ETB
Endothelin receptor ETB is a G protein-coupled endothelin receptor that regulates vascular function through endothelial relaxation, endothelin-1 clearance, and context-dependent smooth muscle contraction[1][2]. Mechanistically, endothelial ETB activation promotes nitric oxide, prostacyclin, and endothelium-derived hyperpolarizing factor release, thereby opposing ET-1-driven vasoconstriction[1][2]. In human renal and splanchnic circulation, ETA receptors mediate ET-1-induced vasoconstriction, whereas ETB receptors clear ET-1 and modulate vascular tone by altering plasma ET-1 concentration[1]. Endothelial-cell-specific ETB knockout mice show endothelial dysfunction, decreased endogenous NO release, and increased plasma ET-1, supporting ETB as a tonic vasodilator receptor[3]. In pulmonary disease models, ETB receptor deficiency increases lung endothelin levels, hypoxia-related vascular leak, HIF-1α, and VEGF content[4]. Compared with ETA, which preferentially binds ET-1 and drives vasoconstriction, ETB binds ET-1 and ET-3 and can function as a clearance, endothelial survival, relaxation, or contractile receptor depending on tissue localization[3][5][4]. For experimental applications, ETB-selective agonists such as IRL1620 or sarafotoxin S6c and antagonists such as BQ788 help distinguish endothelial ETB signaling from ETA-dominant vasoconstriction[4][6].
References:
- [1]. Böhm F, et al. ETA receptors mediate vasoconstriction, whereas ETB receptors clear endothelin-1 in the splanchnic and renal circulation of healthy men. Clin Sci (Lond). 2003 Feb;104(2):143-51. [Content Brief]
- [2]. Grant ES, et al. In vitro expression of endothelin-1 (ET-1) and the ETA and ETB ET receptors by the prostatic epithelium and stroma. J Clin Endocrinol Metab. 1997 Feb;82(2):508-13. [Content Brief]
- [3]. Seo B, et al. Both ETA and ETB receptors mediate contraction to endothelin-1 in human blood vessels. Circulation. 1994 Mar;89(3):1203-8. [Content Brief]
- [4]. Seo B, et al. ETA and ETB receptors mediate contraction to endothelin-1 in renal artery of aging SHR. Effects of FR139317 and bosentan. Hypertension. 1995 Apr;25(4 Pt 1):501-6. [Content Brief]
- [5]. Mikhail M, et al. Role of endothelin-1 and its receptors, ETA and ETB , in the survival of human vascular endothelial cells. Can J Physiol Pharmacol. 2017 Oct;95(10):1298-1305. [Content Brief]
- [6]. McDonald DM, et al. Characterization of endothelin A (ETA) and endothelin B (ETB) receptors in cultured bovine retinal pericytes. Invest Ophthalmol Vis Sci. 1995;36:1088-1094.
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ETB Related Products (42)
Related Products (42)
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Recombinant Proteins (4)
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Ro 46-8443
0 ImagesRo 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ETB (IC50: 34-69 nM) over ETA receptors (IC50: 6800 nM).
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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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[Ala1,3,11,15]-Endothelin (53-63) TFA
![[Ala1,3,11,15]-Endothelin (53-63) TFA](https://file.medchemexpress.com/product_pic/hy-p1019a.gif "Click to View [Ala1,3,11,15]-Endothelin (53-63) TFA Product Detail")
0 ImagesCat. No.: HY-P1019APurity: 98.18%[Ala1,3,11,15]-Endothelin (53-63) (TFA) is an ETB agonist. [Ala1,3,11,15]-Endothelin (53-63) (TFA) has selectivity for ETB with IC50 values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) (TFA) can be used for the research of vasoconstriction.
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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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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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RES-701-1
0 ImagesCat. No.: HY-P10135CAS No.: 151308-34-8RES-701-1 is a cyclic peptide composed of 16 common L-amino acids, acting as a specific antagonist for the ETB receptor. RES-701-1 can inhibit the binding of 125I-ET-1 (125I-labeled Endothelin (ET)-1) to the ETB receptor, with an IC50 value of 10 nM.
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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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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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BQ-3020
0 ImagesCat. No.: HY-P1016CAS No.: 143113-45-5BQ-3020 is a selective endothelin receptor (ETB receptor) agonist that displaces [125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research12.
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ABT-546 hydrochloride
0 ImagesCat. No.: HY-19309CAS No.: 223756-43-2Synonyms: A-216546 hydrochlorideABT-546 (A-216546) hydrochloride 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 hydrochloride 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 hydrochloride crosses the placental barrier but shows extremely low fetal exposure, with a favorable safety profile. ABT-546 hydrochloride inhibits ET-1-induced pressor response and downregulates the NLRP3/ROS/GSDMD-mediated pyroptosis pathway. ABT-546 hydrochloride can be used for research on abdominal aortic aneurysm.
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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.
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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.
