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Isoforms Recommended: ETA
Results for "

eta

" in MedChemExpress (MCE) Product Catalog:

104

Inhibitors & Agonists

1

Screening Libraries

10

Peptides

4

Natural
Products

13

Recombinant Proteins

4

Isotope-Labeled Compounds

12

Antibodies

5

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P0202
    Endothelin 1 (swine, human)
    Maximum Cited Publications
    8 Publications Verification

    ET-1 (swine, human)

    Endothelin Receptor Metabolic Disease Inflammation/Immunology
    Endothelin 1 (swine, human) (ET-1) is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. Endothelin 1 acts through two types of receptors ETA and ETB .
    Endothelin 1 (swine, human)
  • HY-10343
    Sotrastaurin
    20+ Cited Publications

    AEB071

    MARCKS PKC Inflammation/Immunology Cancer
    Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively .
    Sotrastaurin
  • HY-14184
    Macitentan
    10+ Cited Publications

    ACT-064992

    Endothelin Receptor Apoptosis Cardiovascular Disease Endocrinology Cancer
    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) .
    Macitentan
  • HY-A0013
    Bosentan
    Maximum Cited Publications
    30 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-18980
    Rottlerin
    20+ Cited Publications

    Mallotoxin; NSC 56346; NSC 94525

    PKC Autophagy Apoptosis HIV RABV Infection Cancer
    Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation . Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection .
    Rottlerin
  • HY-11103
    Sitaxsentan sodium
    2 Publications Verification

    IPI 1040 sodium; TBC11251 sodium

    Endothelin Receptor TGF-β Receptor Cardiovascular Disease Metabolic Disease
    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 .
    Sitaxsentan sodium
  • HY-12378
    BQ-123
    3 Publications Verification

    Endothelin Receptor Cardiovascular Disease
    BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
    BQ-123
  • HY-10088
    Zibotentan
    1 Publications Verification

    ZD4054

    Endothelin Receptor Apoptosis Endocrinology Cancer
    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 .
    Zibotentan
  • HY-15403
    Atrasentan
    5+ Cited Publications

    ABT-627; (+)-A 127722; A-147627

    Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    Atrasentan (ABT-627) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA .
    Atrasentan
  • HY-15895
    Aprocitentan
    3 Publications Verification

    ACT-132577

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .
    Aprocitentan
  • HY-15894A
    BQ-788
    10+ 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-A0013A
    Bosentan hydrate
    Maximum Cited Publications
    30 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-12307
    (-)-Indolactam V
    2 Publications Verification

    Indolactam V

    PKC Cancer
    (-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.
    (-)-Indolactam V
  • HY-15403A
    Atrasentan hydrochloride
    5+ Cited Publications

    ABT-627 hydrochloride; (+)-A 127722 hydrochloride; A-147627 hydrochloride

    Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    Atrasentan hydrochloride (ABT-627 hydrochloride) is a selective endothelin A receptor antagonist with an IC50 of 0.0551 nM for ETA .
    Atrasentan hydrochloride
  • HY-148396

    DNA/RNA Synthesis Infection Cancer
    UCK2 Inhibitor-3 is a non-competitive inhibitor of uridine-cytidine kinase 2 (UCK2, a pyrimidine salvage enzyme) with an IC50 value of 16.6 μM. UCK2 can replace dihydroorotate dehydrogenase (DHODH), in a certain extent, in infected or rapidly dividing cells to continue efficient uridine salvage. UCK2 Inhibitor-3 also inhibits DNA polymerase eta and kappa with IC50s of 56 μM and 16 μM .
    UCK2 Inhibitor-3
  • HY-17352

    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-15895S

    ACT-132577-d4

    Isotope-Labeled Compounds Endothelin Receptor Cardiovascular Disease Endocrinology
    Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .
    Aprocitentan-d4
  • HY-17351

    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-103460

    Endothelin Receptor Cardiovascular Disease
    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 .
    IRL 2500
  • HY-15195

    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-120295
    A-192621
    2 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-P0202A
    Endothelin 1 (swine, human) TFA
    Maximum Cited Publications
    8 Publications Verification

    ET-1 (swine, human) TFA

    Endothelin Receptor Cardiovascular Disease
    Endothelin 1 (swine, human) (ET-1) TFA is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. Endothelin 1 TFA acts through two types of receptors ETA and ETB .
    Endothelin 1 (swine, human) TFA
  • HY-15404

    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-19431

    Endothelin Receptor Cardiovascular Disease
    Ro 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) .
    Ro 46-8443
  • HY-117664

    Reverse Transcriptase Inflammation/Immunology Cancer
    PNR-7-02 inhibits Pol η function with an IC50 value of near 8 μM, which binds to the little finger domain. PNR-7-02 is also an inhibitor against hRev1 and hpol lambda (λ). PNR-7-02 acts synergistically with Cisplatin (HY-17394) to kill chronic myeloid leukaemia and ovarian cancer cell lines. PNR-7-02 is an indole thio-barbituric acid (ITBA) derivative with both N-napthoyl moiety and 5-chloro substituent on the indole ring .
    PNR-7-02
  • HY-14184S

    ACT-064992-d4

    Isotope-Labeled Compounds Endothelin Receptor Apoptosis Cardiovascular Disease
    Macitentan-d4 is a deuterium labeled Sulfamethoxazole. Macitentan 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) .
    Macitentan-d4
  • HY-14184R

    ACT-064992 (Standard)

    Reference Standards Endothelin Receptor Apoptosis Cardiovascular Disease Endocrinology Cancer
    Macitentan (Standard) is the analytical standard of Macitentan. This product is intended for research and analytical applications. 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) .
    Macitentan (Standard)
  • HY-19529

    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-RS16219

    Small Interfering RNA (siRNA) Others

    SPP1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for SPP1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

    SPP1 Mouse Pre-designed siRNA Set A
    SPP1 Mouse Pre-designed siRNA Set A
  • HY-P1112

    Endothelin Receptor Cardiovascular Disease Neurological Disease
    Sarafotoxin S6a, 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 elicits the pig coronary artery with an EC50 value of 7.5 nM .
    Sarafotoxin S6a
  • HY-146302
    14-3-3η Protein inhibitor 1
    2 Publications Verification

    Apoptosis Cancer
    14-3-3η Protein inhibitor 1 (Compound C11) is a 14-3-3η protein inhibitor with a KD of 35 µM. 14-3-3η Protein inhibitor 1 shows inhibitory activities against several typical human liver cancer cell lines. 14-3-3η Protein inhibitor 1 induces cell apoptosis and G1-S cell cycle arrest with good metabolic stability .
    14-3-3η Protein inhibitor 1
  • HY-P2496

    Endothelin Receptor Cardiovascular Disease
    Endothelin 1 (swine, human), Alexa Fluor 488-labeled is a synthetic Endothelin 1 peptide labled with Alexa Fluor 488. Endothelin 1 (swine, human) is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. Endothelin 1 acts through two types of receptors ETA and ETB .
    Endothelin 1 (swine, human), Alexa Fluor 488-labeled
  • HY-130326

    Ru(η6-p-cymene)Cl2(pta)

    Apoptosis Caspase Cardiovascular Disease Cancer
    RAPTA-C (Ru(η6-p-cymene)Cl2(pta)) acts as an anti-cancer and anti-angiogenic agent. RAPTA-C exhibits anti-metastatic, anti-angiogenic, and anti-tumoral activities through protein and histone-deoxyribonucleic acid alterations. RAPTA-C exhibits cell growth inhibition by triggering G(2)/M phase arrest in cancer cells. RAPTA-C also enhances the levels of p53 and triggers the mitochondrial Apoptotic pathway, resulting in cytochrome C release and caspase-9 activation. RAPTA-C reduces the growth of tumors with the inhibition of angiogenesis in a ovarian carcinoma model .
    RAPTA-C
  • HY-76520

    IPI 1040; TBC-11251

    Endothelin Receptor TGF-β Receptor Cardiovascular Disease Metabolic Disease
    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 .
    Sitaxsentan
  • HY-121197

    Ophiocordin; Azepinostatin

    MARCKS PKA PKC Others
    Balanol (Ophiocordin; Azepinostatin) is a potent and ATP competitive PKC/PKA inhibitor against human PKC isozymes α, β-I, β-II, γ, δ, ε, η (IC50s=4-9 nM) and ζ (IC50=150 nM). Balanol also blocks the phosphorylation of cyclic AMP response element-binding protein (CREB) and myristoylated alanine-rich C kinase substrate (MARCKS). Balanol can be isolated from the fungus Verticillium balanoides .
    Balanol
  • HY-123744

    Endothelin Receptor Cardiovascular Disease Neurological 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-106994A

    YM598

    Endothelin Receptor Cardiovascular Disease Inflammation/Immunology Cancer
    Nebentan 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 .
    Nebentan potassium
  • HY-135283

    A-216546

    Endothelin Receptor Cardiovascular Disease Endocrinology
    ABT-546 (A-216546), a chemical probe, is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [ 125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively .
    ABT-546
  • HY-13711

    Endothelin Receptor Cardiovascular Disease
    S-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 .
    S-1255
  • HY-118497

    Endothelin Receptor Cardiovascular Disease Metabolic Disease
    BMS 182874 is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research .
    BMS 182874
  • HY-P5885

    PKC Others
    PKCη pseudosubstrate inhibitor,myristoylated is cell permeable and can be used to study the mechanism of action of PKCη .
    PKCη pseudosubstrate inhibitor,myristoylated
  • HY-19210

    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-19263

    Endothelin Receptor Cardiovascular Disease
    BMS-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 .
    BMS-193884
  • HY-153463

    SC0062

    Endothelin Receptor Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology
    Diosuxentan is an inhibitor of ETA. Diosuxentan can be used in research for cardiovascular, renal and neuronal inflammation diseases .
    Diosuxentan
  • HY-10383

    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-19274

    Endothelin Receptor Cardiovascular Disease Endocrinology
    ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.
    ZD-1611
  • HY-135500

    Endothelin Receptor Endocrinology
    ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist .
    ACT-373898
  • HY-105183

    Endothelin Receptor Others
    PD 145065 is a highly potent but non-selective endothelin receptor antagonist with an IC50 value of 4 nM for the ETA receptor for rabbit renal artery vascular smooth muscle cells .
    PD 145065
  • HY-115417

    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-14184A

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
    Macitentan n-butyl analogue

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