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endothelin receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Endothelin Receptor (76) Angiotensin Receptor (3) Antibiotic (4) Apoptosis (6) Bacterial (5) CGRP Receptor (1) Cytochrome P450 (2) Drug Metabolite (2) Endogenous Metabolite (1) Isotope-Labeled Compounds (3) Radionuclide-Drug Conjugates (RDCs) (1) Reference Standards (9) TGF-β Receptor (4) Vasopressin Receptor (1)
By Research Areas:	Cancer (19) Cardiovascular Disease (67) Endocrinology (26) Infection (5) Inflammation/Immunology (3) Metabolic Disease (11) Neurological Disease (4)

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Endothelin Receptor Endothelin-Converting Enzyme (ECE)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-17621

Sparsentan RE-021; DARA-a	Angiotensin Receptor Endothelin Receptor	Cardiovascular Disease Endocrinology
Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with K_is of 0.8 and 9.3 nM, respectively .

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-12378

BQ-123 3 Publications Verification	Endothelin Receptor	Cardiovascular Disease
BQ-123 is a potent and selective **endothelin A (ETA) receptor** antagonist with an IC₅₀ of 7.3 nM and a K_i of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .

HY-15403

Atrasentan 5+ Cited Publications ABT-627; (+)-A 127722; A-147627	Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
Atrasentan (ABT-627) is an **endothelin receptor** antagonist with IC₅₀ of 0.0551 nM for ET_A .

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-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-B0323

Sulfisoxazole 5 Publications Verification Sulfafurazole	Endothelin Receptor Bacterial Antibiotic	Infection Endocrinology Cancer
Sulfisoxazole (Sulfafurazole) is an orally active **endothelin receptor** antagonist with IC₅₀ values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole is a sulfonamide antibacterial agent with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A .

HY-15403A

Atrasentan hydrochloride 5+ Cited Publications ABT-627 hydrochloride; (+)-A 127722 hydrochloride; A-147627 hydrochloride	Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
Atrasentan hydrochloride (ABT-627 hydrochloride) is a selective **endothelin A receptor** antagonist with an IC₅₀ of 0.0551 nM for ET_A .

HY-17352

Clazosentan Ro 61-1790; VML 588; AXV-034343	Endothelin Receptor	Cardiovascular Disease
Clazosentan (Ro 61-1790) is a selective **endothelin A (ET_A) receptor** antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction .

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-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-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-P990089

Patecibart Getagozumab; GMA-301	Endothelin Receptor	Cardiovascular Disease
Patecibart is a humanized immunoglobulin G4-kappa, anti-EDNRA monoclonal antibody. Patecibart is an **endothelin receptor** antagonist .

HY-19529

Ro 46-2005	Endothelin Receptor	Cardiovascular Disease Endocrinology
Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.

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-121300

Kendomycin (-)-TAN2162	Antibiotic Bacterial Endothelin Receptor CGRP Receptor	Infection Cancer
Kendomycin ((−)-TAN 2162) is a polyketide antibiotic with remarkable antibacterial and cancer cells cytotoxic activities. Kendomycin tends to be bacteriostatic rather than bactericidal and inhibits the growth of the methicillin-resistant Staphylococcus aureus (MRSA) strain COL at a low concentration (MIC of 5 μg/mL). Kendomycin is a potent antagonist of the **endothelin receptor** and a calcitonin receptor agonist which plays its role as an anti-osteoporotic agent .

HY-119667

Enrasentan SB 217242	Endothelin Receptor	Cardiovascular Disease
Enrasentan (SB 217242) is an **endothelin (ET) receptor** antagonist. Enrasentan has antihypertensive effects .

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-105408A

Fandosentan potassium	Endothelin Receptor Cytochrome P450	Cardiovascular Disease
Fandosentan potassium is a potent endothelin A receptor (ET_AR) antagonist. Fandosentan potassium inhibits CYP2C9 and CYP3A4 activities with IC₅₀ values of 39.6 and 21.6 μM, respectively. Fandosentan potassium reverses the hypoxic pulmonary vasoconstriction in the perinatal lamb. Fandosentan potassium can be used for pulmonary hypertension research ^[1][2].

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-105183

PD 145065	Endothelin Receptor	Others
PD 145065 is a highly potent but non-selective endothelin receptor antagonist with an IC₅₀ value of 4 nM for the ET_A receptor for rabbit renal artery vascular smooth muscle cells .

HY-118497

BMS 182874	Endothelin Receptor	Cardiovascular Disease Metabolic Disease
BMS 182874 is an orallyactive, highly selective **endothelin receptor (ET_A** receptor) antagonist, with IC₅₀ value of 0.150 μM, K_i of 0.055 μM. BMS 182874 reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research .

HY-105168

TAK 044	Endothelin Receptor	Cardiovascular Disease
TAK 044 is an antagonist of **Endothelin Receptor**. TAK 044 strongly inhibits ET-induced deterioration in various animal models. TAK 044 can be used in study ET-related diseases such as acute myocardial infarction,acute renal failure, acute hepatic malfunction, and subarachnoid hemorrhage .

HY-B0323A

Sulfisoxazole diethanolamine Sulfafurazole diethanolamine	Endothelin Receptor Antibiotic Bacterial	Infection Endocrinology Cancer
Sulfisoxazole (Sulfafurazole) diethanolamine is an **endothelin receptor** antagonist with IC₅₀ values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole diethanolamine is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole diethanolamine inhibits breast cancer exosome release by targeting endothelin receptor A .

HY-15402

Edonentan BMS 207940	Endothelin Receptor	Cardiovascular Disease
Edonentan (BMS 207940) is an antagonist for endothelin receptor (ET_A receptor), with a K_i of 10 pM. Edonentan is metabolic stable, exhibits good pharmakokinetic characters in rats. Edonentan regulates the endothelin system, blocks the big Endothelin-induced pressor response in rats model .

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-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-106337

SB 247083	Endothelin Receptor	Cardiovascular Disease
SB 247083 is a selective, competitive and orally active **endothelin-A receptor** antagonist with a K_i of 0.41 nM. SB 247083 shows a K_i of 467 nM to **endothelin-B receptor. SB 247083 shows a K_b** of 3.5 nM for ET-1-induced contraction of rat aorta. SB 247083 can be used for the research of cardiovascular disease .

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-17621S

Sparsentan-d5 RE-021-d₅; DARA-a-d₅	Isotope-Labeled Compounds Angiotensin Receptor Endothelin Receptor	Cardiovascular Disease Endocrinology
Sparsentan-d₅ is deuterium labeled Sparsentan. Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with K_is of 0.8 and 9.3 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-105362

PD 155080	Endothelin Receptor	Cardiovascular Disease
PD 155080 is a selective endothelin A receptor (ET_A receptor) antagonist. PD 155080 reduces coronary resistance in the isolated rat heart model. PD 155080 improves myocardial systolic function and diastolic function in the ischemia/reperfusion model. PD 155080 can be used for the study of cardiovascular diseases .

HY-17352A

Clazosentan disodium Ro 61-1790 disodium; VML 588 disodium; AXV-034343 disodium	Endothelin Receptor	Cardiovascular Disease
Clazosentan disodium (Ro 61-1790) is a selective **endothelin A (ET_A) receptor** antagonist. Clazosentan disodium inhibits ET-1-mediated vasoconstriction. Clazosentan disodium prevents cerebral vasospasm, vasospasm-related cerebral infarction .

HY-13711

S-1255	Endothelin Receptor	Cardiovascular Disease
S-1255 is an orally active and highly selective **endothelin ETA receptor** antagonist (K_d=0.39 nM). S-1255 blocks vasoconstriction and sustains hypotensive effects in hypertensive rats. S-1255 is promising for research of hypertension and cardiovascular disorders .

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-17352R

Clazosentan (Standard) Ro 61-1790 (Standard); VML 588 (Standard); AXV-034343 (Standard)	Endothelin Receptor Reference Standards	Cardiovascular Disease
Clazosentan (Standard) is the analytical standard of Clazosentan. This product is intended for research and analytical applications. Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction .

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-103458

BMS 182874 hydrochloride	Endothelin Receptor	Cardiovascular Disease Metabolic Disease
BMS 182874 hydrochloride is an orallyactive, highly selective **endothelin receptor (ET_A** receptor) antagonist, with IC₅₀ value of 0.150 μM, K_i of 0.055 μM. BMS 182874 hydrochloride reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research .

HY-118497R

BMS 182874 (Standard)	Endothelin Receptor	Cardiovascular Disease Metabolic Disease
BMS 182874 (Standard) is the analytical standard of BMS 182874. This product is intended for research and analytical applications. BMS 182874 is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research .

HY-P2057

PD 142893	Endothelin Receptor	Cardiovascular Disease
PD 142893 is a **endothelin-B receptor** antagonist .

HY-B0323R

Sulfisoxazole (Standard) Sulfafurazole (Standard)	Reference Standards Endothelin Receptor Bacterial Antibiotic	Infection Endocrinology Cancer
Sulfisoxazole (Standard) is the analytical standard of Sulfisoxazole. This product is intended for research and analytical applications. Sulfisoxazole (Sulfafurazole) is an orally active **endothelin receptor** antagonist with IC₅₀ values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole is a sulfonamide antibacterial agent with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A .

HY-114674A

Atrasentan sodium	Endothelin Receptor	Cardiovascular Disease Endocrinology Cancer
Atrasentan sodium is an **endothelin receptor** antagonist with IC₅₀ of 0.0551 nM for ET_A .

Cat. No.	Product Name	Target	Research Area

HY-12378

BQ-123 3 Publications Verification	Endothelin Receptor	Cardiovascular Disease
BQ-123 is a potent and selective **endothelin A (ETA) receptor** antagonist with an IC₅₀ of 7.3 nM and a K_i of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .

HY-105183

PD 145065	Endothelin Receptor	Others
PD 145065 is a highly potent but non-selective endothelin receptor antagonist with an IC₅₀ value of 4 nM for the ET_A receptor for rabbit renal artery vascular smooth muscle cells .

HY-105168

TAK 044	Endothelin Receptor	Cardiovascular Disease
TAK 044 is an antagonist of **Endothelin Receptor**. TAK 044 strongly inhibits ET-induced deterioration in various animal models. TAK 044 can be used in study ET-related diseases such as acute myocardial infarction,acute renal failure, acute hepatic malfunction, and subarachnoid hemorrhage .

HY-P2057

PD 142893	Endothelin Receptor	Cardiovascular Disease
PD 142893 is a **endothelin-B receptor** antagonist .

HY-P1018

IRL 1038	Endothelin Receptor	Neurological Disease
IRL 1038 is an **endothelin B receptor** selective antagonist with a K_i of 6-11 nM .

HY-P4201

JKC 301	Vasopressin Receptor	Cardiovascular Disease
JKC 301 is a selective **Endothelin A receptor** antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking .

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-P10135

RES-701-1	Endothelin Receptor	Cardiovascular Disease
RES-701-1 is a cyclic peptide composed of 16 common L-amino acids, acting as a specific antagonist for the ET_B receptor. RES-701-1 can inhibit the binding of 125I-ET-1 (125I-labeled Endothelin (ET)-1) to the ET_B receptor, with an IC₅₀ value of 10 nM .

Cat. No.	Product Name	Target	Research Area	Image

HY-P990089

Patecibart Getagozumab; GMA-301	Endothelin Receptor	Cardiovascular Disease
Patecibart is a humanized immunoglobulin G4-kappa, anti-EDNRA monoclonal antibody. Patecibart is an **endothelin receptor** antagonist .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-120843

WS009A	Monophenols Microorganisms Phenols Source Classification	Endothelin Receptor
WS009A is an antagonist for **endothelin receptor** (ET Receptor) with IC₅₀ of 5.8 and 6.9 μM for ET-1 receptor and ET-2 receptor. WS009A can be used in 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-17621S

Sparsentan-d5
Sparsentan-d₅ is deuterium labeled Sparsentan. Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with K_is of 0.8 and 9.3 nM, respectively .

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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