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

ETB

 
Cat. No. Product Name Effect Purity
  • HY-P0202
    Endothelin 1 (swine, human)
    		Activator 99.12%
    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.
  • HY-14184
    Macitentan
    		Antagonist 99.87%
    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).
  • HY-15894A
    BQ-788
    		Antagonist 99.70%
    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.
  • HY-15895
    Aprocitentan
    		Antagonist 99.55%
    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.
  • HY-11103
    Sitaxsentan sodium
    		Antagonist 98.83%
    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.
  • HY-183141
    HJP 272
    HJP 272 is a selective endothelin peptide A (ETA) receptor antagonist with an IC50 of 37.01 nM. . HJP 272 can be used for the researches of pulmonary arterial hypertension, fibrosis, renal failure and cancer.
  • HY-15894
    BQ-788 sodium salt
    		Antagonist 99.33%
    BQ-788 sodium salt is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells.
  • HY-B0323
    Sulfisoxazole
    		Antagonist 99.90%
    Sulfisoxazole (Sulfafurazole) is an orally active endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole is a sulfonamide antibacterial agent with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A.
  • HY-16465A
    IRL-1620 TFA
    		Agonist 98.73%
    IRL-1620 (TFA) is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM.
  • HY-114367
    Delphinidin 3-rutinoside chloride
    		Activator 98.83%
    Delphinidin 3-rutinoside chloride is an anthocyanin component. Delphinidin 3-rutinoside chloride is isolable from the fruits of blackcurrant Ribes nigrum L. Delphinidin 3-rutinoside chloride activates the ETB receptor and stimulates the NO/cGMP pathway. Delphinidin 3-rutinoside chloride increases cyclic guanosine monophosphate production and reduces the phosphorylation level of Myosin regulatory light chain. Delphinidin 3-rutinoside chloride stimulates GLP-1 secretion. It significantly induces relaxation of bovine ciliary muscle strips contracted by ET-1 and inhibits ET-1-induced contraction of bovine ciliary muscle strips. Delphinidin 3-rutinoside chloride is applicable to research related to type 2 diabetes.
  • HY-16465
    IRL-1620
    		Agonist 99.69%
    IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM.
  • HY-103460
    IRL 2500
    		Antagonist 99.27%
    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.
  • HY-17351
    Tezosentan
    		Antagonist 98.27%
    Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.
  • HY-120295
    A-192621
    		Antagonist 99.92%
    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.
  • 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-15895S
    Aprocitentan-d4
    		Antagonist 98.76%
    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.
  • HY-P1112
    Sarafotoxin S6a
    		Agonist 98.45%
    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.
  • HY-19431
    Ro 46-8443
    		Antagonist 98.93%
    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).
  • HY-14184S
    Macitentan-d4
    		Antagonist
    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).
  • HY-106994
    Nebentan
    		Antagonist 99.67%
    Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan 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.
Cat. No. Product Name / Synonyms Species Source