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-117644
    L-749329
    		Antagonist
    L-749329 ((Rac)-L-754142) is an ETA and ETB receptor antagonist, with Kis of 0.062 nM and 2.25 nM for ETA and ETB respectively. L-749329 inhibits ET-1-stimulated signaling.
    L-749329
  • HY-134013
    Piperitenone oxide
    Piperitenone oxide is an orally active monoterpene ketone. Piperitenone oxide can be isolated from the essential oils of plants belonging to Mentha x villosa and Ziziphora clinopodioides. Piperitenone oxide induces differentiation. Piperitenone oxide induces chromosome breakage damage, aneuploidy damage and DNA single-strand breaks. Piperitenone oxide reduces ET-1 levels. Piperitenone oxide exerts antihypertensive effects. Piperitenone oxide can be used in studies related to colon cancer.
    Piperitenone oxide
  • HY-B0323R
    Sulfisoxazole (Standard)
    		Antagonist
    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.
    Sulfisoxazole (Standard)
  • HY-10088R
    Zibotentan (Standard)
    		Antagonist
    Zibotentan (Standard) is the analytical standard of Zibotentan. This product is intended for research and analytical applications. Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki 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.
    Zibotentan (Standard)
  • HY-114674A
    Atrasentan sodium
    		Antagonist
    Atrasentan sodium is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA.
    Atrasentan sodium
  • HY-103460R
    IRL 2500 (Standard)
    		Antagonist
    IRL 2500 (Standard) is the analytical standard of IRL 2500 (HY-103460). This product is intended for research and analytical applications. IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo.
    IRL 2500 (Standard)
  • HY-76520S
    Sitaxsentan-13C6
    		Antagonist
    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 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.
    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-180443
    AT1R antagonist 4
    AT1R antagonist 4 (Example 26) is an AT1R antagonist. AT1R antagonist 4 shows excellent antagonistic activity against calcium influx in cells stably expressing AT1 receptors and ETA receptors. AT1R antagonist 4 can be used in kidney disease research.
    AT1R antagonist 4
  • 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 (IPI 1040 sodium; TBC11251 sodium) (HY-11103). This product is intended for research and analytical applications. Sitaxsentan 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 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.
    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 (HY-15195). This product is intended for research and analytical applications. Avosentan 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.
    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-106994AR
    Nebentan potassium (Standard)
    		Antagonist
    Nebentan potassium (Standard) (GT-2331 maleate (Standard)) is the analytical standard of Nebentan (potassium) (HY-106994A). This product is intended for research and analytical applications. Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA 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 Ki of 0.697 nM and 569 nM, respectively. YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo.
    Nebentan potassium (Standard)
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Endothelin Receptor Isoform Comparison

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