From 11:00 pm to 12:00 pm EST ( 8:00 pm to 9:00 pm PST ) on January 6th, the website will be under maintenance. We are sorry for the inconvenience. Please arrange your schedule properly.
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) .
Endothelin 1 (swine, human) (TFA) 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 .
Endothelin 1 (swine, human), Alexa Fluor 488-labeled is a synthetic Endothelin 1 peptide labled with Alexa Fluor 488. Endothelin 1 (swine, human) 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 .
BQ-3020 is a selective endothelin receptor(ETB receptor) agonist that displaces [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research 12.
BQ-3020 ammonium is a selective endothelin receptor(ETB receptor) agonist. BQ-3020 ammonium inhibits [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 ammonium elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 ammonium makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research . .
Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively[1].
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) .
[Ala1,3,11,15]-Endothelin (53-63) is an ETB agonist. [Ala1,3,11,15]-Endothelin (53-63) has selectivity for ET B with IC50 values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) can be used for the research of vasoconstriction
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)[1].
[Ala1,3,11,15]-Endothelin (53-63) (TFA) is an ETB agonist. [Ala1,3,11,15]-Endothelin (53-63) (TFA) has selectivity for ET B with IC50 values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) (TFA) can be used for the research of vasoconstriction .
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 .
SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
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 .
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.
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.
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 .
ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist .
Bosentan-d4 is the deuterium labeled Bosentan. 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.
Endothelin 1 (swine, human) 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 .
BMS-193884 is a selective, orally active, and competitive ETA antagonist with 10000-fold greater affinity for the human ETA receptor (Ki=1.4 nM) than for the ETB receptor .
PD 156252 is a hexapeptide that is a highly potent endothelin (ET) antagonist. PD 156252 has enhanced binding affinity for rabbit ETA and rat ETB receptor subtypes with IC50 values of 1.0 and 40 nM, respectively.
Macitentan n-butyl analogue is a n-butyl analogue of Macitentan. Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
Aprocitentan (ACT-132577) is the major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively .
Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research .
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 .
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 .
Sarafotoxin S6a TFA , 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 TFA elicits the pig coronary artery with an EC50 value of 7.5 nM .
Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver . 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. Bosentan can be used in treatment of pulmonary arterial hypertension .
Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium 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 .
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 .
A-192621 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 .
ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [ 125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively .
Endothelin 1 (swine, human) (TFA) 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 .
BQ-3020 ammonium is a selective endothelin receptor(ETB receptor) agonist. BQ-3020 ammonium inhibits [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 ammonium elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 ammonium makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research . .
Endothelin 1 (swine, human), Alexa Fluor 488-labeled is a synthetic Endothelin 1 peptide labled with Alexa Fluor 488. Endothelin 1 (swine, human) 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 .
BQ-3020 is a selective endothelin receptor(ETB receptor) agonist that displaces [ 125I] ET-1 binding to ETB receptors, with an IC50 value of 0.2 nM. BQ-3020 elicits vasoconstriction in the rabbit pulmonary artery. BQ-3020 makes relaxation of the pig urinary bladder neck and can be used for cardiovascular disease research 12.
[Ala1,3,11,15]-Endothelin (53-63) is an ETB agonist. [Ala1,3,11,15]-Endothelin (53-63) has selectivity for ET B with IC50 values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) can be used for the research of vasoconstriction
[Ala1,3,11,15]-Endothelin (53-63) (TFA) is an ETB agonist. [Ala1,3,11,15]-Endothelin (53-63) (TFA) has selectivity for ET B with IC50 values range from 0.33 nM to 0.61 nM. [Ala1,3,11,15]-Endothelin (53-63) (TFA) can be used for the research of vasoconstriction .
Endothelin 1 (swine, human) 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 .
PD 156252 is a hexapeptide that is a highly potent endothelin (ET) antagonist. PD 156252 has enhanced binding affinity for rabbit ETA and rat ETB receptor subtypes with IC50 values of 1.0 and 40 nM, respectively.
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 .
Sarafotoxin S6a TFA , 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 TFA elicits the pig coronary artery with an EC50 value of 7.5 nM .
EDNRB/Endothelin R Type B Protein, a non-specific receptor for endothelin 1, 2, and 3, activates a phosphatidylinositol-calcium second messenger system through G proteins. This mechanism underscores its pivotal role in mediating cellular responses initiated by endothelin neuropeptides, emphasizing the versatility of EDNRB in transducing signals for various physiological processes. EDNRB/Endothelin R Type B Protein, Human (HEK293, His) is the recombinant human-derived EDNRB/Endothelin R Type B protein, expressed by HEK293 , with C-His labeled tag. The total length of EDNRB/Endothelin R Type B Protein, Human (HEK293, His) is 75 a.a., with molecular weight of ~9.5 kDa.
EDNRB/Endothelin R Type B Protein, a non-specific receptor for endothelin 1, 2, and 3, activates a phosphatidylinositol-calcium second messenger system through G proteins. This mechanism underscores its pivotal role in mediating cellular responses initiated by endothelin neuropeptides, emphasizing the versatility of EDNRB in transducing signals for various physiological processes. EDNRB/Endothelin R Type B Protein, Human (HEK293, Fc) is the recombinant human-derived EDNRB/Endothelin R Type B protein, expressed by HEK293, with C-mFc labeled tag. The total length of EDNRB/Endothelin R Type B Protein, Human (HEK293, Fc) is 75 a.a., with molecular weight of ~47.5 & 43.7 kDa, respectively.
Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively[1].
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)[1].