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BMS 182874 is an orallyactive, highly selective endothelin receptor(ETAreceptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research .
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 .
BMS-193884 is a selective, orally active, and competitive ETA antagonist with 10000-fold greater affinity for the human ETAreceptor (Ki=1.4 nM) than for the ETBreceptor .
ABT-546 (A-216546) is a potent, highly selective and active endothelin ETAreceptor 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 ETAreceptor than for the ETBreceptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively .
L-749329 ((Rac)-L-754142) is an ETA and ETBreceptor antagonist, with Kis of 0.062 nM and 2.25 nM for ETA and ETB respectively. L-749329 inhibits ET-1-stimulated signaling .
Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETBreceptors 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 ETBreceptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETAreceptor 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 .
ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist .
Edonentan (BMS 207940) hydrate is a potent and selective antagonist of the endothelin A (ETA) receptor, with a Ki of 10 pM. In rats, Edonentan has superior (100%) oral bioavailbility .
Nebentan (YM598 free base) is a potent, selective and orally active non-peptide endothelin ETAreceptor 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 .
Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETAreceptor) with IC50 of 220 nM.
BMS-248360 is a potent and orally active dual antagonist of both angiotensin II receptor (AT1) and endothelin A (ETA)receptor, with Kis of 10 nM and 1.9 nM for hAT1 and hETA receptor, respectively. BMS-248360 displays hypertensive effects .
Bosentan-d4 is the deuterium labeled Bosentan. Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETBreceptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
Ro 46-8443 is the first non-peptide endothelin ETBreceptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ETB (IC50: 34-69 nM) over ETAreceptors (IC50: 6800 nM) .
Edonentan (BMS 207940) is an antagonist for endothelin receptor(ETAreceptor), with a Ki of 10 pM. Edonentan is metabolic stable, exhibits good pharmakokinetic characters in rats. Edonentan regulates the endothelin system, blocks the big Endothelin-induced pressor response in rats model .
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 receptorsETA and ETB .
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 .
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) .
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 receptorsETA 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.
Bosentan (Standard) is the analytical standard of Bosentan. This product is intended for research and analytical applications. Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETBreceptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
Bosentan (hydrate) (Standard) is the analytical standard of Bosentan (hydrate). This product is intended for research and analytical applications. 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.
FR139317 (PD 147953) is a selective ETAreceptor antagonist. FR139317 inhibits cerebral activation by intraventricular endothelin-1 in conscious rats. FR139317 also ameliorates cerebral vasospasm in dogs .
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 ETAreceptors in human neuroblastoma cell line SK-N-MC cells with IC50 of 1300 nM .
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).
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 .
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].
Macitentan (Standard) is the analytical standard of Macitentan. This product is intended for research and analytical applications. 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) .
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 .
BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
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 .
BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
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 receptorsETA and ETB .
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 ETBreceptors with Ki of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension .
BE 24566B is a polyketide fungal metabolite originally isolated from S. violaceusniger. It is active against B. subtilis, B. cereus, S. aureus, M. luteus, E. faecalis, and S. thermophilus (MICs=1.56, 1.56, 1.56, 1.56, 3.13, and 3.13 μg/mL, respectively). BE 24566B is an endothelin (ET) receptor antagonist (IC50s=11 and 3.9 μM for ETA and ETB receptors, respectively).
Asterric acid is an antibiotic fungal metabolite that completely inhibits the binding of the potent vasoconstrictor endothelin (ET)-1 to the ETAreceptor in A10 cells at 0.1 μM.1 Asterric acid derivatives have also been shown to inhibit VEGF-induced tube formation of human umbilical vein endothelial cells at 3-10 μM, which suggests its usefulness as an antiangiogenic agent.
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 .
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 .
GPCRs are a large family of cell surface receptors that respond to a variety of external signals. Binding of a signaling molecule to a GPCR results in G protein activation, which in turn triggers the production of any number of second messengers. GPCRs play an important role in the human body, and increased understanding of these receptors has greatly affected modern medicine. In fact, researchers estimate that between one-third to one-half of all approved drugs act by binding to GPCRs. GPCRs are a large group of drug targets in drug discovery.
MCE provides a unique collection of 2,437 small molecules targeting GPCRs that can be used in the screening for various GPCRs-related research and drug development projects.
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 receptorsETA and ETB .
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 receptorsETA and ETB .
BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
PD 145065 is a highly potent but non-selective endothelin receptor antagonist with an IC50 value of 4 nM for the ETAreceptor for rabbit renal artery vascular smooth muscle cells .
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 .
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 receptorsETA and ETB .
EDNRA Protein, a receptor for endothelin-1, activates a phosphatidylinositol-calcium second messenger system through association with G proteins. Its binding affinities follow the order: ET1 > ET2 >> ET3. Additionally, EDNRA interacts with HDAC7 and KAT5. EDNRA Protein, Human (P.pastoris, His) is the recombinant human-derived EDNRA protein, expressed by P. pastoris , with N-His labeled tag. The total length of EDNRA Protein, Human (P.pastoris, His) is 60 a.a., with molecular weight of ~62 kDa.
DEP-1/CD148 protein is a tyrosine phosphatase that affects multiple targets such as CTNND1, FLT3, PDGFRB, and EGFR, thereby affecting cellular processes such as adhesion, migration, proliferation, and differentiation. DEP-1/CD148 is critical in vascular development, regulating macrophage adhesion, platelet activation, and thrombosis, while negatively regulating cell proliferation and PDGF-stimulated migration. DEP-1/CD148 Protein, Human (341a.a, His) is the recombinant human-derived DEP-1/CD148 protein, expressed by E. coli , with N-His labeled tag.
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].
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