2. Signaling Pathways
  3. GPCR/G Protein
  4. Endothelin Receptor
  5. Endothelin Receptor Inhibitor

Endothelin Receptor Inhibitor

Endothelin Receptor Isoform Comparison

Endothelin Receptor Inhibitors (15):

Cat. No. Product Name Effect Purity
  • HY-P991964
    Rendomab B4
    		Inhibitor
    Rendomab B4 (Rendomab-B49) is a monoclonal antibody targeting ETB. Rendomab B4 preferentially binds to ETB in the active conformational state and exhibits selectivity for ETB on melanoma cells. Rendomab B4 inhibits the G protein-dependent phospholipase C (PLC) pathway, blocks ET-3-induced Gαi/o-mediated inhibition of adenylate cyclase, and does not affect the activation of the ERK1/2 pathway. Rendomab B4 is applicable to melanoma-related research.
  • HY-P1236
    Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse
    		Inhibitor 99.55%
    Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
  • HY-P1235A
    Carperitide acetate
    		Inhibitor 99.78%
    Carperitide acetate (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine acetate) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide acetate inhibits endothelin-1 secretion in a dose-dependent way.
  • HY-15404
    Darusentan
    		Inhibitor 98.60%
    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.
  • HY-N7543
    Schisantherin D
    		Inhibitor 99.66%
    Schisantherin D is a lignan. Schisantherin D can be isolated from Kadsura interior. Schisantherin D downregulates the expression of ETBR and inhibits the secretion of ECM and ET-1. Schisantherin D alleviates EtOH + ET-1-induced hepatocyte cytotoxicity. Schisantherin D potently inhibits HIV replication in cells.
  • HY-P1236A
    Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse TFA
    		Inhibitor 99.32%
    Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse (TFA) is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
  • HY-P4641
    H-Trp-Phe-OH
    		Inhibitor 99.87%
    H-Trp-Phe-OH (Trp-Phe) is an ACE inhibitor and endothelial function regulator, with an ACE IC50 of 0.318 mg/mL. H-Trp-Phe-OH increases nitric oxide concentration, reduces endothelin-1 (ET-1) levels, and reverses norepinephrine-mediated endothelial cell dysfunction. H-Trp-Phe-OH exhibits antihypertensive activity. H-Trp-Phe-OH can be used in studies related to hypertension and atherosclerosis.
  • HY-P1235
    Carperitide
    		Inhibitor
    Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) inhibits endothelin-1 secretion in a dose-dependent way.
  • HY-153463
    Diosuxentan
    		Inhibitor
    Diosuxentan is an inhibitor of ETA. Diosuxentan can be used in research for cardiovascular, renal and neuronal inflammation diseases.
  • HY-P990573
    DEDN6526A Antibody
    		Inhibitor
    DEDN6526A (RG-7636) is a humanized antibody expressed in CHO cells, targeting ETBR. DEDN6526A (RG-7636) has a huIgG1 type heavy chain and a huκ type light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for DEDN6526A (RG-7636) can be referenced as Human IgG1 kappa, Isotype Control (HY-P99001).
  • HY-13711
    S-1255
    		Inhibitor
    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.
  • HY-105362
    PD 155080
    		Inhibitor
    PD 155080 is a selective endothelin A receptor (ETA receptor) antagonist. PD 155080 reduces coronary resistance in the isolated rat heart model. PD 155080 improves myocardial systolic function and diastolic function in the ischemia/reperfusion model. PD 155080 can be used for the study of cardiovascular diseases.
  • HY-114674
    A-127722
    		Inhibitor
    A-127722 is A 2, 4-dialarylpyrrolidine-3-carboxylic acid ETA selective endothelin receptor (ET receptor) antagonist with IC50 value of 0.36 nM.
  • HY-11103R
    Sitaxsentan sodium (Standard)
    		Inhibitor
    Sitaxsentan (sodium) (Standard) is the analytical standard of Sitaxsentan sodium (IPI 1040 sodium; TBC11251 sodium) (HY-11103). This product is intended for research and analytical applications. Sitaxsentan 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.
  • HY-19890
    Aminaftone
    		Inhibitor
    Aminaftone, a derivative of 4-aminobenzoic acid, downregulates endothelin-1 (ET-1) production in vitro by interfering with the transcription of the pre-pro-ET-1 gene.