151 Results for "

ETA

" in MedChemExpress (MCE) Product Catalog:
Products (151)

151 Results for "ETA" in MCE Product Catalog:

33
33 Publications Verification
Art. -Nr.: HY-A0013
CAS. Nr.: 147536-97-8
Target:  

Endothelin Receptor

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.
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33
33 Publications Verification
Art. -Nr.: HY-A0013A
CAS. Nr.: 157212-55-0
Target:  

Endothelin Receptor

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.
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28
28 Cited Publications
Art. -Nr.: HY-18980
CAS. Nr.: 82-08-6
Synonyms: Mallotoxin; NSC 56346; NSC 94525
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 .
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24
24 Cited Publications
Art. -Nr.: HY-10343
CAS. Nr.: 425637-18-9
Reinheit:  99.79%
Synonyms: AEB071
Target:  

MARCKS PKC

Forschungsgebiete:  

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 .
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16
16 Cited Publications
Art. -Nr.: HY-15894A
CAS. Nr.: 173326-37-9
Reinheit:  98.66%
Target:  

Endothelin Receptor

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 .
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14
14 Cited Publications
Art. -Nr.: HY-14184
CAS. Nr.: 441798-33-0
Reinheit:  99.85%
Synonyms: ACT-064992
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) .
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10
10 Cited Publications
Art. -Nr.: HY-P0202
CAS. Nr.: 117399-94-7
Synonyms: ET-1 (swine, human)
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 .
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10
10 Cited Publications
Art. -Nr.: HY-P0202A
CAS. Nr.: 394693-38-0
Synonyms: ET-1 (swine, human) TFA
Target:  

Endothelin Receptor

Forschungsgebiete:  

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 .
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10
10 Cited Publications
Art. -Nr.: HY-P70499
Reinheit:  ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: SPP1; Uropontin; Prev. BNSP; Osteopontin/Immunoglobulin Alpha 1 Heavy Chain Constant Region Fusion Protein; Prev. OPN; CDNA FLJ54682, Highly Similar To Osteopontin; Osteopontin; Secreted Phosphoprotein 1 Variant 6; Lnc-PKD2-2-3; Bone Sialoprotein I; ETA-1; SPP1/CALPHA1 Fusion; BSPI; Bone Sialoprotein 1; Early T-Lymphocyte Activation 1; SPP-1; Urinary Stone Protein; Opn; Nephropontin; Secreted Phosphoprotein 1; Secreted Phosphoprotein 1 (Osteopontin, Bone Sialoprotein I, Early T-Lymphocyte Activation 1)
Species:  
Human
Source:  
HEK293
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8
8 Cited Publications
Art. -Nr.: HY-P78358
Reinheit:  ≥ 95%, as determined by reducing SDS-PAGE or Bis-Tris PAGE.
Synonyms: SPP1; Uropontin; Prev. BNSP; Osteopontin/Immunoglobulin Alpha 1 Heavy Chain Constant Region Fusion Protein; Prev. OPN; CDNA FLJ54682, Highly Similar To Osteopontin; Osteopontin; Secreted Phosphoprotein 1 Variant 6; Lnc-PKD2-2-3; Bone Sialoprotein I; ETA-1
Species:  
Mouse
Source:  
HEK293
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7
7 Cited Publications
Art. -Nr.: HY-15403
CAS. Nr.: 173937-91-2
Reinheit:  99.58%
Synonyms: ABT-627; (+)-A 127722; A-147627
Target:  

Endothelin Receptor

Atrasentan (ABT-627) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA .
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7
7 Cited Publications
Art. -Nr.: HY-15403A
CAS. Nr.: 195733-43-8
Reinheit:  99.82%
Synonyms: ABT-627 hydrochloride; (+)-A 127722 hydrochloride; A-147627 hydrochloride
Target:  

Endothelin Receptor

Atrasentan hydrochloride (ABT-627 hydrochloride) is a selective endothelin A receptor antagonist with an IC50 of 0.0551 nM for ETA .
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4
4 Cited Publications
Art. -Nr.: HY-12378
CAS. Nr.: 136553-81-6
Reinheit:  99.82%
Target:  

Endothelin Receptor

Forschungsgebiete:  

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 .
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4
4 Cited Publications
Art. -Nr.: HY-109041
CAS. Nr.: 1008510-37-9
Reinheit:  ≥98.0%
Synonyms: AKB-9778
Target:  

Phosphatase Tie

Forschungsgebiete:  

Inflammation/Immunology

Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM) .
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4
4 Cited Publications
Art. -Nr.: HY-109041A
CAS. Nr.: 1809275-69-1
Synonyms: AKB-9778 sodium
Target:  

Phosphatase Tie

Forschungsgebiete:  

Inflammation/Immunology

Razuprotafib (AKB-9778) sodium is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib sodium promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib sodium inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib sodium shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM) .
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4
4 Cited Publications
Art. -Nr.: HY-P71786
Reinheit:  ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: SPP1; Uropontin; Prev. BNSP; Osteopontin/Immunoglobulin Alpha 1 Heavy Chain Constant Region Fusion Protein; Prev. OPN; CDNA FLJ54682, Highly Similar To Osteopontin; Osteopontin; Secreted Phosphoprotein 1 Variant 6; Lnc-PKD2-2-3; Bone Sialoprotein I; ETA-1
Species:  
Mouse
Source:  
P. pastoris
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3
3 Cited Publications
Art. -Nr.: HY-15895
CAS. Nr.: 1103522-45-7
Reinheit:  99.98%
Synonyms: ACT-132577
Target:  

Endothelin Receptor

Forschungsgebiete:  

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 .
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2
2 Cited Publications
Art. -Nr.: HY-12307
CAS. Nr.: 90365-57-4
Reinheit:  98.42%
Synonyms: Indolactam V
Target:  

PKC

Forschungsgebiete:  

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.
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2
2 Cited Publications
Art. -Nr.: HY-17352
CAS. Nr.: 180384-56-9
Synonyms: Ro 61-1790; VML 588; AXV-034343
Target:  

Endothelin Receptor

Forschungsgebiete:  

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 .
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2
2 Cited Publications
Art. -Nr.: HY-146302
CAS. Nr.: 2770842-10-7
Reinheit:  99.00%
Forschungsgebiete:  

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 .
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