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endothelin ETA receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Endothelin Receptor (64) Angiotensin Receptor (1) Antibiotic (1) Apoptosis (7) Bacterial (1) COX (1) Drug Metabolite (1) Endogenous Metabolite (1) Fluorescent Dye (1) Interleukin Related (1) Isotope-Labeled Compounds (2) MMP (1) NF-κB (1) Prostaglandin Receptor (1) Radionuclide-Drug Conjugates (RDCs) (1) Reference Standards (8) TGF-β Receptor (4) TNF Receptor (1)
By Research Areas:	Cancer (16) Cardiovascular Disease (58) Endocrinology (21) Infection (2) Inflammation/Immunology (5) Metabolic Disease (11) Neurological Disease (5)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

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

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-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-119843

Asterric Acid Dimethylosoic acid; RES-1214-1; TAN 1415A	Antibiotic	Infection
Asterric acid is an antibiotic fungal metabolite that completely inhibits the binding of the potent vasoconstrictor endothelin (ET)-1 to the ETA receptor in A10 cells at 0.1 μM.1 Asterric acid derivatives have also been shown to inhibit VEGF-induced tube formation of human umbilical vein endothelial cells at 3-10 μM, which suggests its usefulness as an antiangiogenic agent.

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-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-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 .

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-101262

SB234551	Endothelin Receptor	Neurological Disease
SB234551 is a selective endothelin *ETA* receptor antagonist. SB234551 can be used in the study of stroke model .

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-102092

FR139317 PD 147953	Endothelin Receptor	Cardiovascular Disease
FR139317 (PD 147953) is a selective **ET_A receptor** antagonist. FR139317 inhibits cerebral activation by intraventricular endothelin-1 in conscious rats. FR139317 also ameliorates cerebral vasospasm in dogs .

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-15402D

Edonentan hydrate BMS 207940 hydrate	Endothelin Receptor	Cardiovascular Disease
Edonentan (BMS 207940) hydrate is a potent and selective antagonist of the **endothelin A (ETA) receptor, with a K_i** of 10 pM. In rats, Edonentan has superior (100%) oral bioavailbility .

HY-114674

A-127722	Endothelin Receptor	Cardiovascular Disease
A-127722 is A 2, 4-dialarylpyrrolidine-3-carboxylic acid ET_A selective endothelin receptor (ET receptor) antagonist with IC₅₀ value of 0.36 nM .

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-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-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-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-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-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.

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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