Catalog No.
Product Name
Application
Product Information
Citations
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Stable Isotope
(Rac)-Ambrisentan-d3 is a deuterated form of (Rac)-Ambrisentan, a selective endothelin receptor antagonist. This stable isotope is utilized in pharmacokinetic studies and metabolic research, allowing for precise tracking of drug metabolism and distribution in biological systems. Its application is essential for understanding the pharmacological properties and efficacy of endothelin receptor-targeted therapies. -
ETA Receptor Antagonist
Sulfatroxazole is a selective antagonist of the endothelin A (ETA) receptor, with an IC50 value of 0.26 μM. This compound is primarily utilized in research focused on cardiovascular disease and pulmonary hypertension by inhibiting the effects of endothelin-1, a potent vasoconstrictor. Its application in biological studies provides insights into the role of ETA signaling in various pathophysiological conditions. -
ETB Agonist
[Ala1,3,11,15]-Endothelin (53-63) is a selective agonist for the ETB receptor, exhibiting potent activity with IC50 values between 0.33 nM and 0.61 nM. This compound is valuable for research focused on vasoconstriction and related physiological processes. Its specificity for the ETB receptor makes it a useful tool for investigating the role of endothelins in vascular biology and potential therapeutic applications. -
ETA Antagonist
BMS-193884 is a selective, orally active antagonist of the endothelin A (ETA) receptor, exhibiting a significant 10,000-fold increased affinity for this target (Ki=1.4 nM) compared to the endothelin B (ETB) receptor. This compound is primarily utilized in research applications focused on vascular biology, cardiovascular conditions, and pathology related to endothelin signaling. Its potent inhibition of ETA receptor activity makes it a valuable tool for investigating endothelin-mediated processes and therapeutic intervention strategies. -
Endothelin Receptor Agonist
[Lys4] Sarafotoxin S6c is a potent partial agonist of the endothelin receptor. This sarafotoxin analogue induces contraction in pig coronary artery tissues, demonstrating an EC50 of 1.5 nM. It serves as a valuable tool for research in cardiovascular physiology and the study of endothelin receptor signaling pathways. -
ETB Receptor Antagonist
RES-701-1 is a cyclic peptide that serves as a specific antagonist for the endothelin receptor type B (ETB). This compound effectively inhibits the binding of 125I-labeled endothelin-1 (ET-1) to the ETB receptor, demonstrating an IC50 value of 10 nM. RES-701-1 is primarily utilized for research applications aimed at studying the role of ETB receptors in cardiovascular and other physiological processes. -
ETA Antagonist
Edonentan hydrate is a potent and selective antagonist of the endothelin A (ETA) receptor, exhibiting a high affinity with a Ki value of 10 pM. This compound demonstrates 100% oral bioavailability in rat models, making it an effective tool for in vivo studies. Edonentan hydrate is primarily utilized in research focused on cardiovascular disease and other conditions where endothelin signaling is implicated. -
ET-A Receptor Antagonist
JKC 302 is an endothelin-1 (ET-1) receptor type A (ET-A) antagonist that inhibits ET-1-induced contraction in asthmatic rat trachea rings. This compound serves as a valuable tool for studying the role of endothelin signaling in respiratory conditions and may aid in the development of therapeutic strategies for asthma and related disorders. Its application in research provides insights into the mechanisms underlying airway hyperreactivity and constriction. -
Endothelin-B Receptor Antagonist
PD 142893 is an endothelin-B receptor antagonist that selectively inhibits the action of endothelin-1, a potent vasoconstrictor. This compound demonstrates significant biological activity in modulating blood pressure and vascular resistance, making it a valuable tool in cardiovascular research. PD 142893 is widely used to study the role of endothelin signaling in various physiological and pathological conditions, including pulmonary hypertension and heart failure. -
ETB Antagonist
K-8794 is a selective endothelin receptor type B (ETB) antagonist that exhibits oral bioactivity. This compound is valuable for investigating its potential therapeutic effects in cardiovascular diseases by modulating endothelin-mediated pathways. K-8794 can aid in elucidating the role of ETB receptors in various biological processes and support research on related cardiovascular conditions. -
Endothelin ETA Receptor Antagonist
S-1255 is a highly selective endothelin ETA receptor antagonist with a dissociation constant (Kd) of 0.39 nM. This compound effectively inhibits vasoconstriction, leading to sustained hypotensive effects in hypertensive animal models. S-1255 serves as a valuable tool in the study of hypertension and related cardiovascular disorders, providing insights into the endothelin signaling pathway and its role in vascular regulation. -
Endothelin-A Antagonist
BMS-187308 is an orally active antagonist of the endothelin-A (ETA) receptor, exhibiting a Ki of 4.7 nM for ETA and a Ki of 1.7 μM for ETB. This compound effectively inhibits the pressor response to endothelin-1 (ET-1) with an ED25 value of 1.2 µmol/kg when administered intravenously. BMS-187308 serves as a valuable tool for research focused on the physiological and pathophysiological roles of endothelin in various biological systems. -
Endothelin Receptor Agonist
Sarafotoxin S6b is a potent vasoconstrictor peptide and a non-selective agonist of endothelin receptors. This compound effectively induces contraction in isolated human coronary arteries, exhibiting Ki values of 0.27 nM, 0.55 nM, and 19.5 nM for the coronary artery, saphenous vein, and coronary artery, respectively. Sarafotoxin S6b is valuable for research applications focused on cardiovascular physiology and the roles of endothelin signaling in vascular constriction. -
Endothelin (ETA) Receptor Antagonist
CI-1020 is a selective antagonist of the endothelin (ETA) receptor, exhibiting an IC50 value of 0.3 nM. This compound effectively inhibits intimal hyperplasia in human saphenous vein organ culture. Furthermore, CI-1020 demonstrates potential in the treatment of hypoxic pulmonary hypertension by blocking ET-1-induced pressor responses following oral administration, making it a valuable tool for research in vascular biology and cardiovascular diseases. -
Endothelin A Receptor Antagonist
Fandosentan potassium is a selective antagonist of the endothelin A receptor (ETAR). It effectively reverses hypoxic pulmonary vasoconstriction in perinatal lamb models, making it a valuable tool for investigating pulmonary hypertension. Additionally, Fandosentan potassium inhibits the activities of CYP2C9 and CYP3A4 with IC50 values of 39.6 μM and 21.6 μM, respectively, supporting its application in exploring drug metabolism and interactions. -
ETB Receptor Agonist
BQ-3020 is a selective endothelin receptor (ETB receptor) agonist known for its ability to displace [125I] ET-1 binding at ETB receptors, exhibiting an IC50 of 0.2 nM. This compound induces vasoconstriction in the rabbit pulmonary artery and promotes relaxation of the pig urinary bladder neck. BQ-3020 is valuable for research in cardiovascular diseases, providing insights into endothelin signaling pathways and their physiological implications. -
ETA Receptor Antagonist
PD 155080 is a selective antagonist of the endothelin A (ETA) receptor. It effectively reduces coronary resistance in isolated rat heart models and enhances both systolic and diastolic myocardial function in ischemia/reperfusion studies. This reagent is valuable for research focused on cardiovascular diseases, including the investigation of endothelin's role in cardiac function and pathology. -
Endothelin converting enzyme inhibitor
Daglutril targets the endothelin receptor, exhibiting the ability to modulate cytokine-induced endothelin-1 production in astrocytes. Its inhibitory effects on endothelin-1 generation make it a valuable research tool for screening compounds that regulate this peptide's synthesis in glial cells. This compound is particularly relevant for studies investigating the role of endothelin-1 in neuroinflammation and related neurological disorders. -
Endothelin Receptor Antagonist
TAK 044 is an antagonist of the Endothelin Receptor, exhibiting potent inhibitory effects on endothelin-induced pathological changes in various animal models. This compound is valuable for exploring the role of endothelin in diseases such as acute myocardial infarction, acute renal failure, acute hepatic malfunction, and subarachnoid hemorrhage. Researchers can leverage TAK 044 to investigate therapeutic strategies targeting endothelin-related conditions. -
Endothelin Antagonist
PD 156252 is a highly potent endothelin antagonist, primarily targeting the ETA and ETB receptor subtypes. It exhibits enhanced binding affinity with IC50 values of 1.0 nM for rabbit ETA receptors and 40 nM for rat ETB receptors. This compound is valuable for research applications focusing on the endothelin system, cardiovascular studies, and investigations into related pathophysiological conditions. -
ETA Receptor Antagonist
BQ-610 is a selective antagonist of the endothelin A receptor (ETA), functioning as a competitive inhibitor of endothelin-1 (ET-1) binding. This inhibition leads to the attenuation of vascular smooth muscle contraction, reduction in cell mitosis, and diminished hormone secretion. BQ-610 has demonstrated efficacy in alleviating cerebral vasospasm in animal models, inhibiting bronchial epithelial and pulmonary vascular cell proliferation induced by cigarette smoke, and delaying natural luteal regression in bovine reproduction. This reagent is valuable for research focusing on vasospasm, abnormal cellular proliferation, and reproductive endocrine disorders. -
Macitentan Metabolite
ACT-373898 is the inactive carboxylic acid metabolite of Macitentan, a non-peptide dual antagonist of ETA and ETB endothelin receptors. This compound serves as a valuable reference for studies examining the pharmacokinetics and metabolic pathways of Macitentan. Its characterization is essential for understanding the therapeutic efficacy and safety profiles associated with endothelin receptor modulation in cardiovascular research. -
Endothelin Receptor Antagonist
TA-0201 is a competitive, non-peptide antagonist targeting endothelin receptors. It effectively inhibits the binding of [125I]ET-1 to cloned human ETA and ETB receptors, demonstrating Ki values of 15 pM and 41 nM, respectively. TA-0201 further reduces the pressor response induced by exogenous big ET-1, making it a valuable tool for studies aimed at understanding endothelin-mediated pathways and potential therapeutic interventions in cardiovascular research. -
Endothelin Receptor Antagonist
Edonentan is a potent endothelin receptor antagonist, specifically targeting the ETA receptor with an affinity (Ki) of 10 pM. This compound demonstrates metabolic stability and favorable pharmacokinetic properties in rat models. Edonentan effectively modulates the endothelin system by inhibiting the hypertensive response induced by big endothelin, making it a valuable tool for research in cardiovascular and renal disease studies. -
Endothelin Receptor Antagonist
PD 145065 is a highly potent non-selective endothelin receptor antagonist, demonstrating an IC50 value of 4 nM for the ETA receptor in rabbit renal artery vascular smooth muscle cells. This compound effectively inhibits endothelin signaling, making it useful for investigating the role of endothelin in cardiovascular biology and related disorders. PD 145065 is a valuable tool for researchers studying vascular physiology and potential therapeutic interventions targeting endothelial dysfunction. -
ETA Receptor Antagonist
SB234551 is a selective antagonist of the endothelin ETA receptor, inhibiting its activity to study its physiological effects. This compound has demonstrated potential in investigations related to stroke models, providing valuable insights into the role of endothelin in cerebrovascular events. Its selective targeting facilitates research into therapeutic strategies for conditions associated with altered endothelin signaling. -
ETB Receptor Agonist
Endothelin (16-21) functions as a selective agonist for the ETB receptor, exhibiting an EC50 of 228 nM in guinea-pig bronchus. This compound effectively induces smooth muscle contraction, making it a valuable tool for studying respiratory conditions such as asthma and cardiovascular diseases, including hypertension. Its targeted mechanism provides insights into ETB receptor signaling pathways relevant to these medical research applications. -
Vasoconstrictor
Big Endothelin-1 (22-38), human is a fragment of the human Big Endothelin-1 propeptide, specifically the 22-38 amino acid sequence. This peptide plays a crucial role in the regulation of vascular tone as it serves as a precursor to the potent vasoconstrictor Endothelin-1. It is utilized in research to study vascular physiology, hypertension, and related cardiovascular disorders, offering insights into the mechanisms of vasoconstriction and its effects on blood pressure regulation. -
Vasodilator
CH-141 is a peripheral vasodilator that acts to dilate blood vessels, thereby reducing vascular resistance. It is primarily employed in hypertension research to investigate mechanisms of blood pressure regulation and vascular function. This compound is instrumental in studying therapeutic strategies for cardiovascular diseases. -
ET Receptor Antagonist
A-127722 is a selective antagonist of the endothelin A (ETA) receptor, functioning through inhibition of endothelin signaling pathways. It exhibits a potent IC50 value of 0.36 nM, making it a valuable tool for research into cardiovascular diseases and conditions associated with endothelin dysregulation. This compound is particularly useful for studies investigating the role of endothelin in hypertension, heart failure, and pulmonary arterial hypertension. -
ETA/ETB Receptor Antagonist
L-749329 is a potent antagonist of the endothelin receptor subtypes ETA and ETB, exhibiting binding affinities (Kis) of 0.062 nM and 2.25 nM, respectively. This compound effectively inhibits endothelin-1 (ET-1)-stimulated signaling pathways, making it a valuable tool for studying the role of endothelin receptors in pathophysiological conditions. L-749329 is applicable in research focused on cardiovascular diseases, vascular biology, and related fields where endothelin signaling is implicated. -
Endothelin Receptor Antagonist
Atrasentan sodium is a selective endothelin receptor antagonist, exhibiting an IC50 of 0.0551 nM for the ETA receptor. This compound demonstrates significant biological activity by inhibiting endothelin-1-mediated vasoconstriction and fibrosis. Atrasentan sodium is primarily utilized in research applications related to cardiovascular diseases, pulmonary hypertension, and kidney injury, making it valuable for studies on endothelin signaling pathways and potential therapeutic interventions. -
ET Receptor Antagonist
Aselacin B is an endothelin-1 receptor antagonist that inhibits the binding of endothelin-1 to both ETA and ETB receptors. This compound plays a significant role in the investigation of cardiovascular diseases by modulating endothelin signaling pathways. Its application may provide insights into the pathophysiology of conditions such as hypertension and heart failure. -
ETA Receptor Antagonist
FR139317 is a selective antagonist of the endothelin A (ETA) receptor. This compound effectively inhibits cerebral activation induced by endothelin-1 in conscious rat models. Additionally, FR139317 demonstrates the capability to reduce cerebral vasospasm in canine subjects, highlighting its relevance in studies related to vascular regulation and cerebrovascular conditions. -
Endothelin Receptor Antagonist
WS009B is a selective endothelin receptor antagonist, exhibiting IC50 values of 0.67 μM for ET-1 and 0.8 μM for ET-2. This compound is useful for research into cardiovascular diseases, as it modulates the endothelin signaling pathway, which plays a critical role in vascular homeostasis and pathological conditions. WS009B's antagonistic properties make it a valuable tool for elucidating the mechanisms underlying endothelin-mediated physiological and pathological processes. -
ET(A)/ET(B) Antagonist
ATZ-1993 is a potent orally active nonpeptide antagonist of endothelin receptor subtype A and B, exhibiting pKi values of 8.69 and 7.20, respectively. This compound demonstrates significant potential in the study of intimal hyperplasia following balloon denudation of the carotid artery. ATZ-1993 can serve as a valuable tool in cardiovascular research, aiding in the exploration of vascular remodeling and related pathophysiological processes. -
Endothelin Receptor Antagonist
BMS 182874 hydrochloride is a highly selective antagonist of the endothelin ETA receptor, exhibiting an IC50 value of 0.150 μM and a Ki of 0.055 μM. This compound demonstrates efficacy in reducing arterial pressure in rat models of hypertension induced by deoxycorticosterone acetate. BMS 182874 hydrochloride is suitable for research applications focused on cardiovascular diseases and endothelin receptor modulation. -
Endothelin B Receptor Antagonist
IRL 1038 is a selective antagonist for the endothelin B receptor, with a binding affinity characterized by a Ki range of 6-11 nM. This compound effectively inhibits the actions of endothelin-1, crucial for studies investigating vascular function, cardiovascular diseases, and related physiological processes. Its application is valuable in elucidating the role of endothelin signaling in various pathophysiological conditions. -
ETA/ETB Receptor Antagonist
IRL-3630 is a selective antagonist of the ETA and ETB receptors, exhibiting binding affinities with Ki values of 1.9 nM and 1.2 nM, respectively. This compound is instrumental in studying the role of endothelin receptors in various physiological and pathological processes. Its applications include cardiovascular research, pulmonary hypertension studies, and investigations into renal function. -
ETA Receptor Antagonist
Clazosentan disodium is a selective endothelin A (ETA) receptor antagonist that effectively inhibits ET-1-mediated vasoconstriction. This compound is utilized in research focused on preventing cerebral vasospasm and related cerebral infarction. Its application may be significant in studies concerning vascular response and associated neurological conditions. -
ETA Antagonist
ETA Antagonist 2 is a selective antagonist of the endothelin A (ETA) receptor, which plays a critical role in vascular biology and pathophysiology. This compound effectively inhibits ETA receptor-mediated signaling pathways, resulting in vasodilation and reduced cellular proliferation. ETA Antagonist 2 is primarily utilized in research focused on cardiovascular diseases, pulmonary hypertension, and renal dysfunction to explore therapeutic avenues for endothelin-related disorders. -
Endothelin Receptor Antagonist
SB-209670 is a highly potent non-peptide antagonist of the endothelin (ET) receptor, exhibiting subnanomolar affinity with Ki values of 0.2 nM for ETA and 18 nM for ETB. This compound effectively inhibits the binding of 125I-labeled ET-1 to both human ET receptor subtypes, making it a valuable tool in cardiovascular and neurological research. SB-209670 demonstrates significant biological activity by reducing blood pressure in hypertensive models, offering neuroprotective effects against ischemia-induced neuronal degeneration, and inhibiting neointima formation following carotid artery balloon angioplasty in rats. -
ET Receptor Antagonist
Aselacin A is an endothelin-1 receptor (ET-1 receptor) antagonist that effectively inhibits the binding of endothelin-1 to both ETA and ETB receptors. Demonstrating IC50 values of 22 μg/mL and 20 μg/mL, it inhibits ET-1 binding to bovine atrial and porcine cerebral membranes, respectively. This compound is valuable for research into cardiovascular diseases and exploring the pathological roles of endothelin signaling in various cardiovascular conditions. -
ET Receptor Antagonist
WS009A is a potent antagonist of endothelin receptors, exhibiting IC50 values of 5.8 µM and 6.9 µM for the ET-1 and ET-2 receptors, respectively. This compound is valuable for investigating the role of endothelin signaling in cardiovascular diseases and potential therapeutic applications. Its effective inhibition of endothelin receptors makes WS009A a useful tool for researchers studying vascular dysfunction and related pathophysiological conditions. -
Drug Metabolite
Desmethyl Bosentan is an active metabolite of the endothelin receptor antagonist bosentan. It functions primarily by activating the pregnane X receptor (PXR), as demonstrated in CV-1 monkey kidney cells expressing the human receptor in a reporter assay at a concentration of 25 μM. This compound is valuable for studying drug metabolism and the regulatory pathways involved in pharmacokinetics and toxicology research. -
Endogenous Metabolite
Hydroxy bosentan is an endogenous metabolite derived from Bosentan, primarily processed by the cytochrome P450 system in the liver. This compound retains 10%-20% of Bosentan's pharmacological activity, serving as a significant contributor to the overall therapeutic effects of the parent compound. Hydroxy bosentan is useful in research focused on metabolic pathways and the pharmacokinetics of endothelin receptor antagonists. -
Stable Isotope
(Rac)-Ambrisentan-d5 is a deuterium-labeled form of (Rac)-Ambrisentan, functioning primarily as a selective endothelin receptor antagonist. Its key biological activity includes inhibition of endothelin-1, a peptide known to play a crucial role in vasoconstriction and blood pressure regulation. This stable isotope is particularly useful in pharmacokinetic studies, allowing for precise tracking of drug metabolism and distribution in biological systems. -
Endothelin Receptor Antagonist
Sulfisoxazole is an orally active endothelin receptor antagonist primarily targeting endothelin receptor A (IC50 = 0.60 μM) and endothelin receptor B (IC50 = 22 μM). This sulfonamide antibacterial agent boasts an oxazole substituent, enhancing its pharmacological profile. Sulfisoxazole is notably effective in inhibiting breast cancer exosome release through its action on endothelin receptor A, making it relevant for cancer research and studies focused on exosome biology.
