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
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Endothelin Receptor Inhibitors
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Endothelin Receptor Agonists
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Endothelin Receptor Antagonists
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Endothelin Receptor Activators
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Endothelin Receptor Modulator
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Endothelin Receptor Control
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Endothelin Receptor Ligands
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Endothelin Receptor Proteins
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Endothelin Receptor Type A (EDNRA) Proteins
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Endothelin R Type B (EDNRB) Proteins
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Endothelin Receptor Related Products (155)
Related Products (155)
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Recombinant Proteins (7)
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Antibodies (1)
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Endothelin Receptor Isoform Comparison
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Vodudeutentan sodium
0 ImagesCat. No.: HY-147417ASCAS No.: 2364572-10-9Vodudeutentan sodium is a deuterated endothelin B receptor (ETBR) antagonist with no activity against human type A endothelin receptor (ETA). Vodudeutentan sodium can be incorporated into a controlled systemic release delivery system and can also be selectively combined with an additional antineoplastic agent. Vodudeutentan sodium is applicable to the research of urothelial carcinoma, bladder cancer and renal cell carcinoma.
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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.
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ETA antagonist 1
0 ImagesCat. No.: HY-112264CAS No.: 161801-60-1ETA antagonist 1 is a ETA selective antagonist with an IC50 of 0.08 μM.
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Sarafotoxin S6a TFA
0 ImagesCat. No.: HY-P1112ASarafotoxin S6a TFA , a sarafotoxin analogue, is a endothelin receptor agonist and has an ETA/ETB 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.
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Edonentan hydrate
0 ImagesCat. No.: HY-15402DCAS No.: 264609-13-4Synonyms: BMS 207940 hydrateEdonentan hydrate (BMS 207940 hydrate) is an orally active, highly selective endothelin A receptor (ETA receptor) antagonist with a Ki value of 0.01 nM against human targets. Edonentan hydrate 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 hydrate can be used in research related to cardiovascular diseases.
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Sulfisoxazole diethanolamine
0 ImagesSulfisoxazole (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.
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JKC 302
0 ImagesCat. No.: HY-P3228CAS No.: 153982-38-8JKC 302 is an ET-A receptor antagonist. JKC 302 partly blocks ET-1-induced contraction in asthmatic rat trachea ring.
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ABT-546
0 ImagesCat. No.: HY-135283CAS No.: 212481-66-8Synonyms: A-216546ABT-546 (A-216546) is an orally active ETA receptor antagonist, with Ki values of 0.46 nM and 13000 nM for human ETA and ETB receptors, respectively, and exhibits >25000-fold selectivity over the ETB receptor. ABT-546 effectively inhibits ET-1 (HY-P0202)-induced phosphoinositide hydrolysis (IC50 = 0.59 nM) and arachidonic acid release (IC50 = 3.03 nM), and antagonizes ET-1-induced contraction in isolated vascular rings. ABT-546 crosses the placental barrier but shows extremely low fetal exposure, with a favorable safety profile. ABT-546 inhibits ET-1-induced pressor response and downregulates the NLRP3/ROS/GSDMD-mediated pyroptosis pathway. ABT-546 can be used for research on abdominal aortic aneurysm.
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Rendomab B4
0 ImagesCat. No.: HY-P991964Synonyms: Rendomab-B49Rendomab B4 (Rendomab-B49) 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.
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PD 142893
0 ImagesCat. No.: HY-P2057CAS No.: 143037-36-9PD 142893 is a endothelin-B receptor antagonist.
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K-8794
0 ImagesCat. No.: HY-157658CAS No.: 180577-26-8K-8794 is an orally active selective endothelin receptor ETB antagonist that can be used in research on cardiovascular diseases.
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Big endothelin-3 (Human, 1-41 amide)
0 ImagesCat. No.: HY-P11605CAS No.: 133551-97-0Big endothelin-3 (Human, 1-41 amide) is a precursor molecule of the Endothelin-3 (ET-3) peptide composing of 41 amino acids.
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S-1255
0 ImagesCat. No.: HY-13711CAS No.: 203918-14-3S-1255 is an orally active and highly selective endothelin ETA receptor antagonist (Kd=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.
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BMS-187308
0 ImagesCat. No.: HY-117814CAS No.: 153624-15-8BMS-187308 is an orally active endothelin-A (ETA) antagonist, with Kis of 4.7 nM for ETA and 1.7 μM for ETB. BMS-187308 inhibits the pressor response to ET-1 (ED25: 1.2 µmol/kg; iv). BMS-187308 is a suitable tool for investigating the role of endothelin.
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Sarafotoxin S6b
0 ImagesCat. No.: HY-P3433CAS No.: 120972-53-4Sarafotoxin S6b is a vasoconstrictor peptide, and a non-selective endothelin receptor agonist. Sarafotoxin S6b can induce contraction in isolated human coronary arteries , the Ki values of Coronary artery, Saphenous vein and Coronary artery are 0.27, 0.55 and 19.5 nM, respectively.
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CI-1020
0 ImagesCat. No.: HY-103459CAS No.: 162256-50-0Synonyms: PD156707CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration.
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Cgs 27830
0 ImagesCat. No.: HY-182561CAS No.: 155485-56-6Cgs 27830 is an endothelin receptor antagonist with 20-fold higher selectivity for ET-A receptors over ET-B receptors. Cgs 27830 blocks activity of ET-A and ET-B receptors. Cgs 27830 does not alter basal vascular tone in the ovine fetal pulmonary circulation. Cgs 27830 prevents big-endothelin-1-induced pulmonary vasoconstriction in late gestation fetal lambs.
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Fandosentan potassium
0 ImagesCat. No.: HY-105408ACAS No.: 221246-12-4Fandosentan potassium is a potent endothelin A receptor (ETAR) 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].
