ETA
Endothelin receptor ETA is a G protein-coupled receptor activated by endothelin-1 and endothelin-2, while endothelin-3 has lower affinity for ETA[1]. Mechanistically, ET-1/ETA signaling contributes to vasoconstriction, vascular and cardiac hypertrophy, inflammation, and cardiovascular disease progression[2]. In kidney disease, ETA activation causes sustained afferent arteriolar vasoconstriction, hyperfiltration, podocyte damage, proteinuria, and GFR decline[3]. Compared with ETB, ETA predominates on smooth muscle and mediates many pathophysiological actions of ET-1, whereas endothelial ETB releases vasodilators and clears ET-1[4]. In human coronary studies, endogenous endothelin predominantly via ETA receptor stimulation contributes to basal constrictor tone and endothelial dysfunction[5]. For experimental applications, selective ETA antagonists such as BQ-123 help delineate receptor function, while approved endothelin receptor antagonists include bosentan, macitentan, and ambrisentan[4].
References:
- [1]. Davenport AP, et al. Endothelin. Pharmacol Rev. 2016 Apr;68(2):357-418. [Content Brief]
- [2]. Dhaun N, et al. Endothelins in cardiovascular biology and therapeutics. Nat Rev Cardiol. 2019 Aug;16(8):491-502. [Content Brief]
- [3]. Martínez-Díaz I, et al. Endothelin Receptor Antagonists in Kidney Disease. Int J Mol Sci. 2023 Feb 8;24(4):3427. [Content Brief]
- [4]. Maguire JJ, et al. Endothelin receptors and their antagonists. Semin Nephrol. 2015 Mar;35(2):125-36. [Content Brief]
- [5]. Halcox JP, et al. Endogenous endothelin in human coronary vascular function: differential contribution of endothelin receptor types A and B. Hypertension. 2007 May;49(5):1134-41. [Content Brief]
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ETA Related Products (45)
Related Products (45)
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Recombinant Proteins (3)
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Nebentan
0 ImagesCat. No.: HY-106994CAS No.: 403604-85-3Synonyms: YM598 free baseNebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan 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.
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Nebentan potassium
0 ImagesSynonyms: YM598Nebentan 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.
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J-104132
0 ImagesCat. No.: HY-10383CAS No.: 198279-45-7J-104132 (L-753037) is a potent, orally active, selective and competitive ETA/ETB receptor antagonist with Ki 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].
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Ro 46-2005
0 ImagesRo 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.
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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.
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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.
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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.
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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.
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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.
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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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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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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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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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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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PD 155080
0 ImagesCat. No.: HY-105362CAS No.: 162412-71-7PD 155080 is a selective endothelin A receptor (ETA 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.
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BQ-610
0 ImagesCat. No.: HY-135446CAS No.: 141595-53-1BQ-610 is a selective antagonist of the endothelin A receptor (ETA receptor). BQ-610 specifically blocks the ETA receptor, competitively inhibiting the binding of endothelin-1 (ET-1) (a vasoconstrictive peptide) to the receptor, thereby blocking the effects of ET-1 such as vascular smooth muscle contraction, cell mitosis, and inhibition of hormone secretion. BQ-610 significantly alleviates cerebral vasospasm in rabbits. BQ-610 blocks the bronchial epithelial and pulmonary vascular cell proliferation caused by cigarette smoke in rat models. BQ-610 can delay the natural luteal regression in the cow's uterus. BQ-610 can be used for research on vasospasm, abnormal cell proliferation, and reproductive endocrine disorders.
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Sitaxsentan-13C6
0 ImagesCat. No.: HY-76520SSynonyms: IPI 1040-13C6 ; TBC-11251-13C6Sitaxsentan-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.
