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β-adrenergic Receptor Antagonist
Ridazolol is a selective β-adrenergic receptor antagonist with a primary affinity for the β-1 adrenergic receptor (β1AR). It exhibits moderate intrinsic sympathomimetic activity (ISA) and effectively competes with isoproterenol to inhibit its relaxation effects. This compound is valuable in the investigation of cardiovascular diseases, providing insights into β-adrenergic signaling pathways and potential therapeutic approaches. -
β(3)-adrenergic Receptor Agonist
L-796568 free base is a potent β(3)-adrenergic receptor agonist. This compound plays a crucial role in research related to obesity and metabolic disorders, facilitating the investigation of adipose tissue regulation and energy expenditure. By targeting the β(3)-adrenergic receptor, L-796568 free base aids in understanding potential therapeutic approaches for weight management and related conditions. -
α1-Adrenergic Receptor Blocker
Trimazosin hydrochloride hydrate is an α1-adrenergic receptor blocker that demonstrates significant hypotensive effects. As a quinazoline derivative structurally related to prazosin, it selectively inhibits α1-adrenergic receptors, contributing to the regulation of blood pressure. This compound is primarily utilized in research on hypertension and related cardiovascular conditions. -
β3 Adrenergic Receptor Agonist
L-770644 dihydrochloride is a potent and selective agonist of the human β3 adrenergic receptor, with an EC50 value of 13 nM. This compound is primarily utilized in research applications exploring metabolic regulation, adipocyte function, and energy expenditure. Its oral bioactivity makes it a valuable tool for studying β3 adrenergic receptor-mediated pathways in various biological contexts. -
β3-Adrenergic Agonist
Trecadrine is a potent β3-adrenergic agonist that selectively activates β3-adrenergic receptors. This compound is known for its role in promoting lipolysis and thermogenesis, making it a valuable tool in metabolic research. Trecadrine is commonly utilized in studies examining obesity, energy expenditure, and the physiological roles of β3-adrenergic signaling pathways. -
Adrenergic Receptor Agonist
β3-AR agonist 2 is a selective agonist of the β3-adrenergic receptor, exhibiting high potency with an EC50 of 8 nM. This compound is instrumental in various research applications, particularly in studies related to metabolic regulation, thermogenesis, and obesity. Its ability to selectively activate β3-AR makes it a valuable tool for exploring adipocyte function and potential therapeutic pathways for metabolic disorders. -
Adrenergic Receptor Modulator
α1 adrenoceptor-MO-1 is an S enantiomer that selectively targets the alpha-1 adrenergic receptor. This compound exhibits alpha-lytic activity and demonstrates analgesic properties, making it more effective than its R enantiomer counterpart. α1 adrenoceptor-MO-1 is suitable for research applications focused on adrenergic signaling and pain modulation. -
Adrenergic Receptor Modulator
D2343 is a β2-adrenoceptor agonist and α1-adrenoceptor inhibitor. This compound exhibits a dual mechanism of action, enhancing β2 receptor activation while simultaneously blocking α1 receptors. It is utilized in research applications that investigate adrenergic signaling pathways and the physiological effects mediated by these receptors. -
Adrenergic Receptor Agonist
Epanolol is a selective β-adrenoceptor partial agonist, demonstrating a higher affinity for β1-adrenoceptors compared to β2-adrenoceptors. This compound exhibits significant cardiovascular effects, making it useful in research focused on heart-related therapies and the modulation of adrenergic signaling pathways. Its specificity for β1-adrenergic receptors lends valuable insight into cardiac function and potential treatments for hypertension and other cardiovascular diseases. -
Adrenergic Receptor Antagonist
Fiduxosin is a potent α1-adrenoceptor antagonist, exhibiting Ki values of 0.160 nM, 24.9 nM, and 0.920 nM for the α1a, α1b, and α1d subtypes, respectively. This compound inhibits adrenergic signaling, making it a valuable tool in the study of cardiovascular and urological diseases. Its selective modulation of α1-adrenoceptors allows for targeted research applications in pharmacology and drug development. -
Adrenergic Receptor Antagonist
MG 1 is a selective α1 adrenergic receptor antagonist, primarily designed to inhibit the activity of these receptors. This compound demonstrates significant biological activity in modulating vascular smooth muscle contraction and has applications in studying cardiovascular function and related signal transduction pathways. MG 1 is valuable for researchers investigating the roles of adrenergic signaling in various physiological and pathological conditions. -
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. -
Adrenergic Receptor
GP2-114 is a selective adrenergic receptor modulator that exhibits current-dependent cardiovascular effects. It is utilized in experimental models to study the physiological impacts on cardiovascular function and adrenergic signaling pathways. The compound offers valuable insights into the role of adrenergic receptors in cardiovascular responses, supporting various research applications in pharmacology and cardiovascular physiology. -
Adrenergic Receptor Agonist
ZK-90055 hydrochloride is a selective β2 adrenergic receptor agonist known for its ability to activate β2 receptors, influencing various physiological responses. This compound is primarily utilized in cardiovascular research and studies related to asthma and bronchial dilation. Its potent agonistic effects on β2 receptors make it a valuable tool for investigating adrenergic signaling pathways and developing therapeutic interventions for related disorders. -
Adrenergic Receptor Antagonist
Fenmetozole Tosylate is an adrenergic receptor antagonist primarily targeting the α2-adrenergic receptor. This compound has been shown to counteract the actions of ethanol and exhibits potential antidepressant properties. It is useful in research applications focused on understanding the mechanisms of alcohol-related effects and the modulation of mood disorders. -
Adrenergic Receptor Agonist
AR-08 is an agonist of the α2-adrenergic receptor, primarily involved in modulating neurotransmitter release and synaptic transmission. This compound exhibits key biological activity in the central nervous system, making it relevant for research into disorders such as attention deficit hyperactivity disorder (ADHD). AR-08 can be utilized to explore adrenergic signaling pathways and assess therapeutic potential in neuropsychiatric applications. -
Adrenergic Receptor Antagonist
Bometolol Hydrochloride is a selective beta-adrenergic receptor antagonist primarily targeting β1-adrenergic receptors. With its capacity to inhibit adrenergic signaling, it is employed in research focused on cardiovascular diseases, particularly in studies investigating heart rate regulation and blood pressure modulation. This compound provides valuable insights into the mechanisms underlying cardiac function and the therapeutic potential for hypertension and related disorders. -
Adrenergic Receptor Antagonist
Falintolol, (Z)- is a selective β-adrenergic receptor antagonist known for its unique oxime functionality. This compound exhibits key biological activity by blocking β-adrenergic signaling pathways, making it valuable for studies in cardiovascular research and the regulation of metabolic processes. Its ability to interact with adrenergic receptors provides insights into the pharmacological modulation of various physiological responses. -
Adrenergic Receptor Antagonist
Phentolamine Analogue 1 is a nonselective alpha-adrenergic receptor antagonist. This compound demonstrates significant inhibitory activity against adrenergic signaling pathways, making it a valuable tool for studying cardiovascular regulation and neuropharmacology. Its application in research may include investigations into blood pressure modulation, vasodilation mechanisms, and the effects of adrenergic receptor blockade in various biological systems. -
Amylin Receptor Antagonist
AC 187 is a potent and orally bioavailable antagonist of the amylin receptor, exhibiting an IC50 of 0.48 nM and a Ki of 0.275 nM. This compound demonstrates selectivity for the amylin receptor over calcitonin and CGRP receptors. AC 187 has been shown to possess neuroprotective effects, making it a valuable tool for research in neurodegenerative diseases and metabolic disorders. -
Amylin Receptor/Calcitonin Receptor/CGRP Receptor Agonit
Davalintide is a potent agonist of the amylin receptor, calcitonin receptor, and calcitonin gene-related peptide (CGRP) receptor, demonstrating high affinity with IC50 values of 0.04 nM, 0.06 nM, and 3.1 nM, respectively. It effectively stimulates cyclic AMP production via the calcitonin receptor, with an EC50 of 1.4 nM. Davalintide has been shown to regulate blood glucose levels and body weight through mechanisms such as delaying gastric emptying, inhibiting glucagon secretion, and suppressing food intake. This peptide is valuable for research applications focused on obesity and diabetes management. -
GLP-1/Amylin Agonist
Zenagamtide is a GLP-1 and amylin receptor agonist that acts as a triple agonist also targeting the calcitonin receptor. It is a peptide comprising 68 amino acids and is capable of crossing the blood-brain barrier, making it effective in modulating appetite and reducing energy intake. Research suggests that Zenagamtide may lead to improvements in body weight, waist circumference, glycated hemoglobin, and lipid profiles, while also enhancing insulin sensitivity and ameliorating features of metabolic dysfunction-associated steatotic liver disease (MASLD). Its biological activity makes it valuable for investigating conditions related to overweight, obesity, and insulin resistance. -
Angiotensin Receptor
CNP-38 is a C-type natriuretic peptide that primarily targets the angiotensin receptor. This compound exhibits potent biological activity associated with vasodilation and blood pressure regulation. CNP-38 is valuable in research applications related to cardiovascular physiology and potential therapeutic strategies for hypertension and heart failure. -
Angiotensin Receptor
Angiotensin II (5-8), human is a biologically active C-terminal fragment of the vasoconstrictor angiotensin II, targeting the angiotensin II type 1 (AT1) receptor. This fragment activates G protein-coupled receptors (GPCRs) in vascular smooth muscle cells, leading to increased intracellular calcium levels and vasoconstriction. Additionally, Angiotensin II (5-8) influences renal function by interacting with the Na+/H+ exchanger in the proximal tubules, making it a valuable tool for research in cardiovascular and renal physiology. -
Angiotensin Receptor Antagonist
Valsartan-d9 is a deuterated form of valsartan, an angiotensin II receptor antagonist. This compound is primarily used in research related to hypertension and heart failure, facilitating investigations into the mechanisms of blood pressure regulation and cardiovascular health. Its unique isotopic labeling allows for advanced tracking and analysis in pharmacokinetic and metabolic studies. -
Angiotensin Receptor Antagonist
Olmesartan lactone impurity is a cyclic ester derivative associated with Olmesartan, an angiotensin II receptor (AT1R) antagonist. This impurity can serve as a reference standard in analytical studies and quality control processes for assessing Olmesartan purity. Its relevance in hypertension research underscores its importance in understanding the pharmacological profiles of angiotensin receptor modulators. -
Angiotensin Receptor Activator
DuP-532 is an angiotensin type 1 receptor antagonist that plays a crucial role in the management of hypertension and heart failure. This compound is capable of reacting with various aryl and heteroaryl halides to yield perfluoroalkyl(hetero)arenes efficiently. Additionally, computational studies indicate that the introduction of a secondary phenyl ring ligand can decrease the energy barrier for the decarboxylation of perfluorocarboxylates, facilitating the perfluoroalkylation process. -
Angiotensin Receptor Inhibitor
H-Val-Pro-Pro-OH TFA is an inhibitor of Angiotensin I converting enzyme (ACE), demonstrating an IC50 of 9 μM. This milk-derived proline peptide derivative is utilized in research applications focused on cardiovascular biology and hypertension. Its role in modulating the renin-angiotensin system makes it a valuable tool for studying the effects of ACE inhibition in various physiological and pathological contexts. -
Angiotensin Receptor Antagonist
Dehydro Olmesartan is a potent angiotensin II receptor (AT1R) antagonist, derived from Olmesartan. This compound exhibits significant antihypertensive activity, making it valuable for research focused on hypertension and cardiovascular diseases. Its ability to inhibit AT1R provides insights into the mechanisms underlying blood pressure regulation and potential therapeutic strategies. -
Angiotensin Receptor Antagonist
Tetrahydro Aldosterone is an angiotensin receptor antagonist that effectively inhibits adrenal angiotensin II receptors, demonstrating an IC50 of 10 μM. This compound is utilized in research to investigate the role of the renin-angiotensin system in cardiovascular and renal physiology. Its application extends to exploring mechanisms of hypertension and related disorders. -
Angiotensin II Analogue
[Sar1, Ile8]-Angiotensin II is a synthetic analogue of angiotensin II that primarily targets angiotensin receptors, inducing various physiological effects. This peptide is known to elicit vasoconstriction in normal arterial tissue and promotes hypertrophic or hyperplastic responses in cultured vascular smooth muscle cells and diseased vasculature. Its versatile biological activity makes it valuable in research applications focused on cardiovascular physiology, vascular remodeling, and related pathophysiological processes. -
Angiotensin Receptor
ZD 7155 is a selective antagonist of the angiotensin II type 1 receptor (AT1R), known for its effects on renal function. Research indicates that ZD 7155 modulates electrolyte excretion, particularly increasing the excretion of sodium, potassium, and chloride in postnatal lamb models. In studies involving 6-week-old lambs, pretreatment with ZD 7155 significantly enhanced urine flow rates and free water clearance, while also reducing urine osmolality. This compound is essential for investigating the role of AT1R in renal physiology and the interactions with nitric oxide in electrolyte regulation. -
Angiotensin Receptor Antagonist
Olmesartan medoxomil impurity C is a chemical impurity related to Olmesartan medoxomil, a selective antagonist of the angiotensin AT1 receptor. It exhibits inhibitory activity with an IC50 value of 66.2 μM, making it relevant for studies focused on hypertension and cardiovascular disorders. This impurity can serve as a reference standard in the characterization and analytical assessment of Olmesartan medoxomil formulations in research applications. -
Angiotensin Receptor Activator
Mitolactol, an angiotensin receptor activator, exhibits effective inhibition of angiotensin-converting enzyme (ACE) with an IC50 value of 1.4 × 10 M. This compound is known for its ability to suppress the pressor response to angiotensin I when administered intravenously at a dose of 0.3 mg/kg in rat models. Mitolactol is of interest for research focusing on cardiovascular physiology, hypertension, and related therapeutic applications. -
Angiotensin II Analog
Nva-VYIHPF is an analog of Angiotensin II that selectively targets the angiotensin receptor type 1 (AT1). This compound exhibits potent binding affinity and biological activity, making it valuable for studying the renin-angiotensin system. Researchers can utilize Nva-VYIHPF in various applications, including cardiovascular research, hypertension studies, and investigations into cellular signaling pathways influenced by angiotensin II. -
Angiotensin Receptor
[Tyr(P)4] Angiotensin II is a phosphopeptide analog of angiotensin II that primarily targets the angiotensin receptor. It is known to induce vasoconstriction in normal arterial smooth muscle and promote cellular hypertrophy or hyperplasia in cultured cells and diseased vascular tissues. This compound is valuable for research into cardiovascular physiology, hypertension, and related pathologies. -
Antiarrhythmic Compounds
BW A256C is an antiarrhythmic compound that acts as both an angiotensin-converting enzyme inhibitor and a beta-adrenergic receptor blocker. This dual action contributes to its effectiveness in modulating cardiovascular responses and stabilizing cardiac rhythm. BW A256C serves as a valuable tool for research focused on cardiac arrhythmias and related cardiovascular conditions. -
Angiotensin Receptor Agonist
Angiotensin II (1-4), human is an endogenous peptide that functions as an agonist for the angiotensin receptor. It primarily binds to the AT II type 1 (AT1) receptor, activating GPCRs in vascular smooth muscle cells, which leads to an increase in intracellular calcium levels. Additionally, Angiotensin II (1-4) influences the sodium/hydrogen exchanger in the proximal tubules of the kidney, playing a critical role in regulating blood pressure and fluid balance. This peptide is valuable for research applications related to cardiovascular function and renal physiology. -
Angiotensin Receptor Antagonist
Saprisartan potassium is a selective angiotensin II receptor type 1 (AT1) antagonist that exhibits long-lasting effects. It demonstrates notable hypotensive activity by inhibiting the AT1 receptor, which plays a crucial role in the regulation of blood pressure and fluid balance. This compound is primarily utilized in research applications related to cardiovascular physiology, hypertension studies, and the investigation of renin-angiotensin system modulation. -
Angiotensin Receptor Agonist
Angiotensin II (3-8), human is a selective agonist of the angiotensin AT1 receptor. Though it exhibits reduced efficacy compared to its full-length counterpart, it serves as a valuable tool in studies investigating angiotensin receptor signaling pathways. This compound is utilized in cardiovascular research and the exploration of blood pressure regulation mechanisms. -
Angiotensin Receptor Antagonist
Saprisartan is a selective angiotensin II type 1 (AT1) receptor antagonist known for its long-acting effects and low receptor dissociation kinetics. It effectively inhibits the binding of angiotensin II, resulting in vasodilation and a decrease in blood pressure. This compound is utilized in research to explore its potential benefits in treating hypertension and related cardiovascular conditions. -
Angiotensin Receptor Activator
AZ11657312 is an angiotensin receptor activator that enhances renal medullary perfusion in the context of angiotensin II treatment. This compound significantly improves tissue oxygenation by inhibiting P2X7 receptor activity, particularly in underoxygenated regions of the kidney. AZ11657312 has been shown to increase sodium excretion dramatically, up to sixfold, while also normalizing blood pressure. Its unique mechanism and biological activity make it a valuable tool for studying renal function and hypertension. -
Angiotensin Receptor Activator
BRL-36378 is an angiotensin receptor activator that modulates the activity of angiotensin-converting enzyme. This compound exhibits significant biological activity, making it valuable for research applications focused on cardiovascular and renal systems. Additionally, BRL-36378 serves as a useful tool in ligand-based virtual screening for the identification of novel lead compounds suitable for chemical optimization. -
Angiotensin Receptor Antagonist
L162441 is an antagonist of the angiotensin type 1 receptor. It selectively inhibits receptor activation, leading to decreased vasoconstriction and reduced blood pressure. This compound is primarily utilized in cardiovascular research to investigate the role of angiotensin signaling in hypertension and other related disorders. -
Angiotensin Receptor Antagonist
LY285434 is a potent angiotensin II receptor antagonist that selectively inhibits the binding of angiotensin II to its receptors. This compound demonstrates significant biological activity in regulating blood pressure and fluid balance, making it a valuable tool for research in cardiovascular physiology and related disorders. Its application includes studying the role of the renin-angiotensin system in hypertension and exploring potential therapeutic strategies for related diseases. -
Angiotensin Receptor Antagonist
A81988 is a potent, competitive antagonist that targets angiotensin AT1 receptors. This non-peptidic compound demonstrates significant inhibition of receptor activity, making it a valuable tool for studying angiotensin signaling pathways. A81988 is applicable in research focused on cardiovascular disorders and hypertension, offering insights into therapeutic interventions for related conditions. -
CXCR6 Antagonist
ML339 is a selective antagonist of the CXCR6 receptor, displaying an IC50 of 140 nM. It inhibits β-arrestin recruitment and the cAMP signaling pathway induced by CXCL16 in human CXCR6, with IC50 values of 0.3 μM and 1.4 μM, respectively. While exhibiting reduced efficacy against mouse CXCR6 with an IC50 of 18 μM, ML339 demonstrates no significant inhibition of CXCR5, CXCR4, or the apelin receptor (APJ), with IC50 values exceeding 79 μM. This compound shows promise for advancing research focused on prostate cancer. -
CXCR Inhibitor
ALX 40-4C is a small peptide inhibitor targeting the chemokine receptor CXCR4. It effectively prevents the binding of SDF-1 to CXCR4 with a Ki of 1 μM, thereby inhibiting the replication of X4 strains of HIV-1. Additionally, ALX 40-4C Trifluoroacetate serves as an antagonist of the APJ receptor, exhibiting an IC50 value of 2.9 μM. This dual activity makes ALX 40-4C a valuable tool for research in HIV-1 studies and chemokine receptor signaling pathways. -
CB1 Antagonist
Monlunabant is a selective antagonist of the cannabinoid receptor 1 (CB1) with an inhibitory constant (Ki) of 0.3 nM for human CB1 receptors, and 613 nM for human CB2 receptors. This compound demonstrates potent activity in modulating cannabinoid signaling pathways, making it a valuable tool for researching the roles of CB1 in various physiological processes. Its applications include the exploration of metabolic disorders, neurodegenerative diseases, and potential therapeutic interventions involving the endocannabinoid system.

