Propranolol's capability to inhibit [3H]-DHA binding to rat brain membranes, with an IC50 of 12 nM, makes it a valuable tool for researching conditions such as hypertension, myocardial infarction, cardiac arrhythmias, and other cardiovascular disorders. -
ADRB2 Agonist
Mabuterol is a selective beta-2 adrenergic receptor (ADRB2) agonist with oral bioavailability. This compound inhibits cell proliferation and effectively suppresses the rise of intracellular calcium levels triggered by PDGF-BB. Additionally, Mabuterol reduces protein expression of Drp-1, cyclin D1, and PCNA, while enhancing Mfn-2 expression in response to PDGF-BB. These properties make it a valuable tool for research into cellular proliferation and signaling pathways. -
Isomer
(2R)-SR59230A is the isomer of SR59230A, serving as a crucial experimental control in research settings. As a potent and selective antagonist of the β3-adrenergic receptor, it penetrates the blood-brain barrier and exhibits IC50 values of 40, 408, and 648 nM for the β3, β1, and β2 receptors, respectively. This compound is valuable for studying the pharmacological roles of β-adrenergic receptors and their implications in metabolic disorders and neurological conditions. -
α1-adrenergic Receptor Antagonist
(R)-Terazosin is a potent α1-adrenergic receptor antagonist, specifically the active R-enantiomer of Terazosin. It exhibits high affinity for the α1a, α1b, and α1d subtypes with Ki values of 6.51 nM, 1.01 nM, and 1.97 nM, respectively. This compound is primarily utilized in research applications focused on cardiovascular studies and the treatment of benign prostatic hyperplasia, offering insights into adrenergic signaling pathways and their therapeutic implications. -
Adrenergic Receptor Antagonist
Dicentrine is an α1-adrenoceptor antagonist derived from the plant Stephania epigaea Lo. This natural product exhibits antihypertensive properties and has shown efficacy against human hyperplastic prostate tissues. Its selective inhibition of adrenergic receptors makes it a valuable compound for studying blood pressure regulation and benign prostatic hyperplasia in various research applications. -
β3-Adrenergic Receptor Agonist
LY377604 is a selective agonist of the human β3-adrenergic receptor, exhibiting an EC50 of 2.4 nM. In addition to its agonistic activity, it antagonizes β1- and β2-adrenergic receptors. This compound is utilized in research applications related to metabolic regulation, cardiovascular studies, and the exploration of therapeutic strategies for obesity and diabetes. -
β-Adrenergic Receptor Agonist
Hexoprenaline is a selective β-adrenergic receptor agonist that promotes bronchodilation through the activation of adenylate cyclase. This compound enhances the uptake of 14C-Aminopyrine and exhibits significant anti-inflammatory and anti-infective properties. Additionally, Hexoprenaline is associated with increased placental weight and improved blood flow. It serves as a valuable reagent for research in inflammation, immunology, infection, endocrinology, and neurological disorders, including asthma, chronic bronchitis, and organophosphorus compound intoxication. -
α2 Agonist
Apraclonidine hydrochloride is a selective α2 adrenergic receptor agonist with weak α1 receptor activity. It is primarily used to reduce intraocular pressure (IOP) in conditions such as glaucoma by decreasing aqueous humor production. Additionally, this compound can facilitate eye lid elevation and is utilized in various ophthalmic research applications. -
β-AR Ligand
CGP 12177 hydrochloride is a selective β-Adrenergic receptor (β-AR) ligand, primarily functioning as a β3-AR agonist (Ki = 88 nM) while acting as an antagonist at β1/β2-ARs (Ki = 0.9 nM for β1; Ki = 4 nM for β2). This compound also exhibits partial agonist activity for α1-AR in rat pulmonary artery. Notably, CGP 12177 hydrochloride influences the expression of uncoupling protein and leptin genes in adipose tissues of NMRI mice, making it a valuable tool for research in cardiovascular and metabolic disease mechanisms. -
β2-Adrenergic Receptor Agonist
Protokylol hydrochloride serves as a potent agonist of the β2-adrenergic receptor. This compound demonstrates significant bronchodilator activity, making it valuable in research related to respiratory function and pulmonary pharmacology. Additionally, it interacts with the TRPV1 receptor, further expanding its potential applications in studying pain pathways and sensory responses. -
Stable Isotope
Propranolol-d7 (ring-d7) is a deuterated analogue of Propranolol hydrochloride, a nonselective β-adrenergic receptor antagonist. It exhibits high affinity for both β1 and β2 adrenergic receptors, with Ki values of 1.8 nM and 0.8 nM, respectively. This compound inhibits [3H]-DHA binding in rat brain membranes with an IC50 of 12 nM, making it a valuable tool for studying cardiovascular conditions such as hypertension, myocardial infarction, and cardiac arrhythmias. Propranolol-d7 (ring-d7) is particularly useful in pharmacokinetic and metabolic studies using mass spectrometry due to its stable isotope labeling. -
β-adrenergic Receptor Antagonist
Propranolol-d7 hydrochloride is a deuterium-labeled β-adrenergic receptor antagonist, exhibiting high affinity for both β1 and β2 adrenergic receptors with Ki values of 1.8 nM and 0.8 nM, respectively. It effectively inhibits [3H]-DHA binding in rat brain membrane preparations, with an IC50 of 12 nM. This compound is widely utilized in research focused on cardiovascular conditions such as hypertension, myocardial infarction, cardiac arrhythmias, and angina pectoris, as well as in studies on pheochromocytoma and hypertrophic cardiomyopathy.
