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Catalog No.
Product Name
Application
Product Information
Citations
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noradrenalin re-uptake inhibitor
Maprotiline hydrochloride is a selective noradrenalin re-uptake inhibitor. -
α-adrenergic (AR) antagonist/CaM inhibitor
Phenoxybenzamine is a cell-permeable, non-specific, irreversible α-adrenergic (AR) antagonist that also acts as an CaM inhibitor. -
Androgen Receptor inhibitor
ARN-509 is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes.- Frédérique Mittler, .et al. , Front Oncol, 2017, 7: 293 PMID: 29322028
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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. -
serotonin (5-HT)/norepinephrine (NE) reuptake inhibitor
Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI). -
alpha-adrenergic receptor agonist / MAO inhibitor
Amitraz, also known as Mitaban and Taktic, is an alpha-adrenergic receptor agonist and MAO inhibitor used as an insecticide in prevention of flea and tick infections. It prevents prostaglandin synthesis and may inhibit beta-cell insulin release. -
serotonin uptake inhibitor
Paroxetine Mesylate is a serotonin uptake inhibitor that is effective in the treatment of depression. -
DOPA decarboxylase inhibitor
Methyldopa Sesquihydrate is a DOPA decarboxylase inhibitor and indirect α2-adrenergic receptor agonist used to treat hypertension. -
alpha-1 adrenergic receptors / mAChRs inhibitor
Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant. -
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. -
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. -
ErbB2 inhibitor
AG-825 is a selective, ATP-competitive inhibitor of ErbB2 (HER2) tyrosine kinase, with an IC₅₀ of 0.35 μM. It exhibits both anticancer and anti-inflammatory activities and has been shown to significantly accelerate apoptosis in human neutrophils. AG-825 also increases β₁-adrenergic receptor (β₁AR) density, suggesting potential cardiomodulatory effects. Due to its multifaceted biological activity, AG-825 is a valuable compound for research in oncology, inflammation, and cardiovascular disease. -
Adrenergic Receptor Inhibitor
Penbutolol sulfate is a potent adrenergic receptor inhibitor, primarily acting as a β-adrenoceptor and 5-HT receptor antagonist, with Ki values of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3 regions, respectively. This compound demonstrates significant biological activity through modulation of neurotransmitter signaling pathways, making it valuable for research applications involving cardiovascular studies and neuropharmacology. -
Triple Reuptake Inhibitor
Tedatioxetine is a serotonin and norepinephrine-preferring triple reuptake inhibitor (TRI) that also functions as an antagonist of 5-HT2A, 5-HT2C, 5-HT3, and α1A-adrenergic receptors. This compound exhibits significant biological activity in modulating neurotransmitter levels, making it relevant for research in neuropharmacology. Its mechanism of action positions it as a valuable tool in studies related to mood disorders and anxiety. -
α2-adrenoceptor Antagonist/5-HT Receptor re-uptake Inhibitor
Napamezole is a potent α2-adrenoceptor antagonist and 5-HT receptor reuptake inhibitor, exhibiting Ki values of 28 nM and 93 nM for rat α2 and α1 adrenergic receptors, respectively. This compound is primarily utilized in research related to depression, facilitating studies on the modulation of serotonergic and adrenergic signaling pathways. Its unique pharmacological profile makes it a valuable tool for investigating potential therapeutic approaches in mood disorders. -
5-HT1A Receptor Inhibitor
LY 178210 is a selective partial agonist of the 5-HT1A receptor, exhibiting Ki values of 0.67 nM for 5-HT1A and 380 nM for 5-HT1D receptors, thereby demonstrating its specificity. Its minimal activity against α₂-adrenergic receptors, 5-HT₂, and other neurotransmitter receptors makes it a valuable tool in neuropharmacology. Additionally, LY 178210 effectively inhibits forskolin-stimulated cyclase activity, though with lower potency compared to full agonists like 8-OH-DPAT. This compound is significant for studies on serotonergic modulation, as it markedly reduces 5-hydroxyindoleacetic acid (5-HIAA) levels in the hypothalamus while increasing serum corticosterone concentrations. -
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. -
Noradrenergic Reuptake Inhibitor
Maprotiline is a selective noradrenergic reuptake inhibitor that exhibits significant antidepressant activity and also shows promise in antitumor and neuropathic pain relief. It facilitates cancer cell apoptosis through modulation of the ERK signaling pathway and interaction with cellular retinoic acid-binding protein 1 (CRABP1). This compound is valuable for research in mental health disorders, oncology, and pain management. -
β₂-adrenergic receptor Agonist/PDE4 Inhibitor
GS-5759 is a dual-action compound functioning as a β₂-adrenergic receptor agonist and a phosphodiesterase 4 (PDE4) inhibitor. By activating the β₂ receptor, GS-5759 elevates intracellular cAMP levels, resulting in bronchial dilation. Additionally, its inhibition of PDE4 activity decreases cAMP degradation, thereby enhancing anti-inflammatory responses. This compound is relevant for research into respiratory disorders, particularly chronic obstructive pulmonary disease (COPD), demonstrating significant bronchodilatory and anti-inflammatory effects in preclinical models. -
α2-adrenoceptor Antagonist/5-HT Receptor re-uptake Inhibitor
Napamezole (hydrochloride) functions as an α2-adrenoceptor antagonist and a serotonin (5-HT) reuptake inhibitor, exhibiting Ki values of 28 nM and 93 nM for rat α2 and α1 adrenergic receptors, respectively. This compound is particularly relevant for research into depression and related neuropsychiatric disorders, facilitating studies on serotonin modulation and adrenergic signaling pathways. Its dual action can provide insights into the mechanisms underlying mood regulation and therapeutic interventions. -
PKC Inhibitor
NA 0345 is a potent protein kinase C (PKC) inhibitor, exhibiting IC50 values of 70 nM in the presence of 12-O-tetradecanoyl-13-acetate and 110 nM in its absence. This compound selectively inhibits PKC activity, effectively reducing the positive inotropic effects associated with α1-adrenergic receptors. NA 0345 is useful in research applications aimed at elucidating the role of PKC in cardiovascular function and signal transduction pathways. -
Adrenergic Receptor Inhibitor
Cetamolol hydrochloride acts as a potent β1-adrenergic receptor inhibitor, exhibiting intrinsic sympathomimetic activity and cardioselectivity. It demonstrates a prolonged inhibitory effect on heart rate and myocardial contractility at low to moderate doses, making it a valuable reagent for cardiovascular research. Its unique profile allows for exploration in studies evaluating hypertension, arrhythmias, and other cardiac conditions. -
β-Adrenergic Receptor Inhibitor
Bufetolol is a selective β-adrenergic receptor inhibitor that modulates cardiac activity by decreasing the maximum rate of depolarization during action potentials. Its antiarrhythmic properties make it a valuable tool for research into the mechanisms of cardiac rhythm disorders. Bufetolol is utilized in studies aimed at exploring therapeutic strategies for arrhythmias and related cardiovascular conditions. -
Adrenergic Receptor Inhibitor
Teoprolol is a selective β-adrenergic receptor inhibitor that effectively modulates adrenergic signaling pathways. It exhibits key biological activities including the reduction of heart rate and myocardial contractility, making it valuable for cardiovascular research. Teoprolol is widely used in studies investigating hypertension, anxiety, and heart failure, contributing to our understanding of adrenergic receptor function and pharmacological interventions. -
α1/β1-Adrenergic Receptor Inhibitor
Amosulalol hydrochloride functions as a dual inhibitor of α1 and β1-adrenergic receptors, demonstrating pronounced antihypertensive effects. By inhibiting α1-adrenergic receptors, it effectively lowers blood pressure, while β1-adrenergic receptor inhibition reduces reflexive increases in heart rate and plasma renin activity. This compound is particularly useful in studies involving spontaneously hypertensive rats, providing valuable insights into cardiovascular mechanisms and potential therapeutic interventions in hypertension. -
AR Inhibitor
Amidephrine hydrochloride is an adrenergic receptor (AR) agonist that functions primarily by stimulating adrenergic signaling pathways. It demonstrates key biological activities relevant to neurological research, making it a valuable reagent for studying various neurological diseases and disorders. Its effects on AR modulation can facilitate investigations into therapeutic interventions and pharmaceutical development in the field of neuroscience. -
Adrenergic Receptor Inhibitor
Tropodifene is an α-adrenergic receptor inhibitor that modulates adrenergic signaling pathways. It is primarily utilized in research related to cardiovascular pharmacology and the study of sympathetic nervous system functions. Its unique mechanism of action makes it valuable for investigating the role of adrenergic receptors in various physiological and pathological conditions. -
Adrenergic Receptor Inhibitor
Benzquinamide is an adrenergic receptor inhibitor that selectively binds to the α2A, α2B, and α2C adrenergic receptors, exhibiting Ki values of 1,365, 691, and 545 nM, respectively. This compound demonstrates antiemetic properties and is utilized in research applications relating to nausea and vomiting. Its mechanism of action involves modulation of adrenergic signaling pathways, making it a valuable tool for studying the role of adrenergic receptors in various physiological and pathological conditions. -
Adenylate Cyclase Inhibitor
KUM 32 is a potent inhibitor of adenylate cyclase that functions by antagonizing epinephrine-induced platelet aggregation. By selectively binding to the alpha-2 adrenergic receptor on human platelets, KUM 32 modulates platelet activation and aggregation pathways. This compound is utilized in research focused on cardiovascular disease and hemostasis, providing insights into the mechanisms of platelet function. -
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. -
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. -
Adrenergic Receptor Inhibitor
Todralazine hydrochloride is a selective β2 adrenergic receptor inhibitor primarily used in the treatment of hypertension. Its mechanism involves blocking β2 adrenergic receptors, contributing to its effectiveness as an antihypertensive agent. In addition to its receptor inhibition, Todralazine hydrochloride exhibits antioxidant properties, providing potential benefits in research focused on oxidative stress and cardiovascular health. -
α1/β1-Adrenergic Receptor Inhibitor
Amosulalol is a dual inhibitor of the α1 and β1-adrenergic receptors, demonstrating significant antihypertensive activity. By selectively inhibiting the α1-adrenergic receptor, Amosulalol effectively reduces blood pressure, while its β1-adrenergic receptor blockade leads to decreased reflex-induced heart rate and plasma renin activity in spontaneously hypertensive rats. This compound is valuable for research applications focused on cardiovascular physiology and the pharmacological modulation of blood pressure. -
β-AR inhibitor
β-AR antagonist 2 functions as a selective antagonist of β-adrenergic receptors, exhibiting an IC50 value of 0.17 μM. This compound has demonstrated significant inhibitory effects on the growth of mouse A549 xenograft tumors and exhibits cardioprotective properties in a model of doxorubicin-induced heart failure in C57 mice. Its applications in cancer research and cardiovascular studies make it a valuable tool for investigating β-AR signaling pathways. -
Adrenergic Receptor Inhibitor
Napitane is an adrenergic receptor inhibitor that primarily targets α-adrenergic receptors, leading to enhanced catecholamine availability. This compound has demonstrated significant potential in antidepressant research, highlighting its efficacy in modulating neurochemical pathways associated with mood regulation. Napitane serves as a valuable tool for investigating mechanisms underlying depression and exploring novel therapeutic approaches for mood disorders. -
α1 Adrenergic Receptor Inhibitor
Conopeptide rho-TIA is a peptide originating from the venom of the predatory sea snail Conus tulipa, serving as a highly selective noncompetitive inhibitor of the human α1B-adrenergic receptor. It also acts as a competitive inhibitor for both the α1A- and α1D-adrenergic receptors. By selectively binding to these receptor subtypes, conopeptide rho-TIA offers valuable insights for the development of novel, subtype-selective α1-adrenergic receptor therapies. Its unique mechanism of action makes it a potent tool for cardiovascular and pharmacological research. -
Adrenergic Receptor Inhibitor
(+)-Amosulalol is an adrenergic receptor inhibitor that serves as an orally active dual blocker of α1 and β1-adrenergic receptors. This compound demonstrates significant antihypertensive activity by selectively inhibiting α1-adrenergic receptors, while also reducing reflex tachycardia and plasma renin activity in spontaneously hypertensive rats through β1-adrenergic receptor inhibition. As a valuable research tool, (+)-Amosulalol can be employed in studies related to cardiovascular physiology and pharmacology. -
Adrenergic Receptor Inhibitor
Besipirdine is an adrenergic receptor inhibitor that exhibits non-receptor-dependent cholinomimetic properties. This compound is known to inhibit voltage-dependent sodium and potassium channels, contributing to its pharmacological profile. Besipirdine's biological activity makes it relevant for research applications focused on neuropharmacology and the modulation of synaptic transmission. -
Adrenergic Receptor Inhibitor
Moprolol is a beta-adrenergic receptor inhibitor that primarily targets beta-adrenergic receptors to modulate cardiovascular responses. This compound is useful in research related to essential hypertension studies, enabling investigations into its effects on blood pressure regulation and heart rate modulation. Its properties make it a valuable tool for exploring the role of adrenergic signaling in hypertensive conditions. -
Adrenergic Receptor Inhibitor
JNJ-7925476 hydrochloride is a triple monoamine uptake inhibitor that targets adrenergic receptors to modulate neurotransmitter availability. It demonstrates significant antidepressant activity, as evidenced by increased extracellular levels of serotonin, dopamine, and norepinephrine in the rat cerebral cortex. This compound is applicable in preclinical research to investigate the mechanisms underlying mood disorders and therapeutic interventions. Additionally, its rapid absorption and higher concentration in the brain support its potential for effective neurological studies. -
α2A/α2B AR Inhibitor
BRL-44408 is a selective antagonist of the α2A and α2B adrenergic receptors. It effectively inhibits the actions of norepinephrine and the agonist Clonidine on the release of [3H]norepinephrine and [3H]5-hydroxytryptamine in K+-stimulated conditions. With a higher affinity for α2A-adrenoceptors in human platelet membranes compared to other antagonists, BRL-44408 may play a significant role in modulating neurotransmitter release, making it a valuable tool for research in adrenergic signaling and related pharmacological studies. -
NET Inhibitor
XEN-2174 is a selective noradrenaline transporter (NET) inhibitor that functions through non-competitive inhibition of noradrenaline reuptake. By increasing the synaptic concentration of noradrenaline, it activates α2-adrenergic receptors at the spinal level, leading to pronounced analgesic effects. This compound demonstrates sustained analgesia in various models of neuropathic and postoperative pain in rats, making it a valuable tool for pain research applications. -
Adrenergic Receptor Inhibitor
(-)-Amosulalol is a selective inhibitor of α1/β1-adrenergic receptors, demonstrating dual action in pharmacological studies. It exhibits antihypertensive properties primarily through the blockade of α1-adrenergic receptors, effectively reducing peripheral vascular resistance. Additionally, (-)-Amosulalol decreases reflex tachycardia and plasma renin activity in models of hypertension, making it valuable for research in cardiovascular diseases and hypertension management. -
Adrenergic Receptor Inhibitor
IMTPPE is an adrenergic receptor inhibitor that selectively targets the androgen receptor (AR) in prostate cancer cells. It effectively inhibits AR transcriptional activity and reduces protein levels, leading to decreased proliferation of AR-positive prostate cancer cells, while showing no effect on AR-negative cells. Additionally, IMTPPE demonstrates significant anti-tumor activity against enzalutamide-resistant 22Rv1 xenograft tumors, making it a valuable tool for studying AR signaling pathways and developing therapeutic strategies for resistant prostate cancer. -
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. -
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. -
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. -
5-HT/NE Reuptake Inhibitor
Dextromilnacipran is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor, derived from the enantiomeric form of milnacipran. This compound also functions as a human alpha-adrenergic receptor antagonist, exhibiting an IC50 value of 3.4 μM. Dextromilnacipran is primarily utilized in research applications targeting mood disorders and neuropharmacology, facilitating investigations into its psychiatric and physiological effects. -
ARα2c Inhibitor
BAY-2925976 is an α2C adrenergic receptor (ARα2C) inhibitor that selectively blocks receptor activity. This compound is primarily utilized in research related to obstructive sleep apnea (OSA), providing insights into its underlying mechanisms and potential therapeutic approaches. BAY-2925976 aids in elucidating the role of ARα2C in respiratory regulation and sleep disorders.
