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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
83 Results for "
ETA Receptor
" in MedChemExpress (MCE) Product Catalog:
Products (83)
83 Results for "ETA Receptor" in MCE Product Catalog:
32
32 Publications Verification
Cat. No.: HY-A0013
CAS No.: 147536-97-8
Target:
Research Areas:
Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
32
32 Publications Verification
Cat. No.: HY-A0013A
CAS No.: 157212-55-0
Target:
Research Areas:
Bosentan hydrate is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
15
15 Cited Publications
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Research Areas:
BQ-788 is a potent, selective ETB receptor antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, poorly inhibiting the binding to ETA receptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM .
14
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Research Areas:
Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .
10
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10
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6
6 Cited Publications
Synonyms: ABT-627; (+)-A 127722; A-147627
Target:
Research Areas:
Atrasentan (ABT-627) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA .
6
6 Cited Publications
Synonyms: ABT-627 hydrochloride; (+)-A 127722 hydrochloride; A-147627 hydrochloride
Target:
Research Areas:
Atrasentan hydrochloride (ABT-627 hydrochloride) is a selective endothelin A receptor antagonist with an IC50 of 0.0551 nM for ETA .
4
4 Cited Publications
Target:
Research Areas:
2
2 Cited Publications
Synonyms: IPI 1040 sodium; TBC11251 sodium
Target:
Research Areas:
Sitaxsentan sodium (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 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 .
2
2 Cited Publications
Target:
Research Areas:
A-192621, a chemical probe, is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level .
2
Target:
Research Areas:
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 .
1
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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 .
1
1 Cited Publications
Cat. No.: HY-17352
CAS No.: 180384-56-9
Synonyms: Ro 61-1790; VML 588; AXV-034343
Target:
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Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction .
1
1 Cited Publications
Cat. No.: HY-17352A
CAS No.: 503271-02-1
Synonyms: Ro 61-1790 disodium; VML 588 disodium; AXV-034343 disodium
Target:
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Clazosentan disodium (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan disodium inhibits ET-1-mediated vasoconstriction. Clazosentan disodium prevents cerebral vasospasm, vasospasm-related cerebral infarction .
1
1 Cited Publications
Cat. No.: HY-P86804
Synonyms: 4930549J05Rik antibody;
A430104F18Rik antibody;
AW552088 antibody;
Cd247 antibody;
CD3 antibody;
CD3 delta antibody;
CD3 epsilon antibody;
CD3 ETA antibody;
CD3 gamma antibody;
CD3 zETA antibody;
CD3H antibody;
CD3Q antibody;
CD3Z antibody;
CD3zETA antibody;
Ctg3 antibody;
FLJ17620 antibody;
FLJ17664 antibody;
FLJ18683 antibody;
FLJ79544 antibody
FLJ94613 antibody;
IMD19 antibody;
Leu-4 antibody;
MGC138597 antibody;
OKT3, delta chain antibody;
OTTHUMP00000032544 antibody;
T cell Receptor antibody;
T3 antibody;
T3d antibody;
T3e antibody;
T3g antibody;
T3z antibody;
TCRE antibody;
TCRk antibody;
Tcrz antibody;
TCRzETA antibody
Cat. No.: HY-17351
CAS No.: 180384-57-0
Synonyms: RO 610612
Target:
Research Areas:
Cardiovascular Disease Neurological Disease Endocrinology Cancer
Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.
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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 .
Synonyms: Ro 67-0565; SPP-301
Target:
Research Areas:
Avosentan (Ro 67-0565; SPP-301) 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 .
Synonyms: Lu-135252
Target:
Research Areas:
Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors . Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
