Endothelin Receptor
Endothelin receptors are G protein-coupled receptors (GPCRs) of the β-group of rhodopsin receptors that bind to endothelin ligands, which are 21 amino acid long peptides derived from longer prepro-endothelin precursors. There are at least four types known, ETA, ETB (ETB1, ETB2) and ETC. The ETA receptor is characterized by having high affinity and selectivity for ET-1 and ET-2 compared to ET-3, whereas the ETB receptor has equivalent high affinity for all three endothelin isopeptides.
Endothelins are synthesized in several tissues, including the vascular endothelium (ET-1 exclusively) and smooth muscle cells. Released endothelin binds to the endothelin receptors ETA and ETB, the ETA receptors on vascular smooth muscle cells mediating vasoconstriction, and the ETB receptors on the endothelium linked to nitric oxide (NO) and prostacyclin release.
Endothelin Receptor Isoform Specific Products
All Product Categories
-
Endothelin Receptor Inhibitors
(18)
View all products
-
Endothelin Receptor Agonists
(14)
View all products
-
Endothelin Receptor Antagonists
(94)
View all products
-
Endothelin Receptor Activators
(2)
View all products
-
Endothelin Receptor Modulator
(1)
View all products
-
Endothelin Receptor Control
(1)
View all products
-
Endothelin Receptor Ligands
(3)
View all products
-
Endothelin Receptor Proteins
(7)
View all products
-
Endothelin Receptor Type A (EDNRA) Proteins
(3)
View all products
-
Endothelin R Type B (EDNRB) Proteins
(4)
View all products
-
Endothelin Receptor Related Products (152)
Related Products (152)
-
Recombinant Proteins (7)
-
Antibodies (1)
-
Endothelin Receptor Isoform Comparison
-
Edonentan
0 ImagesSynonyms: BMS 207940Edonentan (BMS 207940) is an orally active, highly selective endothelin A receptor (ETA receptor) antagonist with a Ki value of 0.01 nM against human targets. Edonentan blocks the pressor response induced by Big Endothelin-1 in conscious normotensive rats and the pressor response induced by ET-1 in conscious normotensive cynomolgus monkeys. Edonentan can be used in research related to cardiovascular diseases.
-
Diosuxentan
0 ImagesCat. No.: HY-153463CAS No.: 2305865-93-2Synonyms: SC0062Diosuxentan is an inhibitor of ETA. Diosuxentan can be used in research for cardiovascular, renal and neuronal inflammation diseases.
-
Sitaxsentan
0 ImagesSynonyms: IPI 1040; TBC-11251Sitaxsentan (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 Ki 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.
-
PD-156707
0 ImagesPD-156707 is an orally active, nonpeptide and selective Endothelin-A receptor antagonist. PD-156707 binds to human ET-A and ET-B receptors with Ki 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.
-
Macitentan (Standard)
0 ImagesSynonyms: ACT-064992 (Standard)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).
-
BQ-123 TFA
0 ImagesCat. No.: HY-12378ABQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
-
Ambrisentan sodium
0 ImagesCat. No.: HY-13209CCAS No.: 1386915-48-5Synonyms: BSF 208075 sodium; LU 208075 sodiumAmbrisentan (BSF 208075) sodium is a selective and orally active ET type A receptor (ETAR) antagonist.
-
Bosentan-d4
0 ImagesCat. No.: HY-115417CAS No.: 1065472-77-6Bosentan-d4 is the deuterium labeled Bosentan. Bosentan 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.
-
(Rac)-Ambrisentan-d3
0 ImagesCat. No.: HY-13209BSCAS No.: 1189479-60-4(Rac)-Ambrisentan-d3 is the deuterium labeled (Rac)-Ambrisentan.
-
Sulfatroxazole-d4
0 ImagesCat. No.: HY-105829SSynonyms: Isosulfafurazole-d4Sulfatroxazole-d4 (Isosulfafurazole-d4) is the deuterium labeled Sulfatroxazole (HY-105829). Sulfatroxazole (Isosulfafurazole) (compound 12) is a selective antagonist of ETA receptor (IC50 of 0.26 μM).
-
[Ala1,3,11,15]-Endothelin (53-63)
![[Ala1,3,11,15]-Endothelin (53-63)](https://file.medchemexpress.com/product_pic/hy-p1019.gif "Click to View [Ala1,3,11,15]-Endothelin (53-63) Product Detail")
0 ImagesCat. No.: HY-P1019CAS No.: 121204-87-3[Ala1,3,11,15]-Endothelin (53-63) is an ETB agonist. [Ala1,3,11,15]-Endothelin (53-63) has selectivity for ETB with IC50 values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) can be used for the research of vasoconstriction
-
BMS-193884
0 ImagesCat. No.: HY-19263CAS No.: 176960-47-7BMS-193884 is a selective, orally active, and competitive ETA antagonist with 10000-fold greater affinity for the human ETA receptor (Ki=1.4 nM) than for the ETB receptor.
-
BMS-248360
0 ImagesCat. No.: HY-114953CAS No.: 254737-87-6BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA) receptor, with Kis of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 displays hypertensive effects.
-
Methylsolfonyl 25(S)-Δ7-dafachronic acid
0 ImagesCat. No.: HY-157940Methylsolfonyl 25(S)-Δ7-dafachronic acid (compound 3) is a selective ssDAF-12 agonist with the IC50 of 0.41 μM. Methylsolfonyl 25(S)-Δ7-dafachronic acid shows low cell cytotoxicity in HepG2 cells with IC50 of >200 μM. Methylsolfonyl 25(S)-Δ7-dafachronic acid can be used for study of parasitism.
-
TBC3711
0 ImagesCat. No.: HY-106182CAS No.: 349453-49-2TBC3711 is a endothelin receptor modulator, used for the research of endothelin-mediated disorders.
-
[Lys4] Sarafotoxin S6c
![[Lys4] Sarafotoxin S6c](https://file.medchemexpress.com/product_pic/hy-p3563.gif "Click to View [Lys4] Sarafotoxin S6c Product Detail")
0 ImagesCat. No.: HY-P3563CAS No.: 1219444-22-0[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.
-
DEDN6526A Antibody
0 ImagesCat. No.: HY-P990573Synonyms: RG-7636DEDN6526A (RG-7636) is a humanized antibody expressed in CHO cells, targeting ETBR. DEDN6526A (RG-7636) has a huIgG1 type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for DEDN6526A (RG-7636) can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
-
Bosentan hydrate (Standard)
0 ImagesBosentan (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.
-
RES-701-1
0 ImagesCat. No.: HY-P10135CAS No.: 151308-34-8RES-701-1 is a cyclic peptide composed of 16 common L-amino acids, acting as a specific antagonist for the ETB receptor. RES-701-1 can inhibit the binding of 125I-ET-1 (125I-labeled Endothelin (ET)-1) to the ETB receptor, with an IC50 value of 10 nM.
-
SB 247083
0 ImagesCat. No.: HY-106337CAS No.: 188186-61-0SB 247083 is a selective, competitive and orally active endothelin-A receptor antagonist with a Ki of 0.41 nM. SB 247083 shows a Ki of 467 nM to endothelin-B receptor. SB 247083 shows a Kb of 3.5 nM for ET-1-induced contraction of rat aorta. SB 247083 can be used for the research of cardiovascular disease.
