Catalog No.
Product Name
Application
Product Information
Citations
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α1D Adrenoceptor Antagonist
TAK-259 is a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist (α1D, Ki = 1.1 nM) with Anti-urinary Frequency Effects and Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities. -
β-adrenergic receptors antagonist
Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias. -
β2-adrenergic receptor agonist
Clorprenaline HCl is a β2-receptor agonist, it has a significant expansion of the bronchial effect. -
β-adrenoceptor agonist
Indacaterol (QAB149) maleate is an ultra-long-acting β-adrenoceptor agonist. -
α1A antagonist
RS 17053 HCl is α1A-adrenoceptor antagonist, with very high affinity for α1A receptors (pKi and pA2 estimates of 9.1 - 9.9) and a 30 - 100 fold selectivity over the α1B and α1D subtypes (pKi and pA2 estimates 7.7 - 7.8). -
β3-adrenergic receptor agonist
Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM. -
β2-adrenergic receptor agonist
Levosalbutamol tartrate(levalbuterol) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist salbutamol. -
A2AR/ENT1 agonist
A2AR-agonist-1 is a potent A2AR and ENT1 agonist with Ki of 4.39 and 3.47 for A2AR and ENT1. -
dual NE/DA transporter inhibitor
Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively. -
α2-adrenoceptor antagonist
Atipamezole is a synthetic α2-adrenoceptor antagonist with a Ki of 1.6 nM. -
muscarinic receptor antagonist and β2-adrenoceptor agonist
Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively. -
β1-adrenergic receptor blocker
Bucindolol is a β1-adrenergic receptor blocker, with intrinsic sympathomimetic activity, used in the research of heart failure. -
β3-adrenoceptor agonist
Amibegron hydrochloride is a selective β3-adrenoceptor agonist, with an EC50 of 3.5 nM for β-adrenoceptor in rat colon; Amibegron hydrochloride has anxiolytic and antidepressant activity. -
peripheral adrenoceptor antagonist
Deriglidole is a peripheral adrenoceptor antagonist with a high affinity for α2-adrenoceptors. -
β adrenergic receptor antagonist
Pargolol hydrochloride is a β adrenergic receptor antagonist. -
β adrenergic receptor antagonist
Spirendolol is a β adrenergic receptor antagonist. -
5-HT2A/α1-adrenergic receptor antagonist
Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist. -
ostsynaptic alpha adrenergic receptor antagonist
Tiodazosin is a potent competitive postsynaptic alpha adrenergic receptor antagonist. -
α1 receptor antagonist
Tamsulosin hydrochloride is a selective α1 receptor antagonist and a medicine which is used in benign prostatic hyperplasia. -
β2-adrenoceptor agonist
Formoterol is a long-acting β2 agonist used in the management of asthma and chronic obstructive pulmonary disease (COPD). -
adrenergic receptor/5-HT receptor inhibitor
Asenapine hydrochloride inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM. -
α-adrenergic receptor agonist
Brimonidine Tartrate is a highly selective α-adrenergic receptor agonist with EC50 of 0.45 nM for the α2A adrenoreceptor, and used to treat open-angle glaucoma or ocular hypertension. -
α2A-adrenoceptor agonist
Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors. -
serotonin (5-HT)/norepinephrine (NE) reuptake inhibitor
Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI). -
triple reuptake inhibitor/5-HT2A/5-HT2C/5-HT3/α1A-adrenergic receptor antagonis
Tedatioxetine hydrobromide acts as a triple reuptake inhibitor and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist. -
β-adrenoceptor blocking agent
(±)-Befunolol is a β-adrenoceptor blocking agent. -
NF-κB Expression Reducer, ERK 1/2 Activator, Beta-Adrenergic Receptor Modulator, Calcium Channel Inhibitor
Eupatorin is a flavonoid that functions primarily as an NF-κB expression reducer and an ERK 1/2 activator, while also modulating beta-adrenergic receptors and inhibiting calcium channels. It demonstrates significant antiproliferative and vasodilatory effects, inducing apoptosis and causing G2/M phase cell cycle arrest, alongside reactive oxygen species (ROS) production. Eupatorin has been shown to impact inflammatory mediators and calcium signaling pathways, making it relevant for research in breast cancer, hypertension, and leukemia. Metabolized by CYP1A1 and other CYP1 enzymes, Eupatorin yields bioactive metabolites that maintain antiproliferative properties. -
Adrenergic Receptor Antagonist
Aaptamine is an alkaloid derived from the marine sponge Aaptos suberitoides, functioning primarily as a competitive antagonist of the α-adrenergic receptor. This compound exhibits significant cytotoxicity against tumor cells, inducing apoptosis and cell cycle arrest while promoting p21 expression through a p53-independent mechanism. Aaptamine also demonstrates a variety of biological activities, including anti-tumor, antioxidant, antibacterial, and analgesic effects, making it a valuable tool for cancer research and therapeutic applications. -
α-1A Adrenergic Receptor Agonist
Dabuzalgron is a selective α-1A adrenergic receptor agonist primarily utilized for the treatment of urinary incontinence. This compound exhibits key biological activity by enhancing bladder function, thereby mitigating symptoms associated with overactive bladder. Additionally, Dabuzalgron has been shown to provide protection against Doxorubicin-induced cardiotoxicity through the preservation of mitochondrial function, making it relevant in cardiovascular research. -
Stable Isotope
N-(Phenylacetyl-d5)glycine is a deuterated form of phenylacetylglycine, functioning as a stable isotope. This compound serves as a gut microbial metabolite that can activate the beta-2 adrenergic receptor (β2AR). Its biological activity includes providing protective effects against cardiac injury induced by ischemia and reperfusion, making it valuable for research in cardiac health and metabolic studies. -
Stable Isotope
D-Mannitol-13C6 is a stable isotope-labeled form of D-Mannitol, targeting metabolic pathways through its role as an osmotic agent. This compound is utilized in various research applications, including studies on calcium and magnesium absorption, cecal fermentation, and the modulation of insulin sensitivity. D-Mannitol has been shown to promote the browning of white adipose tissue by activating the β3-adrenergic receptor, which can lead to enhanced thermogenesis and potential reductions in blood glucose levels. Additionally, it is employed in plant cell culture to maintain osmotic balance and protect cellular integrity. -
Stable Isotope
D-Mannitol-13C is a stable isotope-labeled derivative of D-Mannitol. This compound serves as a valuable osmotic diuretic and is utilized in various research applications, including the study of calcium and magnesium absorption and retention through cecal fermentation. D-Mannitol is known to promote brown adipose tissue formation, enhance insulin sensitivity, and lower blood glucose levels by activating the β3-adrenergic receptor, leading to the conversion of white fat cells into brown fat cells. Additionally, it is employed to maintain osmotic pressure in plant cell cultures, aiding in cellular protection during physiological manipulation. -
Stable Isotope
Perphenazine-d4 is a deuterated derivative of Perphenazine, a typical antipsychotic agent primarily inhibiting the 5-HT2A receptor, alpha-1A adrenergic receptor, dopamine receptor D2/D3, D2L receptor, and histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively. This stable isotope is valuable for pharmacokinetic studies, allowing for the precise tracking of Perphenazine metabolism and distribution in biological systems. Perphenazine-d4 is essential for researchers focusing on neuropharmacology and drug interaction studies involving antipsychotic medications. -
Stable Isotope
D-Mannitol-2-13C is a stable isotope-labeled derivative of D-Mannitol. This 13C-labeled compound plays a critical role in metabolic studies, particularly in understanding carbohydrate metabolism and energy homeostasis. D-Mannitol serves as an osmotic diuretic, promotes the absorption of minerals, enhances brown adipose tissue formation, and demonstrates potential for reducing blood glucose levels through β3-adrenergic receptor activation. It is frequently employed in cell culture applications to maintain osmotic pressure and protect cells, particularly when cell walls are compromised. -
β2AR Activator
Phenylacetylglycine is a gut microbial metabolite that acts as a β2-adrenergic receptor (β2AR) activator. It has demonstrated protective effects against cardiac injury resulting from ischemia/reperfusion. This compound is significant for research into cardiovascular health and the role of microbiota in modulating cardiac responses. -
Dopamine Receptors Blocker
Trifluoperazine dimaleate is a potent dopamine receptor blocker, primarily indicated for research into antipsychotic mechanisms. This compound exhibits significant α1-adrenergic receptor antagonism and serves as an inhibitor of NUPR1, highlighting its potential anticancer properties. Additionally, trifluoperazine dimaleate functions as a calmodulin inhibitor and inhibits P-glycoprotein activity. Its versatile applications extend to studying schizophrenia and the reversible inhibition of influenza virus morphogenesis. -
Stable Isotope
Carvedilol-d3 is a deuterium-labeled analogue of Carvedilol, functioning primarily as a non-selective β/α-1 adrenergic receptor blocker. It exhibits significant biological activity by inhibiting lipid peroxidation in a dose-dependent manner with an IC50 value of 5 μM. This compound serves as a versatile antihypertensive agent and has potential applications in the treatment of angina and congestive heart failure. Furthermore, Carvedilol-d3 promotes autophagy and is known to inhibit the NLRP3 inflammasome, making it valuable for research involving inflammatory processes. -
Stable Isotope
Trifluoperazine-d3 dihydrochloride is a deuterated derivative of Trifluoperazine, primarily targeting dopamine receptors to exert its antipsychotic effects. This compound is a potent α1-adrenergic receptor antagonist and an effective inhibitor of NUPR1, showcasing anticancer properties. Additionally, it functions as a calmodulin inhibitor and can interfere with P-glycoprotein activity. Trifluoperazine-d3 dihydrochloride is valuable for research applications related to schizophrenia and serves as a reversible inhibitor of influenza virus morphogenesis. -
Stable Isotope
Carvedilol-d5 is a deuterium-labeled analogue of Carvedilol, a non-selective β/α-1 adrenergic receptor blocker. It exhibits lipid peroxidation inhibition with an IC50 of 5 μM and serves as a versatile antihypertensive agent, showing potential in the treatment of angina and congestive heart failure. Additionally, Carvedilol functions as an autophagy inducer and inhibits the NLRP3 inflammasome, making it relevant for research in inflammatory pathways and cardiovascular health. -
Stable Isotope
Dronedarone-d6 hydrochloride is a deuterium-labeled derivative of Dronedarone, serving as a stable isotope for research applications. This compound functions primarily as a class III antiarrhythmic agent, effective in the study of atrial fibrillation (AF) and atrial flutter. Dronedarone-d6 hydrochloride exhibits potent blockade of various ion currents, including potassium, sodium, and L-type calcium currents, and also demonstrates antiadrenergic activity through noncompetitive binding to β-adrenergic receptors. Additionally, it acts as a substrate and moderate inhibitor of the CYP3A4 enzyme, making it valuable for pharmacokinetic studies. -
Stable Isotope
Dronedarone-d6 is a deuterium-labeled derivative of the antiarrhythmic agent Dronedarone, primarily targeting various ion channels, including potassium, sodium, and L-type calcium channels. This compound is vital for investigating the mechanisms underlying atrial fibrillation (AF) and atrial flutter, as well as for studying its antiadrenergic properties through its noncompetitive binding to β-adrenergic receptors. In addition, Dronedarone-d6 serves as a substrate and moderate inhibitor of CYP3A4, making it relevant for pharmacokinetic studies in cardiovascular research.
