Catalog No.
Product Name
Application
Product Information
Citations
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β2 Adrenergic Receptor agonist
Vilanterol acetate is a long-acting agonist of the β2 adrenergic receptor. It exhibits pEC50 values of 9.4 for β2-AR, and lower affinities for β1-AR and β3-AR at 6.4 and 6.1, respectively. By selectively activating airway β2 adrenergic receptors, Vilanterol acetate enhances cAMP levels, leading to relaxation of bronchial smooth muscle. This compound is valuable for research in asthma and related respiratory disorders. -
5-HT Receptor Inhibitor
Metrenperone is a selective inhibitor of the 5-HT2 receptor, exhibiting significant antagonist activity on α1 and α2 adrenergic receptors, as well as anti-H1 and anti-dopaminergic effects. It demonstrates notable biological activities, including the reduction of blood pressure, enhancement of bradycardia during peripheral ischemia, and inhibition of serotonin-induced platelet aggregation. Additionally, Metrenperone antagonizes serotonin-mediated vasoconstriction and is involved in promoting the repair of acutely damaged collagen tissue, making it valuable for various research applications in cardiovascular and vascular biology. -
M3 mAChR Antagonist
p-F-HHSiD (p-Fluorohexahydrosiladifenidol) functions as a selective antagonist of the M3 muscarinic acetylcholine receptor (mAChR). This compound exhibits antagonistic activity against various muscarinic receptor subtypes as well as the alpha-1 adrenergic receptor. p-F-HHSiD is valuable for research in cancer, metabolic disorders, neurological pathologies, and cardiovascular diseases, including colon cancer, Alzheimer's disease, and diabetes. -
α1-Adrenergic Receptor Antagonist
A55453 is a potent α1-adrenergic receptor antagonist, structurally related to prazosin. It demonstrates high affinity for α1-adrenergic receptors and is utilized as a valuable probe in research applications focusing on cardiovascular function and pharmacological studies. The use of 125I-A55453 allows for enhanced detection and analysis of receptor interactions in various experimental settings. -
β3/β1 Adrenergic Receptor Agonist
BMS-196085 is a potent and selective full agonist targeting the human β3 adrenergic receptor, exhibiting a Ki value of 21 nM. Additionally, it demonstrates partial agonist activity at the β1 receptor. This compound is valuable for research applications related to obesity and type-II diabetes, offering insights into adrenergic receptor modulation for therapeutic strategies. -
Antiprion Agent
Chloroguanabenz acetate is an antiprion agent and a derivative of the α2-adrenergic receptor agonist guanabenz. It effectively inhibits prion formation in both yeast and mammalian in vitro assays. Additionally, Chloroguanabenz acetate has been shown to decrease levels of the truncated Huntingtin derivative Htt48 in HEK293T cells, making it a valuable tool in the investigation of Huntington's disease. -
Stable Isotope
Betaxolol-d7 hydrochloride is a deuterium-labeled analog of Betaxolol hydrochloride, functioning primarily as a selective beta-1 adrenergic receptor blocker. This stable isotope is instrumental in pharmacokinetic studies and metabolic investigations, particularly in the context of hypertension and glaucoma research. Its unique labeling enables precise tracking and quantification in various biological assays, facilitating advanced research into cardiovascular and ocular conditions. -
Stable Isotope
Ractopamine-d6 is a deuterium-labeled analogue of Ractopamine, a potent β-adrenergic receptor (βAR) agonist with a Kd of approximately 25 nM for both pig β1AR and β2AR. This stable isotope enables detailed studies of protein metabolism and is instrumental in research focused on enhancing lean tissue growth and improving production efficiency in swine. Its application is crucial for understanding the biochemical pathways influenced by β-adrenergic signaling in agricultural and animal health settings. -
Adrenergic Receptor Inhibitor
Bamosiran is a small interfering RNA that specifically targets the β-adrenergic receptor 2. This compound is recognized for its ability to significantly reduce intraocular pressure, making it valuable in the study of ocular conditions. Its role as an adrenergic receptor inhibitor aids in investigating therapeutic strategies for glaucoma and other eye disorders. -
β2-adrenergic Receptor Agonist
β2AR agonist 3 is a selective agonist of the β2-adrenergic receptor, involved in mediating various physiological responses. This compound has demonstrated potential in the modulation of metabolic pathways and holds promise for research in type 2 diabetes. Its application may facilitate investigations into β2AR-related mechanisms and therapeutic approaches in metabolic disorders. -
α1 Adrenergic Receptors Antagonist
Doxazosin-d8 is a deuterium-labeled derivative of Doxazosin, a selective antagonist of postsynaptic α1 adrenergic receptors. This compound exhibits potent inhibitory effects on α1 receptor-mediated pathways, making it valuable for studying cardiovascular function and related pharmacological effects. Doxazosin-d8 can be utilized in research applications focusing on hypertension, benign prostatic hyperplasia, and other conditions influenced by α1 adrenergic signaling. -
Alpha 2-adrenergic Receptor Antagonist
Vatinoxan is an alpha 2-adrenergic receptor antagonist that selectively inhibits α2-adrenergic receptors, primarily affecting the peripheral nervous system due to limited central nervous system penetration. By binding to these receptors, Vatinoxan mitigates cardiovascular responses typically induced by α2-adrenergic agonists. This compound is valuable in research related to cardiovascular physiology, sedation, and analgesia. -
β-Adrenergic Receptor Blocker
Proxodolol free base is a selective β-adrenergic receptor blocker. It exhibits efficacy in reducing blood pressure and may be utilized in research focused on arterial hypertension and related cardiovascular conditions. This compound can aid in elucidating the mechanisms of β-adrenergic signaling and its impact on cardiovascular health. -
Stable Isotope
Guanfacine-13C,15N3 is a stable isotope-labeled form of Guanfacine, an orally active noradrenergic α2A adrenergic receptor agonist. This compound exhibits high selectivity for the α2A receptor subtype, contributing to its pharmacological effects such as hypotension and sedation. Guanfacine-13C,15N3 serves as a valuable tool in research applications focused on prefrontal cortex cognitive disorders, including Tourette's syndrome and attention deficit hyperactivity disorder (ADHD). -
Drug Derivative
Photoazolol-1 is a β-adrenergic receptor (βAR) blocker derivative that exhibits unique light-dependent activity. Upon photoactivation, Photoazolol-1 transitions from an inverse agonist to a neutral antagonist, making it a valuable tool for studies involving receptor modulation. This compound's distinct photochemical properties enable innovative research applications in drug development and receptor behavior analysis. -
α1-AR Antagonist
RS-100329 is a selective antagonist of the α1-adrenergic receptor (α1-AR), demonstrating effective inhibition of α1-AR-mediated contractions in lower urinary tract tissues both in vitro and in vivo. This compound is valuable for research applications related to the symptomatic management of benign prostatic hyperplasia, facilitating studies on urinary tract dynamics and receptor signaling pathways. -
β3-Adrenergic Receptor Agonist
Fasobegron is a potent β3-adrenergic receptor agonist, exhibiting a human EC50 of 4.8 nM. Additionally, it demonstrates an EC50 of 250 nM for human β1-adrenergic receptors. This compound is primarily utilized in research related to the treatment of overactive bladder. -
β2AR Blocker
Todralazine is a β2 adrenergic receptor (β2AR) blocker that exhibits antioxidant properties and free radical scavenging activity. This compound demonstrates potential in the regulation of blood pressure through its anti-hypertensive effects. It is a valuable reagent for research applications focused on cardiovascular physiology and the modulation of adrenergic signaling pathways. -
Inotropic Compound
Butopamine hydrochloride is an orally active inotropic compound that primarily targets beta-adrenergic receptors. It is known to enhance cardiac output by increasing heart rate and contractility, making it a valuable tool in cardiovascular research. Its potency may surpass that of Dobutamine, positioning it as an important agent for studies focused on heart function and related conditions. -
Beta 3 Receptor Agonist
BMS-194449 is a selective agonist for the beta-3 adrenergic receptor, exhibiting a binding affinity characterized by a Ki value of 160 nM. This compound is instrumental for research into metabolic disorders, particularly obesity and non-insulin dependent diabetes. Its activation of beta-3 receptors plays a critical role in regulating energy expenditure and lipid metabolism, making it a valuable tool for investigations in these areas. -
β-Adrenergic Receptor Blocker
Proxodolol is a β-adrenergic receptor blocker that inhibits β-adrenergic signaling pathways. It is primarily used in research to investigate its effects on arterial hypertension and related cardiovascular conditions. This compound serves as a valuable tool in studying the physiological implications of β-blockade in various therapeutic contexts. -
β2-AR Agonist
Arformoterol maleate is a long-acting β2-adrenergic receptor (β2-AR) agonist, with a half-maximal effective concentration (Kd) of 2.9 nM. This compound is primarily utilized in research related to chronic obstructive pulmonary disease (COPD), demonstrating significant bronchodilation and improving airflow in affected individuals. Its pharmacological properties make it valuable for studying respiratory diseases and the underlying mechanisms of β2-AR signaling. -
Adrenergic Receptor
Parethoxycaine hydrochloride is an anesthetic that acts primarily on the adrenergic receptors, exhibiting nerve conduction blocking activity. It demonstrates non-selective inhibitory effects on the responses of various stimulants in smooth muscle tissues, such as the rat vas deferens and guinea pig ileum. This compound also enhances the action of norepinephrine and its derivatives influence calcium transport processes, displaying distinct effects on calcium dose-response relationships. Parethoxycaine hydrochloride is valuable for research applications involving the modulation of adrenergic signaling and calcium dynamics in neuronal and smooth muscle systems. -
I2 Ligand
Metrazoline is an imidazoline I2 receptor ligand with low affinity for adrenergic receptors. This compound is used in research to study its role in modulating neuroprotective and antihypertensive effects. It serves as a valuable tool for investigating the physiological and pharmacological functions associated with imidazoline receptors in both in vitro and in vivo settings. -
4-Hydroxypropranolol Metabolite
(±)-4-Hydroxy propranolol β-D-glucuronide is a glucuronidated metabolite of the β-adrenergic receptor antagonist, 4-Hydroxypropranolol. It primarily serves as a marker for metabolic studies involving propranolol administration. This compound is valuable for research exploring drug metabolism, pharmacokinetics, and the therapeutic effects of β-blockers in cardiovascular studies. -
Adrenergic Receptor
(3aR,9aR)-Fluparoxan is a highly selective and potent antagonist of the α2B adrenergic receptor. This compound demonstrates significant potential in neurodevelopmental disorder and neurodegenerative disease research by promoting neurological recovery and function. Its unique mechanism of action positions (3aR,9aR)-Fluparoxan as a valuable tool in neuroscience studies, facilitating the exploration of related therapeutic pathways. -
α2-Adrenoceptor Ligand
TDIQ hydrochloride is a selective ligand for the α2-adrenergic receptors, exhibiting high affinity with Ki values of 75 nM, 95 nM, and 65 nM for the α2A, α2B, and α2C subtypes, respectively. This compound serves as a valuable tool for studying the physiological roles of α2-adrenoceptors and their potential therapeutic applications in various neuropsychiatric and cardiovascular disorders. Its specificity makes it suitable for pharmacological investigations and drug development in receptor-targeted therapies. -
Vasorelaxant Agent
Vasorelaxant agent-2 is an effective vasorelaxant agent that targets the α1A-adrenergic receptor, displaying an affinity of pD2=5.4. This compound demonstrates notable vasodilatory activity, evidenced by an EC50 of 0.79 μM in rat aortic rings. It is a valuable tool for research on vascular function and the modulation of blood pressure. -
α2-adrenoceptor Antagonist
A 80426 mesylate is an α2-adrenoceptor antagonist that modulates neurotransmitter release by inhibiting presynaptic α2-adrenergic receptors. This compound demonstrates potential in the study of antidepressant mechanisms and is utilized in research exploring mood disorders and anxiety. Its ability to enhance noradrenergic neurotransmission makes it a valuable tool for investigating therapeutic strategies within the central nervous system. -
Vasopressor
Mephentermine hemisulfate is a sympathomimetic amine that functions primarily as a vasopressor. It is utilized to increase blood pressure by stimulating adrenergic receptors, leading to vasoconstriction and increased heart rate. This compound has applications in cardiovascular research, particularly in studies related to blood pressure regulation and adrenergic signaling pathways. -
β Adrenergic Receptor Antagonist
Soquinolol is a selective β adrenergic receptor antagonist primarily used in cardiovascular research. This compound exhibits significant inhibition of β-adrenergic signaling, making it valuable for studying cardiac dysfunction and heart failure mechanisms. Its application extends to investigations into therapeutic strategies for managing hypertension and arrhythmias. -
ADRB2 Agonist
Mabuterol hydrochloride is a selective, orally active agonist of the beta-2 adrenergic receptor (ADRB2). This compound demonstrates key biological activity by inhibiting cell proliferation and reducing intracellular calcium levels induced by PDGF-BB. Additionally, Mabuterol hydrochloride downregulates protein expression of Drp-1, cyclin D1, and PCNA, while enhancing Mfn-2 expression in response to PDGF-BB. These properties make Mabuterol hydrochloride valuable for research in cellular signaling and related therapeutic applications. -
Anti-tumor Agent
Scoulerine hydrochloride is a multi-target inhibitor primarily acting as an anti-tumor agent. It disrupts the PI3K/Akt/mTOR signaling pathway and α1D-adrenergic receptors, leading to microtubule destabilization, cell cycle arrest, and apoptosis in cancer cells. This compound also inhibits mitochondrial dehydrogenase activity and demonstrates effects on GABA receptors and BACE1, suppressing tumor cell proliferation, migration, invasion, and stem cell-like properties. Additionally, Scoulerine hydrochloride exhibits pharmacological activities against Plasmodium falciparum, as well as antibacterial, antiemetic, and antitussive properties, while also influencing endoplasmic reticulum stress and mitochondrial function. It is particularly relevant in studies focused on leukemia, ovarian cancer, and colorectal cancer. -
Stable Isotope
Gramine-d2 is a deuterium-labeled derivative of Gramine, a natural alkaloid derived from giant reed. This compound functions as an adiponectin receptor agonist, exhibiting IC50 values of 3.2 μM for AdipoR2 and 4.2 μM for AdipoR1. Additionally, Gramine acts as an agonist for human and mouse β2-Adrenergic receptors, demonstrating anti-tumor, anti-viral, and anti-inflammatory activities. Gramine-d2 is valuable for research applications that require stable isotopic labeling in biological studies. -
Ergot Derivatives
Cianergoline is an ergot derivative primarily known for its ability to reduce intraocular pressure (IOP). Its action is mediated by the inhibition of sympathetic nervous function through interactions with both prejunctional (DA2) and postjunctional (α1) adrenergic receptors. This compound is valuable for research applications focused on glaucoma and the underlying mechanisms of ocular hypertension. -
Neuropeptide
BNP(1-32), porcine is an atrial natriuretic peptide that primarily targets neuropeptide pathways. This cardiac hormone exhibits significant natriuretic, diuretic, and vasorelaxant effects, making it valuable for cardiovascular research. Furthermore, BNP(1-32) has been shown to influence passive avoidance learning in rodent models, highlighting its potential role in neurobiology studies involving dopaminergic and cholinergic systems, as well as adrenergic receptor interactions. -
mAChR Antagonist
4-Piperidyl N-(2-biphenyl)carbamate is a competitive antagonist of muscarinic acetylcholine receptors (mAChR), exhibiting notable selectivity for the M2 and M3 subtypes. With pKi values of 7.33 for M2 and 7.51 for M3, this compound demonstrates a markedly higher affinity compared to β2 adrenergic receptors, which has a pKi of 4.94. This specificity makes it a valuable tool for research into mAChR-related signaling pathways and potential therapeutic applications in various neurological disorders. -
NR4A1 Inhibitor
Glycerol kinase, microorganism functions as an NR4A1 inhibitor by directly binding to and inhibiting the transcription factor NR4A1, which plays a critical role in hepatic gluconeogenesis. This inhibition leads to reduced blood glucose levels and positively influences UCP1 expression through the β-adrenergic receptor-cAMP-CREB signaling pathway, promoting the browning of white adipose tissue and enhancing thermogenesis. Additionally, it modulates intracellular fatty acid composition and energy metabolism. Research using glycerol kinase in diabetic mouse models has demonstrated its ability to counteract NR4A1-induced hyperglycemia, indicating its potential applications in diabetes and obesity studies. -
Xylazine Metabolite
2,6-Dimethylphenylthiourea is a metabolite of xylazine, an established α2-adrenergic agonist. This compound serves as a valuable tool in pharmacological research, specifically in studies examining the metabolic pathways of xylazine and its effects on α2-adrenergic receptors. It provides insights into its pharmacokinetics and potential physiological implications. -
Drug Derivative
(±)-p-Fluoro pseudoephedrine hydrochloride is a drug derivative associated with the pharmacological activity of pseudoephedrine. This compound exhibits decongestant properties, primarily functioning as a sympathomimetic agent that influences adrenergic receptors. Its biological activity is employed in studies related to respiratory distress, providing valuable insights into drug metabolism and therapeutic efficacy in treatments for nasal congestion. -
Clonidine Metabolite
4-Hydroxyclonidine is a metabolite of Clonidine, primarily functioning as an alpha-2 adrenergic agonist. It exhibits comparable potency to Clonidine in displacing labeled Clonidine from specific antibodies. This compound is of significant interest in pharmacological research, particularly in studies examining adrenergic receptor interactions and the metabolic pathways of antihypertensive agents. -
Propranolol Active Metabolite
Norpropranolol hydrochloride is the active metabolite of Propranolol, primarily targeting beta-adrenergic receptors. It exhibits significant cardiovascular effects, including the reduction of heart rate and blood pressure. This compound is used in research applications focused on studying cardiovascular pharmacology and the modulation of stress response pathways. -
Bufuralol Metabolite
4-Hydroxybufuralol is a primary metabolite of Bufuralol, known for its significant role in pharmacokinetics. It exhibits interactions with beta-adrenergic receptors, contributing to cardiovascular research applications. This compound is essential for studies focused on drug metabolism and the pharmacological effects of beta-blockers. -
Alprenolol Metabolite
4-Hydroxyalprenolol is a metabolite of the β-receptor blocker Alprenolol, known for its role in modulating adrenergic signaling. This compound exhibits biological activity related to cardiovascular function and may be utilized in research focused on the pharmacokinetics and pharmacodynamics of β-blockers. Its analysis can provide insights into the metabolism of therapeutic agents and their effects on β-adrenergic receptors. -
NR2B Antagonist
NMDA-IN-1 dihydrochloride is a selective antagonist of the NMDA NR2B receptor, exhibiting a Ki of 0.85 nM and an IC50 of 9.7 nM for NR2B-mediated Ca2+ influx. This compound effectively inhibits Glu/Gly-stimulated Ca2+ flux in Ltk- cells expressing hNR1a/NR2B, demonstrating specificity as it does not interact with NR2A, NR2C, NR2D, hERG channels, or α1-adrenergic receptors. NMDA-IN-1 dihydrochloride displays significant efficacy in mechanical hyperalgesia models in rats and is relevant for investigations into stroke, Parkinson's disease, and neuropathic pain. -
Stable Isotope
O-Desmethyl carvedilol-d5 is a deuterium-labeled derivative of O-Desmethylcarvedilol, a potent active metabolite of the non-selective β-adrenergic receptor antagonist Carvedilol. This compound exhibits inhibitory effects on store-overload-induced calcium release in HEK293 cells expressing the RyR2 R4496C mutation, with an IC50 of 7.62 μM. Additionally, O-Desmethyl carvedilol-d5 contributes to cardiovascular research by attenuating heart rate increases and stabilizing diastolic blood pressure in response to Isoproterenol in conscious rabbit models, demonstrating ED50 values of 32 and 5 μg/kg, respectively. -
P2X1 Receptor Antagonist
NF449 octasodium is a potent antagonist of the P2X1 receptor, exhibiting IC50 values of 0.28 nM, 0.69 nM, and 120 nM for recombinant P2X1, recombinant P2X1 with 5, and P2X2+3 receptors, respectively. It selectively targets the Gsα subunit of G proteins, effectively inhibiting GTP[γS] binding to Gsα-s and reducing adenylyl cyclase activity. NF449 octasodium is useful in research focused on the regulation of P2X1 receptor-mediated signaling pathways and β-adrenergic receptor interactions. -
Potassium Channel Blocker
Besipirdine hydrochloride is a potassium channel blocker that exerts both cholinergic and adrenergic effects. Its cholinergic activity is characterized by stimulation of phosphatidylinositol turnover and a reduction in potassium currents, while its adrenergic activity promotes norepinephrine release through the inhibition of presynaptic α2-adrenergic receptors and the blocking of norepinephrine reuptake. This compound is applicable in research related to Alzheimer's disease, providing insights into potential therapeutic pathways. -
α2 Receptor Agonist
p-Iodoclonidine hydrochloride is a partial agonist of the α2-adrenergic receptor, primarily influencing adrenergic signaling pathways. It exhibits low levels of adenylate cyclase inhibition in platelet membranes and enhances ADP-induced platelet aggregation with an EC50 of 1.5 μM. This compound is useful for research applications focusing on adrenergic receptor physiology and platelet function. -
α1A-Adrenergic Receptor Agonist
Cirazoline hydrochloride is a potent full agonist of the α1A-adrenergic receptor, exhibiting a competitive inhibition constant (Ki) of 120 nM. It also acts as a partial agonist at the α1B-adrenergic receptor with a Ki of 960 nM and the α1D-adrenergic receptor with a Ki of 660 nM. This compound is valuable for research applications involving α1-adrenergic signaling pathways and the study of cardiovascular and neurological conditions.
