Catalog No.
Product Name
Application
Product Information
Citations
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EndothelinA receptor antagonist
Ambrisentan functions as an endothelin receptor antagonist, and is selective for the type A endothelin receptor (ETA).- Naoki Dohi, .et al. , PLoS One, 2021, 16(8): e0255656 PMID: 34343209
- Tony Ngo, .et al. , Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
- Toshiaki Okamoto, .et al. , World J Hepatol, 2016, Aug 8; 8(22): 933-941 PMID: 27574547
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ETA-receptor Antagonist
Zibotentan (ZD4054)is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).- Tony Ngo, .et al. , Nat Chem Biol, 2017, Feb; 13(2): 235-242 PMID: 27992882
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endothelin receptor modulator
Endothelin Mordulator 1 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders. -
Endothelin antagonist
Avosentan (SPP301) is a potent and highly selective ETA receptor blocker. -
Endothelin receptor antagonist
Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). -
ETA receptor antagonist
Sitaxentan sodium (TBC-11251) is a selective endothelin receptor-A antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively. -
ETA receptor antagonist
Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist. Antihypertensive. Sitaxsentan is used in treatment of chronic heart failure. -
ETA antagonist
Atrasentan is an experimental drug that is being studied for the treatment of various types of cancer, including non-small cell lung cancer. It is an endothelin receptor antagonist selective for subtype A (ETA). -
ETBR antagonist
BQ-788 sodium salt is a selective ETBR (Endothelin receptor B ) antagonist. - Aminaftone, a derivative of 4-aminobenzoic acid, downregulates endothelin-1 (ET-1) production in vitro by interfering with the transcription of the pre-pro-ET-1 gene.
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angiotensin II and endothelin A receptor antagonist
Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively. -
endothelin (ET) receptor antagonist
Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively. -
endothelin A (ETA) receptor antagonist
Darusentan is a selective endothelin A (ETA) receptor antagonist. -
ETA antagonist
ETA antagonist 1 is a ETA selective antagonist with an IC50 of 0.08 μM. - Endothelin-2, human, endogenous peptide found predominately in the kidney and intestine. Displays similar selectivity for ETA and ETB endothelin receptors.
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ET-A and ET-B antagonist
Bosentan is an endothelin (ET) receptor antagonist for ET-A and ET-B with Ki of 4.7 nM and 95 nM, respectively. -
Endothelin antagonist receptor
Atrasentan hydrochloride is an endothelin antagonist receptor (IC50=0.0551 nM, ETA) being developed for the treatment of prostate cancer. -
Vasoconstrictor
Endothelin-1 (1-31) (Human) is a potent vasoconstrictor that primarily targets endothelin receptors to induce vascular smooth muscle contraction. This peptide plays a significant role in regulating blood pressure and is involved in various cardiovascular pathologies. It is widely utilized in research applications focused on cardiovascular physiology, hypertension, and related therapeutic interventions. -
endothelin ETA and ETB receptor antagonist
Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). -
dual ETA/ETB antagonist
Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. -
Endothelin Receptor Inhibitor
Carperitide is a synthetic analogue of Atrial Natriuretic Peptide (ANP) that acts as an endothelin receptor inhibitor. This 28-amino acid peptide significantly reduces endothelin-1 secretion in a dose-dependent manner, thereby promoting vasodilation and natriuresis. It is primarily used in research applications related to cardiovascular physiology, providing insights into heart failure mechanisms and the regulation of blood pressure. -
ETA/ETB Antagonist
Macitentan-d4 is a deuterated analog of the dual ETA and ETB endothelin receptor antagonist, Macitentan. This compound exhibits significant biological activity by blocking the effects of endothelin-1, which is implicated in conditions such as pulmonary arterial hypertension (PAH) and idiopathic pulmonary fibrosis (IPF). Macitentan-d4 serves as a valuable tool for research into the underlying mechanisms of endothelin signaling and its role in cardiovascular and pulmonary disorders. -
Endothelin Receptor Antagonist
Sulfisoxazole diethanolamine is an endothelin receptor antagonist, exhibiting IC50 values of 0.60 μM and 22 μM for endothelin receptor A and endothelin receptor B, respectively. This sulfonamide antibacterial compound, characterized by its oxazole substituent, demonstrates significant inhibition of breast cancer exosome release through the selective targeting of endothelin receptor A. Its mechanism of action holds potential for applications in cancer research and related therapeutic studies. -
Antibiotic
Kendomycin ((−)-TAN 2162) is a polyketide antibiotic primarily targeting bacterial growth inhibition. It exhibits significant antibacterial activity, particularly against methicillin-resistant Staphylococcus aureus (MRSA) with a minimum inhibitory concentration (MIC) of 5 μg/mL. In addition to its antibacterial properties, Kendomycin acts as a potent antagonist of the endothelin receptor and a calcitonin receptor agonist, highlighting its potential applications in anti-osteoporotic research. -
HIV Inhibitor
Schisantherin D is a dibenzocyclooctadiene lignan that exhibits significant anti-HIV activity with an EC50 of 0.5 μg/mL. This compound selectively inhibits endothelin receptor B (ETBR) and demonstrates hepatoprotective properties. Schisantherin D is valuable for research applications focused on HIV replication and the exploration of liver protective mechanisms. -
Fungal Metabolite
BE 24566B is a polyketide fungal metabolite that acts as an endothelin receptor antagonist, targeting both ETA and ETB receptors with IC50 values of 11 μM and 3.9 μM, respectively. This compound demonstrates antibacterial activity against a range of Gram-positive bacteria, including B. subtilis, B. cereus, S. aureus, M. luteus, E. faecalis, and S. thermophilus, with reported MICs of 1.56 μg/mL for five of these species and 3.13 μg/mL for E. faecalis and S. thermophilus. BE 24566B is valuable for research applications in antimicrobial studies and receptor pharmacology. -
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. -
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.
