Catalog No.
Product Name
Application
Product Information
Citations
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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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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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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. -
endothelin receptor modulator
Endothelin Mordulator 1 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders. -
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. - 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. -
ETA antagonist
ETA antagonist 1 is a ETA selective antagonist with an IC50 of 0.08 μM. - 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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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.
