Endothelin Receptor Inhibitor

RES-701-3 peptide TFA is a class II lasso peptide. RES-701-3 peptide TFA can be isolated from the fermentation broth of Streptomyces species. RES-701-3 peptide TFA potently inhibits the binding of ET-1 to ET_B, with an IC₅₀ of approximately 5-10 nM. RES-701-3 peptide TFA is applicable to research related to systemic hypertension, myocardial infarction, and myocardial ischemia.

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.

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.

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.

Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a K_i of 1.4 nM to the ET-A receptor and a K_i 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 K_i of 13 nM.

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.

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.

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.

SM19712 is an orally active, selective endothelin converting enzyme (ECE) inhibitor. SM19712 inhibits conversion of big ET-1 to ET-1. SM19712 attenuates colonic angiogenesis, tissue injury, inflammation, without altering colon shortening or myeloperoxidase levels in mice. SM19712 can be used for the research of inflammatory bowel disease (colitis), ischemic acute renal failure, acute myocardial infarction, and myocardial ischemia/reperfusion injury.

Diosuxentan is an inhibitor of ET_A. Diosuxentan can be used in research for cardiovascular, renal and neuronal inflammation diseases.

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).

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.

S-1255 is an orally active and highly selective endothelin ETA receptor antagonist (K_d=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.

PD 155080 is a selective endothelin A receptor (ET_A 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.

SM19712 free acid is an orally active, selective endothelin converting enzyme (ECE) inhibitor. SM19712 free acid inhibits conversion of big ET-1 to ET-1. SM19712 free acid attenuates colonic angiogenesis, tissue injury, inflammation, without altering colon shortening or myeloperoxidase levels in mice. SM19712 free acid can be used for the research of inflammatory bowel disease (colitis), ischemic acute renal failure, acute myocardial infarction, and myocardial ischemia/reperfusion injury.

A-127722 is A 2, 4-dialarylpyrrolidine-3-carboxylic acid ET_A selective endothelin receptor (ET receptor) antagonist with IC₅₀ value of 0.36 nM.

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 K_i 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.

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.