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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FR139317
0 ImagesCat. No.: HY-102092CAS No.: 142375-60-8Synonyms: PD 147953FR139317 (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.
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WS009B
0 ImagesCat. No.: HY-117634CAS No.: 136286-50-5WS009B 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.
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ATZ-1993
0 ImagesCat. No.: HY-122237CAS No.: 219705-77-8ATZ-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.
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Sitaxsentan sodium (Standard)
0 ImagesSynonyms: IPI 1040 sodium (Standard); TBC11251 sodium (Standard)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.
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ZD-1611
0 ImagesCat. No.: HY-19274CAS No.: 186497-38-1ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.
