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Endothelin Receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Endothelin Receptor (97) Endothelin-Converting Enzyme (ECE) (1) Amino Acid Derivatives (1) Angiotensin Receptor (3) Antibiotic (5) Apoptosis (6) Bacterial (5) CGRP Receptor (1) Cytochrome P450 (2) Drug Metabolite (2) Endogenous Metabolite (1) Estrogen Receptor/ERR (3) HIV (1) Integrin (1) Isotope-Labeled Compounds (3) Reference Standards (9) TGF-β Receptor (4) Vasopressin Receptor (1)
By Research Areas:	Cancer (22) Cardiovascular Disease (85) Endocrinology (29) Infection (7) Inflammation/Immunology (4) Metabolic Disease (13) Neurological Disease (9)

107

Inhibitors & Agonists

Peptides

Inhibitory Antibodies

Natural
Products

Recombinant Proteins

Isotope-Labeled Compounds

Antibodies

Endothelin 1 (swine, human) Maximum Cited Publications 8 Publications Verification 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 .

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.

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) .

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 .

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 .

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 .

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 .

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 .

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.

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 .

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 .

IRL-1620 1 Publications Verification	Endothelin Receptor	Neurological Disease Endocrinology
IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a K_i of 16 pM.

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 .

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 .

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.

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 .

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 .

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 .

Endothelin 1 (swine, human) TFA Maximum Cited Publications 8 Publications Verification 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 .

IRL-1620 TFA 1 Publications Verification	Endothelin Receptor	Cardiovascular Disease Neurological Disease Endocrinology
IRL-1620 (TFA) is a potent and selective endothelin receptor type B (ETB) agonist with a K_i of 16 pM .

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) .

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 .

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 .

Endothelin-2 (49-69), human Endothelin-2 (human, canine); Human Endothelin-2	Endothelin Receptor	Cardiovascular Disease Cancer
Endothelin-2 (49-69), human (Endothelin-2 (human, canine)) is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.

Endothelin-2 (49-69), human TFA Endothelin-2 (49-69) (human, canine) TFA; Human Endothelin-2 TFA	Endothelin Receptor	Cardiovascular Disease Cancer
Endothelin-2 (49-69), human (TFA) (Endothelin-2 (49-69) (human, canine) (TFA)) is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.

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.

Sarafotoxin S6c SRTX-c	Endothelin Receptor	Cardiovascular Disease
Sarafotoxin S6c (SRTX-c) is a potent **endothelin-B receptor** agonist. Sarafotoxin S6c can cause vasoconstriction in both endothelium-intact and endothelium-denuded vessels .

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) .

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 .

BQ-3020 ammonium	Endothelin Receptor	Cardiovascular Disease
BQ-3020 ammonium is a selective **endothelin receptor** (ET_B receptor) agonist. BQ-3020 ammonium inhibits [ ¹²⁵I] ET-1 binding to ET_B receptors, with an IC₅₀ value of 0.2 nM. BQ-3020 ammonium elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 ammonium makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research . .

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 .

Endothelin 1 (swine, human), Alexa Fluor 488-labeled	Endothelin Receptor	Cardiovascular Disease
Endothelin 1 (swine, human), Alexa Fluor 488-labeled is a synthetic Endothelin 1 peptide labled with Alexa Fluor 488. Endothelin 1 (swine, human) 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 .

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

BQ-3020	Endothelin Receptor	Cardiovascular Disease
BQ-3020 is a selective **endothelin receptor** (ET_B receptor) agonist that displaces [ ¹²⁵I] ET-1 binding to ET_B receptors, with an IC₅₀ value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research ¹ ².

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].

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 .

Endothelin (16-21)	Endothelin Receptor	Cardiovascular Disease
Endothelin (16-21) is a selective ETB receptor agonist (EC₅₀=228 nM in guinea-pig bronchus). Endothelin (16-21) can induce smooth muscle contraction. Endothelin (16-21) is promising for research of respiratory (e.g., asthma) and cardiovascular (e.g., hypertension) diseases .

[Lys4] Sarafotoxin S6c	Endothelin Receptor	Cardiovascular Disease
[Lys4] Sarafotoxin S6c, a sarafotoxin analogue, is a potent and partial agonist of **endothelin receptor. [Lys4] Sarafotoxin S6c elicits contraction of pig coronary artery, with an EC₅₀** of 1.5 nM .

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 .

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 .

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 .

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 .

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 .

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 .

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 .

Cat. No.	Product Name	Target	Research Area

HY-P0202

Endothelin 1 (swine, human) Maximum Cited Publications 8 Publications Verification 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-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-P0204A

Endothelin-3, human, mouse, rabbit, rat TFA 1 Publications Verification Endothelin 3 (Rat,Human) TFA	Endothelin Receptor Integrin	Neurological Disease
Endothelin-3, human, mouse, rabbit, rat TFA (Endothelin 3 (Rat,Human) TFA) is an adhesion stimulant. Endothelin-3, human, mouse, rabbit, rat TFA stimulates the adhesion of enteric neural crest cells to various ECM components. Endothelin-3, human, mouse, rabbit, rat TFA plays an important role in the maintenance and self-renewal of intestinal progenitor cells, participates in the migration of enteric neural crest cells, and helps maintain a suitable environment for the colonization of enteric neural crest cells. Endothelin-3, human, mouse, rabbit, rat TFA acts synergistically with the β1-integrin signaling pathway during enteric nervous system development. Endothelin-3, human, mouse, rabbit, rat TFA can be used in studies related to distal aganglionosis .

HY-16465

IRL-1620 1 Publications Verification	Endothelin Receptor	Neurological Disease Endocrinology
IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a K_i of 16 pM.

HY-P10633

SmBiT Tag	Amino Acid Derivatives	Others
SmBiT Tag is an 11-amino-acid short peptide with extremely low natural affinity for LgBiT, with a K_d value of approximately 190 μM. It serves as a core component of the NanoLuc Binary Technology (NanoBiT) system. NanoBiT is a bioluminescent reporter system based on protein fragment complementation technology, which is used to monitor dynamic protein-protein interactions in live cells and in vitro .

HY-P0202A

Endothelin 1 (swine, human) TFA Maximum Cited Publications 8 Publications Verification 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-16465A

IRL-1620 TFA 1 Publications Verification	Endothelin Receptor	Cardiovascular Disease Neurological Disease Endocrinology
IRL-1620 (TFA) is a potent and selective endothelin receptor type B (ETB) agonist with a K_i of 16 pM .

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-P0207

Endothelin-2 (49-69), human Endothelin-2 (human, canine); Human Endothelin-2	Endothelin Receptor	Cardiovascular Disease Cancer
Endothelin-2 (49-69), human (Endothelin-2 (human, canine)) is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.

HY-P0207A

Endothelin-2 (49-69), human TFA Endothelin-2 (49-69) (human, canine) TFA; Human Endothelin-2 TFA	Endothelin Receptor	Cardiovascular Disease Cancer
Endothelin-2 (49-69), human (TFA) (Endothelin-2 (49-69) (human, canine) (TFA)) is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.

HY-102029

Sarafotoxin S6c SRTX-c	Endothelin Receptor	Cardiovascular Disease
Sarafotoxin S6c (SRTX-c) is a potent **endothelin-B receptor** agonist. Sarafotoxin S6c can cause vasoconstriction in both endothelium-intact and endothelium-denuded vessels .

HY-P1016B

BQ-3020 ammonium	Endothelin Receptor	Cardiovascular Disease
BQ-3020 ammonium is a selective **endothelin receptor** (ET_B receptor) agonist. BQ-3020 ammonium inhibits [ ¹²⁵I] ET-1 binding to ET_B receptors, with an IC₅₀ value of 0.2 nM. BQ-3020 ammonium elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 ammonium makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research . .

HY-P2496

Endothelin 1 (swine, human), Alexa Fluor 488-labeled	Endothelin Receptor	Cardiovascular Disease
Endothelin 1 (swine, human), Alexa Fluor 488-labeled is a synthetic Endothelin 1 peptide labled with Alexa Fluor 488. Endothelin 1 (swine, human) 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-P1016

BQ-3020	Endothelin Receptor	Cardiovascular Disease
BQ-3020 is a selective **endothelin receptor** (ET_B receptor) agonist that displaces [ ¹²⁵I] ET-1 binding to ET_B receptors, with an IC₅₀ value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research ¹ ².

HY-P5769

Endothelin (16-21)	Endothelin Receptor	Cardiovascular Disease
Endothelin (16-21) is a selective ETB receptor agonist (EC₅₀=228 nM in guinea-pig bronchus). Endothelin (16-21) can induce smooth muscle contraction. Endothelin (16-21) is promising for research of respiratory (e.g., asthma) and cardiovascular (e.g., hypertension) diseases .

HY-P3563

[Lys4] Sarafotoxin S6c	Endothelin Receptor	Cardiovascular Disease
[Lys4] Sarafotoxin S6c, a sarafotoxin analogue, is a potent and partial agonist of **endothelin receptor. [Lys4] Sarafotoxin S6c elicits contraction of pig coronary artery, with an EC₅₀** of 1.5 nM .

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-P3433

Sarafotoxin S6b	Endothelin Receptor	Cardiovascular Disease
Sarafotoxin S6b is a vasoconstrictor peptide, and a non-selective **endothelin receptor agonist. Sarafotoxin S6b can induce contraction in isolated human coronary arteries , the K_i** values of Coronary artery, Saphenous vein and Coronary artery are 0.27, 0.55 and 19.5 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 .

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-P5130

Big endothelin-1 (rat 1-39)	Endothelin Receptor	Cardiovascular Disease
Big endothelin-1 (rat 1-39) is a 39-residues peptide. Big endothelin-1 (rat 1-39) induces diuretic and natriuretic response in conscious Sprague-Dawley rats. Big endothelin-1 (rat 1-39) raises blood pressure in mice .

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 .

HY-P991964

Rendomab B4 Rendomab-B49	Endothelin Receptor	Cancer
Rendomab B4 is a monoclonal antibody targeting ETB. Rendomab B4 preferentially binds to ETB in the active conformational state and exhibits selectivity for ETB on melanoma cells. Rendomab B4 inhibits the G protein-dependent phospholipase C (PLC) pathway, blocks ET-3-induced Gαi/o-mediated inhibition of adenylate cyclase, and does not affect the activation of the ERK1/2 pathway. Rendomab B4 is applicable to melanoma-related research .

Recombinant Proteins Recommended:

Endothelin Receptor

Species:	Human (4)
Tag:	GFP (1) His (1) Tag Free (1) Fc (1)
Source:	HEK293 (4)

Cat. No.	Compare	Product Name	Species	Source	Image

HY-P74180

	EDNRB/Endothelin R Type B Protein, Human (HEK293, His) EDNRB; Endothelin Receptor non-selective type; Endothelin Receptor type B; ETRB	Human	HEK293
	EDNRB/Endothelin R Type B Protein, a non-specific receptor for endothelin 1, 2, and 3, activates a phosphatidylinositol-calcium second messenger system through G proteins. This mechanism underscores its pivotal role in mediating cellular responses initiated by endothelin neuropeptides, emphasizing the versatility of EDNRB in transducing signals for various physiological processes. EDNRB/Endothelin R Type B Protein, Human (HEK293, His) is the recombinant human-derived EDNRB/Endothelin R Type B protein, expressed by HEK293 , with C-His labeled tag.

HY-P74181

	EDNRB/Endothelin R Type B Protein, Human (HEK293, Fc) EDNRB; Endothelin Receptor non-selective type; Endothelin Receptor type B; ETRB	Human	HEK293
	EDNRB/Endothelin R Type B Protein, a non-specific receptor for endothelin 1, 2, and 3, activates a phosphatidylinositol-calcium second messenger system through G proteins. This mechanism underscores its pivotal role in mediating cellular responses initiated by endothelin neuropeptides, emphasizing the versatility of EDNRB in transducing signals for various physiological processes. EDNRB/Endothelin R Type B Protein, Human (HEK293, Fc) is the recombinant human-derived EDNRB/Endothelin R Type B protein, expressed by HEK293 , with C-mFc labeled tag.

HY-P704571

	EDNRB/Endothelin R Type B Protein-VLP, Human (HEK293) EDNRB; Endothelin Receptor non-selective type; Endothelin Receptor type B; ETRB	Human	HEK293
	EDNRB/Endothelin R Type B Protein-VLP, Human (HEK293) is recommended for animal immunization, ELISA. It is not recommended for receptor-ligand interaction detection and SPR/BLI assay since there are other irrelevant membrane proteins of the host on the VLP envelope, and the receptor-ligand interaction will have strong background interference. High requirements for chips and experimental protocols are needed for SPR/BLI assays. If VLP control is required, it is recommended HY-P705433.

HY-P704572

	EDNRB/Endothelin R Type B Protein-VLP, Human (HEK293, GFP) EDNRB; Endothelin Receptor non-selective type; Endothelin Receptor type B; ETRB	Human	HEK293
	EDNRB/Endothelin R Type B Protein-VLP, Human (HEK293, GFP) is recommended for animal immunization, ELISA. It is not recommended for receptor-ligand interaction detection and SPR/BLI assay since there are other irrelevant membrane proteins of the host on the VLP envelope, and the receptor-ligand interaction will have strong background interference. High requirements for chips and experimental protocols are needed for SPR/BLI assays. If VLP control is required, it is recommended HY-P705433.

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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 .

Host:	Rabbit (4)
Reactivity:	Human (2) Rat (3) Mouse (1)
Application:	ICC/IF (1) IP (1) WB (4) FC (1)
Isotype:	IgG (4)
Conjugation:	Non-conjugated (4)
Clonality:	Monoclonal (3) Recombinant (2)
Modification:	Unmodified (3)

Cat. No.	Compare	Product Name	Application	Reactivity	Image

HY-P83510

	Endothelin Receptor B Antibody (YA3255) Endothelin B Receptor; ET-B; ET-BR; Endothelin Receptor non-selective type	WB, IP	Human
	Endothelin Receptor B Antibody (YA3255) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to Endothelin Receptor B.

HY-P810444

	Endothelin Receptor B Antibody (YA9754) Endothelin Receptor non-selective type, ET-B; ET-BR, Endothelin Receptor type B	WB, FC, ICC/IF	Human, Mouse, Rat
	Endothelin Receptor B Antibody (YA9754) is a Rabbit-derived and non-conjugated IgG Monoclonal antibody, targeting to Endothelin Receptor B.

HY-P83206

	GPR37 Antibody (YA2951) GPR37; Probable G-protein coupled Receptor 37; Endothelin B Receptor-like protein 1; ETBR-LP-1; Parkin-associated Endothelin Receptor-like Receptor; PAELR	WB	Rat
	GPR37 Antibody (YA2951) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to GPR37.

HY-P83206A

	GPR37 Antibody (YA2951)(PBS only) GPR37; Probable G-protein coupled Receptor 37; Endothelin B Receptor-like protein 1; ETBR-LP-1; Parkin-associated Endothelin Receptor-like Receptor; PAELR	WB	Rat
	GPR37 Antibody (YA2951) is a Rabbit-derived and non-conjugated IgG monoclonal antibody, targeting to GPR37.