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ETA/ETB receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (7) Bacterial (1) COX (1) Drug Metabolite (1) Endogenous Metabolite (1) Endothelin Receptor (44) Fluorescent Dye (1) Interleukin Related (1) Isotope-Labeled Compounds (2) MMP (1) NF-κB (1) Prostaglandin Receptor (1) Reference Standards (7) TGF-β Receptor (4) TNF Receptor (1)
By Research Areas:	Cancer (14) Cardiovascular Disease (40) Endocrinology (17) Infection (1) Inflammation/Immunology (5) Metabolic Disease (8) Neurological Disease (4)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-P0202

Endothelin 1 (swine, human) 5+ Cited Publications ET-1 (swine, human)	Endothelin Receptor	Metabolic Disease Inflammation/Immunology
Endothelin 1 (swine, human) (ET-1) is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. Endothelin 1 acts through two types of receptors ET_A and ET_B .

HY-A0013

Bosentan Maximum Cited Publications 30 Publications Verification	Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ET_A and ET_B receptors with K_i of 4.7 nM and 95 nM in human SMC, respectively.

HY-14184

Macitentan 10+ Cited Publications ACT-064992	Endothelin Receptor Apoptosis	Cardiovascular Disease Endocrinology Cancer
Macitentan (ACT-064992) is an orally active, non-peptide dual *ETA* and *ETB* (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .

HY-11103

Sitaxsentan sodium 2 Publications Verification IPI 1040 sodium; TBC11251 sodium	Endothelin Receptor TGF-β Receptor	Cardiovascular Disease Metabolic Disease
Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC₅₀ of 1.4 nM and a K_i of 0.43 nM. Sitaxsentan sodium exhibits an IC₅₀ for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan sodium can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .

HY-10088

Zibotentan 1 Publications Verification ZD4054	Endothelin Receptor Apoptosis	Endocrinology Cancer
Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ET_A) receptor antagonist with a K_i of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research .

HY-15894A

BQ-788 10+ Cited Publications	Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
BQ-788 is a potent, selective **ETB receptor antagonist with IC₅₀** of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC₅₀ of 1300 nM .

HY-A0013A

Bosentan hydrate Maximum Cited Publications 30 Publications Verification	Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
Bosentan hydrate is a competitive and dual antagonist of endothelin-1 (ET) for the ET_A and ET_B receptors with K_i of 4.7 nM and 95 nM in human SMC, respectively.

HY-17351

Tezosentan RO 610612	Endothelin Receptor	Cardiovascular Disease Neurological Disease Endocrinology Cancer
Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA₂s of 9.5, 7.7 for ET_A and ET_B receptors, respectively.

HY-103460

IRL 2500	Endothelin Receptor	Cardiovascular Disease
IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC₅₀ values of 1.3 and 94 nM for ET_B and ET_A receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo .

HY-15195

Avosentan Ro 67-0565; SPP-301	Endothelin Receptor	Cardiovascular Disease Endocrinology
Avosentan (Ro 67-0565; SPP-301) is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks *ETB* receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure .

HY-120295

A-192621 2 Publications Verification	Endothelin Receptor Apoptosis	Cardiovascular Disease Endocrinology
A-192621, a chemical probe, is a potent, nonpeptide, orally active and selective endothelin B (ET_B) receptor antagonist with an IC₅₀ of 4.5 nM and a K_i of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ET_A (IC₅₀ of 4280 nM and K_i of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level .

HY-15404

Darusentan Lu-135252	Endothelin Receptor	Cardiovascular Disease Endocrinology
Darusentan (Lu-135252) is a selective *endothelin receptor* A** (ET-A) *receptor* antagonist, which binds with a K_i of 1.4 nM to the ET-A receptor and a K_i of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors . Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a K_i of 13 nM .

HY-19431

Ro 46-8443	Endothelin Receptor	Cardiovascular Disease
Ro 46-8443 is the first non-peptide endothelin *ET_B* receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ET_B (IC₅₀: 34-69 nM) over ET_A receptors (IC₅₀: 6800 nM) .

HY-P0202A

Endothelin 1 (swine, human) TFA 5+ Cited Publications ET-1 (swine, human) TFA	Endothelin Receptor	Cardiovascular Disease
Endothelin 1 (swine, human) (ET-1) TFA is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. Endothelin 1 TFA acts through two types of receptors ET_A and ET_B .

HY-14184S

Macitentan-d4 ACT-064992-d₄	Isotope-Labeled Compounds Endothelin Receptor Apoptosis	Cardiovascular Disease
Macitentan-d₄ is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .

HY-14184R

Macitentan (Standard) ACT-064992 (Standard)	Reference Standards Endothelin Receptor Apoptosis	Cardiovascular Disease Endocrinology Cancer
Macitentan (Standard) is the analytical standard of Macitentan. This product is intended for research and analytical applications. Macitentan (ACT-064992) is an orally active, non-peptide dual *ETA* and *ETB* (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .

HY-P1112

Sarafotoxin S6a	Endothelin Receptor	Cardiovascular Disease Neurological Disease
Sarafotoxin S6a, a sarafotoxin analogue, is a endothelin receptor agonist and has an *ET_A/ET_B* selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a elicits the pig coronary artery with an EC₅₀ value of 7.5 nM .

HY-P2496

Endothelin 1 (swine, human), Alexa Fluor 488-labeled	Endothelin Receptor Fluorescent Dye NF-κB COX Prostaglandin Receptor Apoptosis TNF Receptor Interleukin Related MMP	Cardiovascular Disease Inflammation/Immunology Cancer
Endothelin 1 (swine, human), Alexa Fluor 488-labeled is an Endothelin-1 conjugated with Alexa Fluor 488 (HY-D1304). Endothelin-1 is an endogenous vasoconstrictor and agonist of *ETA/ETB* *receptor. Endothelin 1 (swine, human) exerts effects including promoting mitosis, angiogenesis, tumor invasion and metastasis, and inhibiting apoptosis. Endothelin 1 (swine, human) induces inflammation and oxidative stress by activating the NF-κB* pathway. Endothelin 1 (swine, human), Alexa Fluor 488-labeled is specifically designed for fluorescence imaging, flow cytometry or receptor localization studies, and can be used in research related to sepsis, atherosclerosis, systemic inflammatory response syndrome, cancer and congestive heart failure .

HY-76520

Sitaxsentan IPI 1040; TBC-11251	Endothelin Receptor TGF-β Receptor	Cardiovascular Disease Metabolic Disease
Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC₅₀ of 1.4 nM and a K_i of 0.43 nM. Sitaxsentan exhibits an IC₅₀ for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .

HY-106994A

Nebentan potassium YM598	Endothelin Receptor	Cardiovascular Disease Inflammation/Immunology Cancer
Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ET_A receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium inhibits [ ¹²⁵I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with K_i of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .

HY-123744

PD-156707	Endothelin Receptor	Cardiovascular Disease Neurological Disease
PD-156707 is an orally active, nonpeptide and selective Endothelin-A receptor antagonist. PD-156707 binds to human *ET-A* and *ET-B* receptors with K_i values of 0.17 nM and 133.8 nM, respectively. PD-156707 shows reversal of established chronic hypoxic pulmonary hypertension in rats. PD-156707 can be used for the study of diseases associated with abnormal *ET-A* receptor activation, particularly pulmonary hypertension, stroke, and heart failure .

HY-19263

BMS-193884	Endothelin Receptor	Cardiovascular Disease
BMS-193884 is a selective, orally active, and competitive *ET_A* antagonist with 10000-fold greater affinity for the human ET_A receptor (K_i=1.4 nM) than for the ET_B receptor .

HY-10383

J-104132	Endothelin Receptor	Cardiovascular Disease Metabolic Disease
J-104132 (L-753037) is a potent, orally active, selective and competitive **ETA/ETB receptor antagonist with K_i** of 0.034 nM for ETA and 0.104 nM for ETB receptors. J-104132 inhibits Endothelin-1 (ET-1) (HY-P71446)-induced signaling and vascular contractions in vitro. J-104132 alleviates hypertension, vascular remodeling, and diabetic endothelial dysfunction in vivo by dual ETA/ETB blockade. J-104132 can be used for research on diabetic vascular complications ^[1][3].

HY-135500

ACT-373898	Endothelin Receptor	Endocrinology
ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist .

HY-115417

Bosentan-d4	Endothelin Receptor	Cardiovascular Disease Endocrinology
Bosentan-d4 is the deuterium labeled Bosentan. Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ET_A and ET_B receptors with K_i of 4.7 nM and 95 nM in human SMC, respectively.

HY-135283

ABT-546 A-216546	Endothelin Receptor	Cardiovascular Disease Endocrinology
ABT-546 (A-216546), a chemical probe, is a potent, highly selective and active endothelin ET_A receptor antagonist with a K_i of 0.46 nM for [ ¹²⁵I]endothelin-1 binding to cloned human endothelin ET_A. ABT-546 is >25,000-fold more selective for the **ET_A receptor** than for the ET_B receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC₅₀ of 0.59 nM and 3 nM, respectively .

HY-14184A

Macitentan n-butyl analogue	Endothelin Receptor	Cardiovascular Disease Endocrinology
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).

HY-124234

TA-0201	Endothelin Receptor	Cardiovascular Disease
TA-0201 is a novel orally active, competitive, non-peptide endothelin receptor antagonist. TA-0201 antagonizes the specific binding of [ ¹²⁵I]ET-1 to cloned human receptors of ET_A and ET_B with K_i values of 15 pM and 41 nM, respectively. TA-0201 inhibits the pressor response to the exogenous big ET-1 .

HY-19210

SB-209670	Endothelin Receptor	Cardiovascular Disease
SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (K_i=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .

HY-117644

L-749329 (Rac)-L-754142	Endothelin Receptor	Cardiovascular Disease
L-749329 ((Rac)-L-754142) is an *ET_A* and *ET_B* receptor antagonist, with K_is of 0.062 nM and 2.25 nM for ET_A and ET_B respectively. L-749329 inhibits ET-1-stimulated signaling .

HY-P10151

PD 156252	Endothelin Receptor	Cardiovascular Disease
PD 156252 is a hexapeptide that is a highly potent endothelin (ET) antagonist. PD 156252 has enhanced binding affinity for rabbit ETA and rat ETB receptor subtypes with IC50 values of 1.0 and 40 nM, respectively.

HY-A0013AR

Bosentan hydrate (Standard)	Reference Standards Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
Bosentan (hydrate) (Standard) is the analytical standard of Bosentan (hydrate). This product is intended for research and analytical applications. Bosentan hydrate is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.

HY-106994

Nebentan YM598 free base	Endothelin Receptor	Cardiovascular Disease Inflammation/Immunology Cancer
Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ET_A receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan inhibits [ ¹²⁵I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with K_i of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .

HY-15195R

Avosentan (Standard) Ro 67-0565 (Standard); SPP-301 (Standard)	Reference Standards Endothelin Receptor	Cardiovascular Disease Endocrinology
Avosentan (Standard) is the analytical standard of Avosentan (HY-15195). This product is intended for research and analytical applications. Avosentan is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction, and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks *ETB* receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure.

HY-N5170

Aselacin A	Endothelin Receptor	Cardiovascular Disease
Aselacin A targets endothelin-1 receptor (ET-1 receptor), inhibits the the binding of ET-1 to **ETA receptor and ETB receptor. Aselacin A inhibits the ET-1 binding to bovine atrial membrane and porcine cerebral membrane with IC₅₀** of 22 μg/mL and 20 μg/mL. Aselacin A can be used for research of cardiovascular diseases .

HY-P1112A

Sarafotoxin S6a TFA	Endothelin Receptor	Cardiovascular Disease Neurological Disease
Sarafotoxin S6a TFA , a sarafotoxin analogue, is a endothelin receptor agonist and has an *ET_A/ET_B* selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a TFA elicits the pig coronary artery with an EC₅₀ value of 7.5 nM .

HY-10088R

Zibotentan (Standard) ZD4054 (Standard)	Reference Standards Endothelin Receptor Apoptosis	Endocrinology Cancer
Zibotentan (Standard) is the analytical standard of Zibotentan. This product is intended for research and analytical applications. Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research .

HY-135390

Hydroxy desmethyl Bosentan Ro 64-1056	Drug Metabolite	Cardiovascular Disease
Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver . Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ET_A and ET_B receptors with K_i of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension .

HY-W781265

BE 24566B L-755,805	Endothelin Receptor Bacterial	Infection
BE 24566B is a polyketide fungal metabolite originally isolated from S. violaceusniger. It is active against B. subtilis, B. cereus, S. aureus, M. luteus, E. faecalis, and S. thermophilus (MICs=1.56, 1.56, 1.56, 1.56, 3.13, and 3.13 μg/mL, respectively). BE 24566B is an endothelin (ET) receptor antagonist (IC₅₀s=11 and 3.9 μM for ETA and ETB receptors, respectively).

HY-11103R

Sitaxsentan sodium (Standard) IPI 1040 sodium (Standard); TBC11251 sodium (Standard)	Endothelin Receptor Reference Standards TGF-β Receptor	Cardiovascular Disease Metabolic Disease
Sitaxsentan (sodium) (Standard) is the analytical standard of Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) (HY-11103). This product is intended for research and analytical applications. Sitaxsentan sodium is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC₅₀ of 1.4 nM and a K_i of 0.43 nM. Sitaxsentan sodium exhibits an IC₅₀ for the ETB receptor of as high as 9800 nM. Sitaxsentan sodium is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan sodium can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .

HY-76520S

Sitaxsentan-13C6 IPI 1040-¹³C₆ ; TBC-11251-¹³C₆	Isotope-Labeled Compounds Endothelin Receptor TGF-β Receptor	Cardiovascular Disease Metabolic Disease
Sitaxsentan- ¹³C₆ (IPI 1040- ¹³C₆) is ¹³C labeled Sitaxsentan (HY-76520). Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC₅₀ of 1.4 nM and a K_i of 0.43 nM. Sitaxsentan exhibits an IC₅₀ for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .

HY-182561

Cgs 27830	Endothelin Receptor	Cardiovascular Disease
Cgs 27830 is an endothelin receptor antagonist with 20-fold higher selectivity for *ET-A* receptors over *ET-B* receptors. Cgs 27830 blocks activity of *ET-A* and *ET-B* receptors. Cgs 27830 does not alter basal vascular tone in the ovine fetal pulmonary circulation. Cgs 27830 prevents big-endothelin-1-induced pulmonary vasoconstriction in late gestation fetal lambs .

HY-78096

O-Deshydroxyethyl bosentan	Endogenous Metabolite	Metabolic Disease
O-Deshydroxyethyl bosentan is a metabolite of Bosentan (HY-A0013), which is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors .

HY-103460R

IRL 2500 (Standard)	Reference Standards Endothelin Receptor	Cardiovascular Disease
IRL 2500 (Standard) is the analytical standard of IRL 2500 (HY-103460). This product is intended for research and analytical applications. IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC₅₀ values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo .

HY-183141

HJP 272	Endothelin Receptor	Cardiovascular Disease Metabolic Disease Cancer
HJP 272 is a selective endothelin peptide A (ET_A) receptor antagonist with an IC₅₀ of 37.01 nM. . HJP 272 can be used for the researches of pulmonary arterial hypertension, fibrosis, renal failure and cancer .

HY-106994AR

Nebentan potassium (Standard) YM598 (Standard)	Reference Standards Endothelin Receptor	Cardiovascular Disease Inflammation/Immunology Cancer
Nebentan potassium (Standard) (GT-2331 maleate (Standard)) is the analytical standard of Nebentan (potassium) (HY-106994A). This product is intended for research and analytical applications. Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium inhibits [125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with K_i of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .

Cat. No.	Product Name	Target	Research Area

HY-P0202

Endothelin 1 (swine, human) 5+ Cited Publications ET-1 (swine, human)	Endothelin Receptor	Metabolic Disease Inflammation/Immunology
Endothelin 1 (swine, human) (ET-1) is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. Endothelin 1 acts through two types of receptors ET_A and ET_B .

HY-P0202A

Endothelin 1 (swine, human) TFA 5+ Cited Publications ET-1 (swine, human) TFA	Endothelin Receptor	Cardiovascular Disease
Endothelin 1 (swine, human) (ET-1) TFA is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. Endothelin 1 TFA acts through two types of receptors ET_A and ET_B .

HY-P1112

Sarafotoxin S6a	Endothelin Receptor	Cardiovascular Disease Neurological Disease
Sarafotoxin S6a, a sarafotoxin analogue, is a endothelin receptor agonist and has an *ET_A/ET_B* selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a elicits the pig coronary artery with an EC₅₀ value of 7.5 nM .

HY-P2496

Endothelin 1 (swine, human), Alexa Fluor 488-labeled	Endothelin Receptor Fluorescent Dye NF-κB COX Prostaglandin Receptor Apoptosis TNF Receptor Interleukin Related MMP	Cardiovascular Disease Inflammation/Immunology Cancer
Endothelin 1 (swine, human), Alexa Fluor 488-labeled is an Endothelin-1 conjugated with Alexa Fluor 488 (HY-D1304). Endothelin-1 is an endogenous vasoconstrictor and agonist of *ETA/ETB* *receptor. Endothelin 1 (swine, human) exerts effects including promoting mitosis, angiogenesis, tumor invasion and metastasis, and inhibiting apoptosis. Endothelin 1 (swine, human) induces inflammation and oxidative stress by activating the NF-κB* pathway. Endothelin 1 (swine, human), Alexa Fluor 488-labeled is specifically designed for fluorescence imaging, flow cytometry or receptor localization studies, and can be used in research related to sepsis, atherosclerosis, systemic inflammatory response syndrome, cancer and congestive heart failure .

HY-P10151

PD 156252	Endothelin Receptor	Cardiovascular Disease
PD 156252 is a hexapeptide that is a highly potent endothelin (ET) antagonist. PD 156252 has enhanced binding affinity for rabbit ETA and rat ETB receptor subtypes with IC50 values of 1.0 and 40 nM, respectively.

HY-P1112A

Sarafotoxin S6a TFA	Endothelin Receptor	Cardiovascular Disease Neurological Disease
Sarafotoxin S6a TFA , a sarafotoxin analogue, is a endothelin receptor agonist and has an *ET_A/ET_B* selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a TFA elicits the pig coronary artery with an EC₅₀ value of 7.5 nM .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N5170

Aselacin A	Natural Products Microorganisms Source Classification	Endothelin Receptor
Aselacin A targets endothelin-1 receptor (ET-1 receptor), inhibits the the binding of ET-1 to **ETA receptor and ETB receptor. Aselacin A inhibits the ET-1 binding to bovine atrial membrane and porcine cerebral membrane with IC₅₀** of 22 μg/mL and 20 μg/mL. Aselacin A can be used for research of cardiovascular diseases .

Cat. No.	Product Name	Chemical Structure

HY-14184S

Macitentan-d4
Macitentan-d₄ is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .

HY-76520S

Sitaxsentan-13C6

Sitaxsentan- ¹³C₆ (IPI 1040- ¹³C₆) is ¹³C labeled Sitaxsentan (HY-76520). Sitaxsentan (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally active endothelin A receptor (ETA) antagonist with an IC₅₀ of 1.4 nM and a K_i of 0.43 nM. Sitaxsentan exhibits an IC₅₀ for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .

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