2. Signaling Pathways
  3. GPCR/G Protein
  4. Endothelin Receptor

Endothelin Receptor

Endothelin Receptor

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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:

Endothelin Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-114674A
    Atrasentan sodium
    		Antagonist
    Atrasentan sodium is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA.
    Atrasentan sodium
  • HY-N5171
    Aselacin B
    		Antagonist
    Aselacin B targets endothelin-1 receptor (ET-1 receptor), inhibits the the binding of ET-1 to ETA receptor and ETB receptor. Aselacin B can be used for research of cardiovascular diseases.
    Aselacin B
  • HY-76520S
    Sitaxsentan-13C6
    		Antagonist
    Sitaxsentan-13C6 (IPI 1040-13C6) is 13C labeled Sitaxsentan (HY-76520). Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist.
    Sitaxsentan-<sup>13</sup>C<sub>6</sub>
  • HY-118497R
    BMS 182874 (Standard)
    		Antagonist
    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.
    BMS 182874 (Standard)
  • HY-102092
    FR139317
    		Antagonist
    FR139317 (PD 147953) is a selective ETA receptor antagonist. FR139317 inhibits cerebral activation by intraventricular endothelin-1 in conscious rats. FR139317 also ameliorates cerebral vasospasm in dogs.
    FR139317
  • HY-117634
    WS009B
    		Antagonist
    WS009B is a selective endothelin receptor antagonist (ET-1: IC50=0.67 μM; ET-2: IC50=0.8 μM). WS009B can be used in the study of cardiovascular diseases.
    WS009B
  • HY-122237
    ATZ-1993
    		Antagonist
    ATZ-1993 is an orally active, nonpeptide endothelin receptor subtype Aand endothelin receptor subtype B antagonist with pKi values of 8.69, 7.20, respectively. ATZ-1993 has the potential for the research of intimal hyperplasia after balloon denudation of the carotid artery.
    ATZ-1993
  • HY-103458
    BMS 182874 hydrochloride
    		Antagonist
    BMS 182874 hydrochloride is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki 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.
    BMS 182874 hydrochloride
  • HY-11103R
    Sitaxsentan sodium (Standard)
    		Inhibitor
    Sitaxsentan (sodium) (Standard) is the analytical standard of Sitaxsentan (sodium). This product is intended for research and analytical applications. Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is an orally active, highly selective antagonist of endothelin A receptors.
    Sitaxsentan sodium (Standard)
  • HY-P1018
    IRL 1038
    		Antagonist
    IRL 1038 is an endothelin B receptor selective antagonist with a Ki of 6-11 nM.
    IRL 1038
  • HY-15195R
    Avosentan (Standard)
    		Antagonist
    Avosentan (Standard) is the analytical standard of Avosentan. This product is intended for research and analytical applications. 0
    Avosentan (Standard)
  • HY-118695
    IRL-3630
    		Antagonist
    IRL-3630 (Compound 3) is an ETA/ETB antagonist (Ki: 1.9 and 1.2 nM).
    IRL-3630
  • HY-19890
    Aminaftone
    		Inhibitor
    Aminaftone, a derivative of 4-aminobenzoic acid, downregulates endothelin-1 (ET-1) production in vitro by interfering with the transcription of the pre-pro-ET-1 gene.
    Aminaftone
  • HY-101598
    PD-159020
    		Antagonist
    PD-159020 is a non-selective ETA/ETB antagonist, with IC50s of 30 and 50 nM for hETA and hETB, respectively.
    PD-159020
  • HY-19274
    ZD-1611
    		Antagonist
    ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.
    ZD-1611
  • HY-17352A
    Clazosentan disodium
    		Antagonist
    Clazosentan disodium (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan disodium inhibits ET-1-mediated vasoconstriction. Clazosentan disodium prevents cerebral vasospasm, vasospasm-related cerebral infarction.
    Clazosentan disodium
  • HY-15895R
    Aprocitentan (Standard)
    		Antagonist
    Aprocitentan (Standard) is the analytical standard of Aprocitentan. This product is intended for research and analytical applications. Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively.
    Aprocitentan (Standard)
  • HY-19210
    SB-209670
    		Antagonist
    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 (Ki=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.
    SB-209670
  • HY-N5170
    Aselacin A
    		Antagonist
    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.
    Aselacin A
  • HY-120843
    WS009A
    		Antagonist
    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.
    WS009A
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Endothelin Receptor Isoform Comparison

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