Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
Endothelin A Receptor Antagonist
JKC 301 is a selective Endothelin A receptor antagonist that effectively mitigates the pressor effects of nicotine in rat models. This compound is particularly valuable for investigating the cardiovascular diseases associated with smoking. Its targeted mechanism makes JKC 301 a useful tool for researchers studying the pathophysiological effects of nicotine on cardiovascular function. -
Precursor of Endothelin-1
Big Endothelin-1 (1-39), porcine is the precursor peptide of endothelin-1 (ET-1), a potent vasoconstrictor significantly involved in cardiovascular regulation. This reagent exhibits similar pressor effects in vivo, making it valuable for studies investigating vascular function and regulation. It is useful in research applications that aim to elucidate the roles of endothelin peptides in physiological and pathological processes. -
ETB Receptor Antagonist
BQ-788 is a selective endothelin B (ETB) receptor antagonist, exhibiting a potent IC50 of 1.2 nM against endothelin-1 (ET-1) binding in human Girardi heart cells. It demonstrates limited inhibitory activity on ETA receptors in the human neuroblastoma SK-N-MC cell line, with an IC50 of 1300 nM. This compound is primarily utilized in research on cardiovascular and neurobiological systems, aimed at elucidating the role of ETB receptors in various physiological and pathological conditions. -
Daul ETA/ETB Receptor Antagonist
J-104132 is a potent, orally active dual antagonist of the ETA and ETB receptors, exhibiting a Ki of 0.034 nM for ETA and 0.104 nM for ETB receptors. It effectively inhibits Endothelin-1 (ET-1)-induced signaling and vascular contractions in vitro. In vivo studies demonstrate that J-104132 mitigates hypertension, vascular remodeling, and diabetic endothelial dysfunction through dual blockade of ETA and ETB receptors, making it valuable for research into diabetic vascular complications. -
Endothelin-A Receptor Antagonist
SB 247083 is a selective and competitive antagonist of the endothelin-A receptor, exhibiting a Ki value of 0.41 nM. It displays a significantly lower affinity for the endothelin-B receptor with a Ki of 467 nM. SB 247083 effectively inhibits ET-1-induced contractions in rat aorta, with a Kb of 3.5 nM. This reagent is valuable for research focusing on cardiovascular diseases and their underlying mechanisms. -
ETA Receptor Antagonist
Clazosentan is a selective endothelin A (ETA) receptor antagonist. It effectively inhibits ET-1-mediated vasoconstriction, making it a valuable tool in research focused on cardiovascular function and cerebral health. Clazosentan is primarily utilized in studies investigating the prevention of cerebral vasospasm and associated complications, including cerebral infarction. -
Endothelin Receptor Agonist
Sarafotoxin S6a is an endothelin receptor agonist that selectively targets ETA and ETB receptors, exhibiting a profile comparable to Endothelin-3. This compound is known to effectively stimulate vasoconstriction in pig coronary arteries, with an EC50 value of 7.5 nM, making it a valuable tool for studying cardiovascular physiology and pathophysiology. Its targeted interactions facilitate research in vascular biology and related therapeutic areas. -
Endothelin Receptor Antagonist
BMS 182874 is a selective endothelin receptor type A (ETA) antagonist, demonstrating an IC50 value of 0.150 μM and a Ki of 0.055 μM. This compound effectively reduces arterial pressure in models of deoxycorticosterone acetate-induced hypertension in rats, making it a valuable tool for cardiovascular disease research. BMS 182874's targeted action on the endothelin receptor provides insights into vascular function and potential therapeutic approaches for hypertension. -
ETB Receptor Antagonist
Ro 46-8443 is a selective antagonist of the endothelin ETB receptor, exhibiting at least 100-fold selectivity for ETB over ETA receptors (IC50: 34-69 nM vs. 6800 nM). Its specificity allows for targeted investigations into ETB receptor-related biological mechanisms. This compound is valuable for research applications focused on cardiovascular effects, cell proliferation, and pathophysiological conditions related to endothelin signaling. -
Endothelin-B Receptor Agonist
Sarafotoxin S6c is a potent agonist of the endothelin-B receptor. This compound induces vasoconstriction in both endothelium-intact and endothelium-denuded vascular tissues, making it a valuable tool for studying endothelial function and vascular tone regulation. Its application in research aids in elucidating the role of endothelin pathways in cardiovascular physiology and pathology. -
ET(A) Receptor Antagonist
Nebentan is a selective, orally active non-peptide antagonist of the endothelin ETA receptor. It demonstrates significant inhibitory activity against [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptors, with Ki values of 0.697 nM and 569 nM, respectively. Research indicates that Nebentan may effectively mitigate the progression of cor pulmonale and myocardial infarction in vivo, making it a valuable tool for studies related to cardiovascular and pulmonary diseases. -
ET Receptor Antagonist
Enrasentan is an endothelin (ET) receptor antagonist with notable antihypertensive effects. It primarily functions by blocking the action of endothelin, a potent vasoconstrictor, thereby promoting vasodilation and lowering blood pressure. This compound is utilized in cardiovascular research to investigate mechanisms of hypertension and potential therapeutic interventions. -
ET(A) Receptor Antagonist
Nebentan potassium (YM598) is a selective, orally active non-peptide antagonist of the endothelin ETA receptor. It demonstrates significant inhibition of [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptors, with Kis of 0.697 nM and 569 nM, respectively. This compound has shown potential in ameliorating the progression of cor pulmonale and myocardial infarction in vivo, making it valuable for cardiovascular research applications. -
ETA Inhibitor
Diosuxentan is a selective inhibitor of the endothelin A (ETA) receptor. It demonstrates significant biological activity in suppressing vascular responses associated with endothelin-1, making it relevant for studies investigating cardiovascular, renal, and neuroinflammatory conditions. Diosuxentan provides valuable insights for research focused on the therapeutic modulation of ETA-mediated pathways. -
Endothelin-A Receptor Antagonist
PD-156707 is a selective endothelin-A receptor antagonist that exhibits potent oral activity. This compound binds to human ET-A and ET-B receptors with Ki values of 0.17 nM and 133.8 nM, respectively. PD-156707 has demonstrated efficacy in reversing established chronic hypoxic pulmonary hypertension in rat models. It is suitable for research on diseases related to aberrant endothelin-A receptor activation, with potential applications in pulmonary hypertension, stroke, and heart failure studies. -
ETA Receptor Antagonist
ABT-546 is a potent and highly selective endothelin ETA receptor antagonist, exhibiting a binding affinity (Ki) of 0.46 nM for [125I]endothelin-1 in cloned human ETA receptors. With over 25,000-fold selectivity for the ETA receptor compared to the ETB receptor, ABT-546 effectively inhibits endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis, displaying IC50 values of 0.59 nM and 3 nM, respectively. This compound serves valuable applications in cardiovascular and neurobiological research, particularly in studies investigating endothelin-mediated pathways. -
ETAR Antagonist
Ambrisentan sodium is a selective antagonist of the endothelin type A receptor (ETAR). This compound demonstrates potent inhibition of ETAR, making it valuable for investigating the role of endothelin signaling in various physiological processes and pathological conditions. It is primarily used in research related to cardiovascular diseases and pulmonary hypertension. -
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. -
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.
