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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
143 Results for "
ETA
" in MedChemExpress (MCE) Product Catalog:
Products (143)
143 Results for "ETA" in MCE Product Catalog:
32
32 Publications Verification
Referencia número: HY-A0013
No. CAS: 147536-97-8
Target:
Áreas de investigación:
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
Referencia número: HY-A0013A
No. CAS: 157212-55-0
Target:
Áreas de investigación:
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.
23
23 Cited Publications
Synonyms: AEB071
Áreas de investigación:
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 .
23
23 Cited Publications
Synonyms: Mallotoxin; NSC 56346; NSC 94525
15
15 Cited Publications
Target:
Áreas de investigación:
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
14 Cited Publications
Synonyms: ACT-064992
Target:
Áreas de investigación:
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
10 Cited Publications
Referencia número: HY-P0202
No. CAS: 117399-94-7
Synonyms: ET-1 (swine, human)
Target:
Áreas de investigación:
10
10 Cited Publications
Referencia número: HY-P0202A
No. CAS: 394693-38-0
Synonyms: ET-1 (swine, human) TFA
Target:
Áreas de investigación:
10
10 Cited Publications
Referencia número: HY-P70499
Pureza: ≥ 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
6
6 Cited Publications
Synonyms: ABT-627; (+)-A 127722; A-147627
Target:
Áreas de investigación:
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:
Áreas de investigación:
Atrasentan hydrochloride (ABT-627 hydrochloride) is a selective endothelin A receptor antagonist with an IC50 of 0.0551 nM for ETA .
5
5 Cited Publications
Referencia número: HY-P78358
Pureza: ≥ 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
4
4 Cited Publications
Target:
Áreas de investigación:
4
4 Cited Publications
Synonyms: AKB-9778
Target:
Áreas de investigación:
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) .
3
3 Cited Publications
Synonyms: ACT-132577
Target:
Áreas de investigación:
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 .
3
3 Cited Publications
Referencia número: HY-P71786
Pureza: ≥ 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:
Source:
2
2 Cited Publications
Synonyms: Indolactam V
(-)-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.
2
2 Cited Publications
Target:
Áreas de investigación:
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 .
2
2 Cited Publications
Target:
Áreas de investigación:
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
2 Cited Publications
Synonyms: IPI 1040 sodium; TBC11251 sodium
Target:
Áreas de investigación:
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 .
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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
