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Results for "

ETB receptor

" in MedChemExpress (MCE) Product Catalog:

55

Inhibitors & Agonists

12

Peptides

2

Natural
Products

2

Isotope-Labeled Compounds

2

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P0202
    Endothelin 1 (swine, human)
    Maximum Cited Publications
    8 Publications Verification

    ET-1 (swine, human)

    		 Endothelin Receptor Metabolic Disease Inflammation/Immunology
    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 .
    Endothelin 1 (swine, human)
  • HY-A0013
    Bosentan
    Maximum Cited Publications
    30 Publications Verification

    		 Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    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
  • HY-14184
    Macitentan
    10+ Cited Publications

    ACT-064992

    		 Endothelin Receptor Apoptosis Cardiovascular Disease Endocrinology Cancer
    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) .
    Macitentan
  • HY-11103
    Sitaxsentan sodium
    2 Publications Verification

    IPI 1040 sodium; TBC11251 sodium

    		 Endothelin Receptor TGF-β Receptor Cardiovascular Disease Metabolic Disease
    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 .
    Sitaxsentan sodium
  • HY-15894A
    BQ-788
    10+ Cited Publications

    		 Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    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 .
    BQ-788
  • HY-10088
    Zibotentan
    1 Publications Verification

    ZD4054

    		 Endothelin Receptor Apoptosis Endocrinology Cancer
    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 .
    Zibotentan
  • HY-15894
    BQ-788 sodium salt
    10+ Cited Publications

    		 Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    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 .
    BQ-788 sodium salt
  • HY-A0013A
    Bosentan hydrate
    Maximum Cited Publications
    30 Publications Verification

    		 Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    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.
    Bosentan hydrate
  • HY-16465
    IRL-1620
    1 Publications Verification

    		 Endothelin Receptor Neurological Disease Endocrinology
    IRL-1620 is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM.
    IRL-1620
  • HY-114367
    Delphinidin 3-rutinoside chloride
    1 Publications Verification

    Delphinidin 3-O-rutinoside chloride

    		 Endothelin Receptor NO Synthase Myosin GLP Receptor Neurological Disease Metabolic Disease
    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 .
    Delphinidin 3-rutinoside chloride
  • HY-103460
    IRL 2500

    		Endothelin Receptor Cardiovascular Disease
    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 .
    IRL 2500
  • HY-17351
    Tezosentan

    RO 610612

    		 Endothelin Receptor Cardiovascular Disease Neurological Disease Endocrinology Cancer
    Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.
    Tezosentan
  • HY-15195
    Avosentan

    Ro 67-0565; SPP-301

    		 Endothelin Receptor Cardiovascular Disease Endocrinology
    Avosentan (Ro 67-0565; SPP-301) is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks ETB receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure .
    Avosentan
  • HY-120295
    A-192621
    2 Publications Verification

    		 Endothelin Receptor Apoptosis Cardiovascular Disease Endocrinology
    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 .
    A-192621
  • HY-19431
    Ro 46-8443

    		Endothelin Receptor Cardiovascular Disease
    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) .
    Ro 46-8443
  • HY-15404
    Darusentan

    Lu-135252

    		 Endothelin Receptor Cardiovascular Disease Endocrinology
    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 .
    Darusentan
  • HY-16465A
    IRL-1620 TFA
    1 Publications Verification

    		 Endothelin Receptor Cardiovascular Disease Neurological Disease Endocrinology
    IRL-1620 (TFA) is a potent and selective endothelin receptor type B (ETB) agonist with a Ki of 16 pM .
    IRL-1620 TFA
  • HY-P0202A
    Endothelin 1 (swine, human) TFA
    Maximum Cited Publications
    8 Publications Verification

    ET-1 (swine, human) TFA

    		 Endothelin Receptor Cardiovascular Disease
    Endothelin 1 (swine, human) (ET-1) TFA is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. Endothelin 1 TFA acts through two types of receptors ETA and ETB .
    Endothelin 1 (swine, human) TFA
  • HY-14184S
    Macitentan-d4

    ACT-064992-d4

    		 Isotope-Labeled Compounds Endothelin Receptor Apoptosis Cardiovascular Disease
    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) .
    Macitentan-d4
  • HY-14184R
    Macitentan (Standard)

    ACT-064992 (Standard)

    		 Reference Standards Endothelin Receptor Apoptosis Cardiovascular Disease Endocrinology Cancer
    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) .
    Macitentan (Standard)
  • HY-P1112
    Sarafotoxin S6a

    		Endothelin Receptor Cardiovascular Disease Neurological Disease
    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
  • HY-P1016B
    BQ-3020 ammonium

    		Endothelin Receptor Cardiovascular Disease
    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 . .
    BQ-3020 ammonium
  • HY-P2496
    Endothelin 1 (swine, human), Alexa Fluor 488-labeled

    		Endothelin Receptor Fluorescent Dye NF-κB COX Prostaglandin Receptor Apoptosis TNF Receptor Interleukin Related MMP Cardiovascular Disease Inflammation/Immunology Cancer
    Endothelin 1 (swine, human), Alexa Fluor 488-labeled is an Endothelin-1 conjugated with Alexa Fluor 488 (HY-D1304). Endothelin-1 is an endogenous vasoconstrictor and agonist of ETA/ETB receptor. Endothelin 1 (swine, human) exerts effects including promoting mitosis, angiogenesis, tumor invasion and metastasis, and inhibiting apoptosis. Endothelin 1 (swine, human) induces inflammation and oxidative stress by activating the NF-κB pathway. Endothelin 1 (swine, human), Alexa Fluor 488-labeled is specifically designed for fluorescence imaging, flow cytometry or receptor localization studies, and can be used in research related to sepsis, atherosclerosis, systemic inflammatory response syndrome, cancer and congestive heart failure .
    Endothelin 1 (swine, human), Alexa Fluor 488-labeled
  • HY-76520
    Sitaxsentan

    IPI 1040; TBC-11251

    		 Endothelin Receptor TGF-β Receptor Cardiovascular Disease Metabolic Disease
    Sitaxsentan (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 exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .
    Sitaxsentan
  • HY-P1016
    BQ-3020

    		Endothelin Receptor Cardiovascular Disease
    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 1 2.
    BQ-3020
  • HY-P5769
    Endothelin (16-21)

    		Endothelin Receptor Cardiovascular Disease
    Endothelin (16-21) is a selective ETB receptor agonist (EC50=228 nM in guinea-pig bronchus). Endothelin (16-21) can induce smooth muscle contraction. Endothelin (16-21) is promising for research of respiratory (e.g., asthma) and cardiovascular (e.g., hypertension) diseases .
    Endothelin (16-21)
  • HY-123744
    PD-156707

    		Endothelin Receptor Cardiovascular Disease Neurological Disease
    PD-156707 is an orally active, nonpeptide and selective Endothelin-A receptor antagonist. PD-156707 binds to human ET-A and ET-B receptors with Ki values of 0.17 nM and 133.8 nM, respectively. PD-156707 shows reversal of established chronic hypoxic pulmonary hypertension in rats. PD-156707 can be used for the study of diseases associated with abnormal ET-A receptor activation, particularly pulmonary hypertension, stroke, and heart failure .
    PD-156707
  • HY-106994A
    Nebentan potassium

    YM598

    		 Endothelin Receptor Cardiovascular Disease Inflammation/Immunology Cancer
    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 potassium
  • HY-10383
    J-104132

    		Endothelin Receptor Cardiovascular Disease Metabolic Disease
    J-104132 (L-753037) is a potent, orally active, selective and competitive ETA/ETB receptor antagonist with Ki of 0.034 nM for ETA and 0.104 nM for ETB receptors. J-104132 inhibits Endothelin-1 (ET-1) (HY-P71446)-induced signaling and vascular contractions in vitro. J-104132 alleviates hypertension, vascular remodeling, and diabetic endothelial dysfunction in vivo by dual ETA/ETB blockade. J-104132 can be used for research on diabetic vascular complications [1][3].
    J-104132
  • HY-135500
    ACT-373898

    		Endothelin Receptor Endocrinology
    ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist .
    ACT-373898
  • HY-19263
    BMS-193884

    		Endothelin Receptor Cardiovascular Disease
    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 .
    BMS-193884
  • HY-115417
    Bosentan-d4

    		Endothelin Receptor Cardiovascular Disease Endocrinology
    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.
    Bosentan-d4
  • HY-14184A
    Macitentan n-butyl analogue

    		Endothelin Receptor Cardiovascular Disease Endocrinology
    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).
    Macitentan n-butyl analogue
  • HY-124234
    TA-0201

    		Endothelin Receptor Cardiovascular Disease
    TA-0201 is a novel orally active, competitive, non-peptide endothelin receptor antagonist. TA-0201 antagonizes the specific binding of [ 125I]ET-1 to cloned human receptors of ETA and ETB with Ki values of 15 pM and 41 nM, respectively. TA-0201 inhibits the pressor response to the exogenous big ET-1 .
    TA-0201
  • HY-135283
    ABT-546

    A-216546

    		 Endothelin Receptor Cardiovascular Disease Endocrinology
    ABT-546 (A-216546), a chemical probe, 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 .
    ABT-546
  • HY-19210
    SB-209670

    		Endothelin Receptor Cardiovascular Disease
    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 .
    SB-209670
  • HY-117644
    L-749329

    (Rac)-L-754142

    		 Endothelin Receptor Cardiovascular Disease
    L-749329 ((Rac)-L-754142) is an ETA and ETB receptor antagonist, with Kis of 0.062 nM and 2.25 nM for ETA and ETB respectively. L-749329 inhibits ET-1-stimulated signaling .
    L-749329
  • HY-P10135
    RES-701-1

    		Endothelin Receptor Cardiovascular Disease
    RES-701-1 is a cyclic peptide composed of 16 common L-amino acids, acting as a specific antagonist for the ETB receptor. RES-701-1 can inhibit the binding of 125I-ET-1 (125I-labeled Endothelin (ET)-1) to the ETB receptor, with an IC50 value of 10 nM .
    RES-701-1
  • HY-157658
    K-8794

    		Endothelin Receptor Cardiovascular Disease
    K-8794 is an orally active selective endothelin receptor ETB antagonist that can be used in research on cardiovascular diseases .
    K-8794
  • HY-P10151
    PD 156252

    		Endothelin Receptor Cardiovascular Disease
    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.
    PD 156252
  • HY-A0013AR
    Bosentan hydrate (Standard)

    		Reference Standards Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    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.
    Bosentan hydrate (Standard)
  • HY-N5170
    Aselacin A

    		Endothelin Receptor Cardiovascular Disease
    Aselacin A targets endothelin-1 receptor (ET-1 receptor), inhibits the the binding of ET-1 to ETA receptor and ETB receptor. Aselacin A inhibits the ET-1 binding to bovine atrial membrane and porcine cerebral membrane with IC50 of 22 μg/mL and 20 μg/mL. Aselacin A can be used for research of cardiovascular diseases .
    Aselacin A
  • HY-15195R
    Avosentan (Standard)

    Ro 67-0565 (Standard); SPP-301 (Standard)

    		 Reference Standards Endothelin Receptor Cardiovascular Disease Endocrinology
    Avosentan (Standard) is the analytical standard of Avosentan (HY-15195). This product is intended for research and analytical applications. Avosentan is an orally active endothelin (ETA) receptor antagonist. Avosentan can block the ETA receptor, thereby reducing vascular contraction, and exerting a renal protective effect. Avosentan inhibits vascular contraction caused by ET-1 and alleviates the reduction in retinal and optic nerve head blood flow induced by it, lowering intraocular pressure in the glaucoma monkey model. Avosentan non-specifically blocks ETB receptors at high doses, inhibiting ETB-mediated diuresis and natriuresis, and may cause fluid retention. Avosentan can be used to reduce proteinuria with diabetic nephropathy, but induces significant fluid overload and congestive heart failure.
    Avosentan (Standard)
  • HY-P1112A
    Sarafotoxin S6a TFA

    		Endothelin Receptor Cardiovascular Disease Neurological Disease
    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 .
    Sarafotoxin S6a TFA
  • HY-10088R
    Zibotentan (Standard)

    ZD4054 (Standard)

    		 Reference Standards Endothelin Receptor Apoptosis Endocrinology Cancer
    Zibotentan (Standard) is the analytical standard of Zibotentan. This product is intended for research and analytical applications. 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 .
    Zibotentan (Standard)
  • HY-106994
    Nebentan

    YM598 free base

    		 Endothelin Receptor Cardiovascular Disease Inflammation/Immunology Cancer
    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 .
    Nebentan
  • HY-135390
    Hydroxy desmethyl Bosentan

    Ro 64-1056

    		 Drug Metabolite Cardiovascular Disease
    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 .
    Hydroxy desmethyl Bosentan
  • HY-W781265
    BE 24566B

    L-755,805

    		 Endothelin Receptor Bacterial Infection
    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).
    BE 24566B
  • HY-11103R
    Sitaxsentan sodium (Standard)

    IPI 1040 sodium (Standard); TBC11251 sodium (Standard)

    		 Endothelin Receptor Reference Standards TGF-β Receptor Cardiovascular Disease Metabolic Disease
    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 .
    Sitaxsentan sodium (Standard)
  • HY-76520S
    Sitaxsentan-13C6

    IPI 1040-13C6 ; TBC-11251-13C6

    		 Isotope-Labeled Compounds Endothelin Receptor TGF-β Receptor Cardiovascular Disease Metabolic Disease
    Sitaxsentan- 13C6 (IPI 1040- 13C6) is 13C labeled Sitaxsentan (HY-76520). Sitaxsentan (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 exhibits an IC50 for the ETB receptor of as high as 9800 nM. Sitaxsentan is metabolized by CYP2C9 and CYP3A4, normalizes shunt-induced endothelial abnormalities, restores BMPR signaling, and suppresses pulmonary vascular remodeling and hemodynamic deterioration. Sitaxsentan can be applied in the research of pulmonary arterial hypertension and portopulmonary hypertension .
    Sitaxsentan-13C6

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