Catalog No.
Product Name
Application
Product Information
Citations
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CRFR Antagonist
DMP 904 is a noncompetitive antagonist of the corticotropin-releasing factor receptor (CRFR), effectively inhibiting CRF-stimulated adenylate cyclase activity and adrenocorticotropic hormone (ACTH) release. This compound demonstrates significant antidepressant and anxiolytic properties, making it a valuable tool for research in stress-related disorders and neuropsychiatric conditions. Its mechanism of action can provide insights into the therapeutic potential for anxiety and depression treatments. -
CGRP Agnalogue
[Tyr22] Calcitonin Gene Related Peptide, (22-37), rat is a CGRP analogue that targets the CGRP receptor and modulates adenylate cyclase activity. This peptide fragment, derived from the rat CGRP sequence, exhibits key biological activities associated with pain modulation and vasodilation. It is suitable for research applications studying neurogenic inflammation, cardiovascular regulation, and the pathophysiology of migraine headaches. -
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. -
GCGR Antagonist
Glucagon receptor antagonist-7 is a potent inhibitor of the human glucagon receptor (hGCGR), demonstrating an IC50 of 181 nM for blocking the binding of 125I-labeled glucagon. With a KDB of 81 nM, it inhibits glucagon-stimulated adenylyl cyclase activity in CHO cells. This compound effectively reduces glucagon-mediated glycogenolysis in human hepatocytes and has been shown to lower blood glucose levels, making it a valuable tool for research in glucose metabolism and diabetes therapeutic strategies. -
sst2/sst5 Receptor Partial Agonist
Angiopeptin is a cyclic octapeptide analogue of somatostatin that acts as a partial agonist at the sst2 and sst5 receptors, exhibiting IC50 values of 0.26 nM and 6.92 nM, respectively. This compound effectively inhibits growth hormone secretion and reduces insulin-like growth factor-1 (IGF-1) production. Angiopeptin also modulates cellular signaling by inhibiting adenylate cyclase and stimulating extracellular acidification. Its unique properties make it a valuable tool for research into coronary atherosclerosis and related metabolic disorders. -
Adrenergic Receptor Agonist
Phenylephrine is a selective α1-adrenoceptor agonist that primarily functions as a decongestant. It exerts its biological activity by inducing vasoconstriction, leading to decreased nasal congestion. This compound is widely utilized in research applications related to cardiovascular studies, nasal physiology, and adrenergic receptor signaling pathways. -
Analgesic
α2AR agonist 2 is a selective agonist for the α2B adrenergic receptor, demonstrating an IC50 of 1.2 µM. This compound is primarily utilized in research focused on analgesic effects, particularly in the contexts of inflammatory and neuropathic pain. Its selective action makes it a valuable tool for studying pain modulation pathways and developing novel therapeutic strategies. -
β-Adrenoceptor Agonist
(-)-Isoproterenol hydrochloride is a potent β-adrenoceptor agonist. It primarily acts on β1 and β2 adrenergic receptors, resulting in increased heart rate and myocardial contractility. This compound is widely used in research related to cardiac function and ventricular remodeling, making it essential for studies exploring cardiovascular physiology and related therapeutic interventions. -
β3-AR Antagonist
SR59230A is a potent and selective antagonist of the β3-adrenergic receptor, demonstrating IC50 values of 40 nM, 408 nM, and 648 nM for β3, β1, and β2 receptors, respectively. Its ability to penetrate the blood-brain barrier makes it a valuable tool for exploring the physiological roles of β3-AR in the central nervous system. This compound is primarily utilized in research related to metabolic disorders, obesity, and cardiovascular diseases, providing insight into the therapeutic potential of β3-AR modulation. -
α1/β-adrenergic Receptors Antagonist
Labetalol is a competitive antagonist of α1-adrenergic and non-selective β-adrenergic receptors. This antihypertensive agent is orally bioavailable and effectively addresses hypertension by reducing peripheral vascular resistance with minimal impact on cardiac output. Labetalol is particularly relevant for research on cardiovascular diseases, including hypertension during pregnancy, and its ability to partially traverse the blood-brain barrier also makes it a candidate for neurological studies of vascular conditions. -
β3 Adrenergic Receptor Antagonist
L748337 is a selective β3-adrenergic receptor antagonist with a high affinity for the β3 receptor (Ki = 4.0 nM) compared to β1 (Ki = 390 nM) and β2 receptors (Ki = 204 nM). This compound predominantly couples to Gi proteins, leading to the activation of MAPK signaling pathways, which subsequently enhances the phosphorylation of Erk1/2 with a pEC50 value of 11.6. L748337 is applicable in research focused on cancer, nonalcoholic fatty liver disease (NAFLD), and various cardiovascular disorders. -
CXCR7 Antagonist
CXCR7 antagonist-1 functions as a CXCR7 antagonist by inhibiting the binding of the SDF-1 (CXCL12) and I-TAC (CXCL11) chemokines to the CXCR7 receptor. This inhibition plays a critical role in suppressing tumor cell proliferation and tumor growth, thereby providing potential therapeutic applications in cancer treatment. Additionally, CXCR7 antagonist-1 may be beneficial in the study and management of various inflammatory diseases and other pathologies associated with the CXCR7 pathway. -
β2-Adrenergic Receptor Blocker
Butaxamine hydrochloride is a specific antagonist of the β2-adrenergic receptor. This compound effectively inhibits the reduction of urine volume in ethanol-anesthetized, water-diuretic rats, demonstrating its role in regulating diuresis. Butaxamine hydrochloride is valuable for studying β2-adrenergic receptor signaling and its implications in renal function and fluid regulation. -
β/α-1 Blocker
(S)-Carvedilol is a non-selective β/α-1 blocker that primarily targets adrenergic receptors. This compound demonstrates protective effects against the vascular and cardiac toxicity induced by Doxorubicin (DOX). It is utilized in research related to cardioprotection and the mitigation of chemotherapy-related side effects. -
α Blocker
(R)-Carvedilol primarily targets alpha (α) adrenergic receptors, acting as an α-blocker while exhibiting no β-receptor activity. This compound is noted for its ability to inhibit spontaneous Ca2+ waves, thereby contributing to its cardioprotective effects. Research applications for (R)-Carvedilol include the study of stress-induced ventricular tachycardia and the potential inhibition of UV-induced skin tumor development, suggesting its utility in cancer research and cardiovascular studies. -
α2A Agonist
Guanfacine functions as a selective α2A adrenergic receptor agonist, exhibiting potent noradrenergic activity. Its mechanism leads to reduced sympathetic outflow, resulting in hypotension and sedation. Guanfacine is utilized in research related to prefrontal cortex cognitive disorders, including Tourette’s syndrome and attention deficit hyperactivity disorder (ADHD), making it valuable for understanding the pharmacological modulation of these conditions. -
β1-AR Agonist
Dobutamine is a synthetic catecholamine that acts primarily as a selective agonist of the β1-adrenergic receptor (β1-AR). It is known to enhance cardiac output and improve conditions of hypoperfusion by elevating heart rate and contractility. Dobutamine is utilized in various research applications, including studies on cardiac function, mechanisms of heart failure, and other cardiovascular disorders. -
Adrenergic Receptor Agonist
Xamoterol hemifumarate is a selective and potent agonist of the beta-1 adrenergic receptor. It has significant potential for studying arrhythmogenesis and elucidating the relationship between β1-adrenergic stimulation and the potassium ion channel IKr. This compound is valuable for research applications focused on cardiac function and the mechanisms underlying arrhythmic conditions. -
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.
