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Results for "

ET receptor antagonist

" in MedChemExpress (MCE) Product Catalog:

45

Inhibitors & Agonists

6

Peptides

1

Natural
Products

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-119667
    Enrasentan

    SB 217242

    		 Endothelin Receptor Cardiovascular Disease
    Enrasentan (SB 217242) is an endothelin (ET) receptor antagonist. Enrasentan has antihypertensive effects .
    Enrasentan
  • HY-13209
    Ambrisentan
    2 Publications Verification

    BSF 208075; LU 208075

    		 Endothelin Receptor Cardiovascular Disease Endocrinology
    Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
    Ambrisentan
  • HY-15894
    BQ-788 sodium salt
    5+ Cited Publications

    		 Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    BQ-788 sodium salt is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells .
    BQ-788 sodium salt
  • HY-15404
    Darusentan

    Lu-135252

    		 Endothelin Receptor Cardiovascular Disease Endocrinology
    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 .
    Darusentan
  • HY-155737
    ET receptor antagonist 1

    		Estrogen Receptor/ERR Cardiovascular Disease
    ET receptor antagonist 1 (compound 16h) is an orally active ET receptor antagonist (IC50=0.18 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 1 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
    ET receptor antagonist 1
  • HY-155739
    ET receptor antagonist 3

    		Estrogen Receptor/ERR Cardiovascular Disease
    ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist (IC50=0.26 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 3 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
    ET receptor antagonist 3
  • HY-155738
    ET receptor antagonist 2

    		Estrogen Receptor/ERR Cardiovascular Disease
    ET receptor antagonist 2 (compound 16j) is an orally active ET receptor antagonist (IC50=0.22 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 2 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
    ET receptor antagonist 2
  • HY-120843
    WS009A

    		Endothelin Receptor Cardiovascular Disease
    WS009A is an antagonist for endothelin receptor (ET Receptor) with IC50 of 5.8 and 6.9 μM for ET-1 receptor and ET-2 receptor. WS009A can be used in research of cardiovascular diseases .
    WS009A
  • HY-P3228
    JKC 302

    		Endothelin Receptor Cardiovascular Disease
    JKC 302 is an ET-A receptor antagonist. JKC 302 partly blocks ET-1-induced contraction in asthmatic rat trachea ring .
    JKC 302
  • HY-117634
    WS009B

    		Endothelin Receptor Cardiovascular Disease
    WS009B 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 .
    WS009B
  • HY-13209C
    Ambrisentan sodium

    BSF 208075 sodium; LU 208075 sodium

    		 Endothelin Receptor Cardiovascular Disease Endocrinology
    Ambrisentan (BSF 208075) sodium is a selective and orally active ET type A receptor (ETAR) antagonist .
    Ambrisentan sodium
  • HY-17351
    Tezosentan

    RO 610612

    		 Endothelin Receptor 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.
    Tezosentan
  • HY-P10135
    RES-701-1

    		Endothelin Receptor Cardiovascular Disease
    RES-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 .
    RES-701-1
  • HY-17352
    Clazosentan

    Ro 61-1790; VML 588; AXV-034343

    		 Endothelin Receptor Cardiovascular Disease
    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 .
    Clazosentan
  • HY-117644
    L-749329

    (Rac)-L-754142

    		 Endothelin Receptor Cardiovascular Disease
    L-749329 ((Rac)-L-754142) is an ETA and ETB receptor antagonist, with Kis of 0.062 nM and 2.25 nM for ETA and ETB respectively. L-749329 inhibits ET-1-stimulated signaling .
    L-749329
  • HY-15894A
    BQ-788
    5+ Cited Publications

    		 Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    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 .
    BQ-788
  • HY-17352A
    Clazosentan disodium

    Ro 61-1790 disodium; VML 588 disodium; AXV-034343 disodium

    		 Endothelin Receptor Cardiovascular Disease
    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 .
    Clazosentan disodium
  • HY-A0013A
    Bosentan hydrate
    Maximum Cited Publications
    29 Publications Verification

    		 Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    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.
    Bosentan hydrate
  • HY-13209R
    Ambrisentan (Standard)

    BSF 208075 (Standard); LU 208075 (Standard)

    		 Reference Standards Endothelin Receptor Cardiovascular Disease Endocrinology
    Ambrisentan (Standard) is the analytical standard of Ambrisentan. This product is intended for research and analytical applications. Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
    Ambrisentan (Standard)
  • HY-A0013
    Bosentan
    Maximum Cited Publications
    29 Publications Verification

    		 Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    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.
    Bosentan
  • HY-123744
    PD-156707

    		Endothelin Receptor Cardiovascular Disease
    PD-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 .
    PD-156707
  • HY-114674
    A-127722

    		Endothelin Receptor Cardiovascular Disease
    A-127722 is A 2, 4-dialarylpyrrolidine-3-carboxylic acid ETA selective endothelin receptor (ET receptor) antagonist with IC50 value of 0.36 nM .
    A-127722
  • HY-105168
    TAK 044

    		Endothelin Receptor Cardiovascular Disease
    TAK 044 is an antagonist of Endothelin Receptor. TAK 044 strongly inhibits ET-induced deterioration in various animal models. TAK 044 can be used in study ET-related diseases such as acute myocardial infarction,acute renal failure, acute hepatic malfunction, and subarachnoid hemorrhage .
    TAK 044
  • HY-19210
    SB-209670

    		Endothelin Receptor Cardiovascular Disease
    SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
    SB-209670
  • HY-78096
    O-Deshydroxyethyl bosentan

    		Endogenous Metabolite Metabolic Disease
    O-Deshydroxyethyl bosentan is a metabolite of Bosentan (HY-A0013), which is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors .
    O-Deshydroxyethyl bosentan
  • HY-17352R
    Clazosentan (Standard)

    		Endothelin Receptor Cardiovascular Disease
    Clazosentan (Standard) is the analytical standard of Clazosentan. This product is intended for research and analytical applications. 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 .
    Clazosentan (Standard)
  • HY-19529
    Ro 46-2005

    		Endothelin Receptor Cardiovascular Disease Endocrinology
    Ro 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.
    Ro 46-2005
  • HY-115417
    Bosentan-d4

    		Endothelin Receptor Cardiovascular Disease Endocrinology
    Bosentan-d4 is the deuterium labeled Bosentan. 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.
    Bosentan-d4
  • HY-11103
    Sitaxsentan sodium
    1 Publications Verification

    IPI 1040 sodium; TBC11251 sodium

    		 Endothelin Receptor Cardiovascular Disease Endocrinology
    Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) is a potent, selective and orally activeendothelin 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 inhibits ET-1-induced phosphoinositide turnover. Sitaxsentan sodium can significantly alleviate pulmonary arterial hypertension (PAH) symptoms. Sitaxsentan sodium can be used for the study of PAH .
    Sitaxsentan sodium
  • HY-P10151
    PD 156252

    		Endothelin Receptor Cardiovascular Disease
    PD 156252 is a hexapeptide that is a highly potent endothelin (ET) antagonist. PD 156252 has enhanced binding affinity for rabbit ETA and rat ETB receptor subtypes with IC50 values of 1.0 and 40 nM, respectively.
    PD 156252
  • HY-A0013AR
    Bosentan hydrate (Standard)

    		Reference Standards Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    Bosentan (hydrate) (Standard) is the analytical standard of Bosentan (hydrate). This product is intended for research and analytical applications. 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.
    Bosentan hydrate (Standard)
  • HY-13209S
    Ambrisentan-d10

    BSF 208075-d10; LU 208075-d10

    		 Isotope-Labeled Compounds Cardiovascular Disease
    Ambrisentan-d10 (BSF 208075-d10; LU 208075-d10) is the deuterium labled Ambrisentan (HY-13209). Ambrisentan is a selective ET type A receptor (ETAR) antagonist.
    Ambrisentan-d10
  • HY-107431
    Diphenylpyraline

    		Histamine Receptor Inflammation/Immunology
    Diphenylpyraline is a potent histamine H1 receptor antagonist. Diphenylpyraline acts as an orally active antihistamine agent with antimuscarinic and antiallergic effects. Diphenylpyraline can be used for the research of allergic diseases, including rhinitis and hay fever, and pruritic skin disorders et.al .
    Diphenylpyraline
  • HY-120295
    A-192621
    1 Publications Verification

    		 Endothelin Receptor Apoptosis Cardiovascular Disease Endocrinology
    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 .
    A-192621
  • HY-10383
    J-104132

    		Endothelin Receptor Cardiovascular Disease Metabolic Disease
    J-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].
    J-104132
  • HY-107431R
    Diphenylpyraline (Standard)

    		Reference Standards Histamine Receptor Inflammation/Immunology
    Diphenylpyraline (Standard) is the analytical standard of Diphenylpyraline. This product is intended for research and analytical applications. Diphenylpyraline is a potent histamine H1?receptor antagonist. Diphenylpyraline acts as an orally active antihistamine agent?with antimuscarinic and antiallergic effects. Diphenylpyraline can be used for the research of allergic diseases, including rhinitis and hay fever, and pruritic skin disorders et.al .
    Diphenylpyraline (Standard)
  • HY-16474
    Relugolix

    TAK-385

    		 GnRH Receptor Endocrinology Cancer
    Relugolix (TAK-385)?is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .
    Relugolix
  • HY-15195
    Avosentan

    Ro 67-0565; SPP-301

    		 Endothelin Receptor Cardiovascular Disease Endocrinology
    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 .
    Avosentan
  • HY-15195R
    Avosentan (Standard)

    Ro 67-0565 (Standard); SPP-301 (Standard)

    		 Reference Standards Endothelin Receptor Cardiovascular Disease Endocrinology
    Avosentan (Standard) is the analytical standard of Avosentan (HY-15195). This product is intended for research and analytical applications. Avosentan 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.
    Avosentan (Standard)
  • HY-P4683A
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin acetate

    		Vasopressin Receptor Cardiovascular Disease
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin is a potent vasopressin V1 receptor (VP V1R) antagonist. (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin significantly decreases the mean arterial pressure (MAP) in rats .
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin acetate
  • HY-P4683
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin

    		Vasopressin Receptor Cardiovascular Disease
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin is a potent vasopressin V1 receptor (VP V1R) antagonist. (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin significantly decreases the mean arterial pressure (MAP) in rats .
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin
  • HY-16474S
    Relugolix-d6

    TAK-385-d6

    		 Isotope-Labeled Compounds GnRH Receptor Endocrinology Cancer
    Relugolix-d6 is deuterium labeled Relugolix. Relugolix (TAK-385)?is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .
    Relugolix-d6
  • HY-16474R
    Relugolix (Standard)

    TAK-385 (Standard)

    		 Reference Standards GnRH Receptor Endocrinology Cancer
    Relugolix (Standard) is the analytical standard of Relugolix. This product is intended for research and analytical applications. Relugolix (TAK-385) is a potent, orally active, nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist. Relugolix possesses high affinity and potent antagonistic activity for human receptor (binding IC50=0.33 nM) and monkey receptor (IC50=0.32 nM) compared with TAK-013 (HY-100209) . Relugolix is used for the study of sex-hormone-dependent diseases, such as including endometriosis, uterine fibroids and prostate cancer et al .
    Relugolix (Standard)
  • HY-135390
    Hydroxy desmethyl Bosentan

    Ro 64-1056

    		 Drug Metabolite Cardiovascular Disease
    Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver . 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. Bosentan can be used in treatment of pulmonary arterial hypertension .
    Hydroxy desmethyl Bosentan
  • HY-W781265
    BE 24566B

    L-755,805

    		 Endothelin Receptor Bacterial Infection
    BE 24566B is a polyketide fungal metabolite originally isolated from S. violaceusniger. It is active against B. subtilis, B. cereus, S. aureus, M. luteus, E. faecalis, and S. thermophilus (MICs=1.56, 1.56, 1.56, 1.56, 3.13, and 3.13 μg/mL, respectively). BE 24566B is an endothelin (ET) receptor antagonist (IC50s=11 and 3.9 μM for ETA and ETB receptors, respectively).
    BE 24566B

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