Search Result
Results for "
endothelin A
" in MedChemExpress (MCE) Product Catalog:
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P2538
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- HY-105362
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Endothelin Receptor
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Cardiovascular Disease
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PD 155080 is a selective endothelin A receptor (ETA 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 .
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- HY-P2539
-
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Vasopressin Receptor
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Cardiovascular Disease
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Big Endothelin-1 (1-39), porcine is the precursor of endothelin-1. Endothelin-1 (ET-1) is a potent vasopressor peptide. Big Endothelin-1 (1-39), porcine has similar pressor effects in vivo .
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- HY-P3615
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-
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- HY-10282
-
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Endothelin Receptor
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Others
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Daglutril is a compound with the potential to regulate cytokine-induced endothelin-1 production in astrocytes. In studies, it has an inhibitory effect on the production of endothelin-1 induced by some cytokines and can be used as a tool to screen compounds that inhibit endothelin-1 production in astrocytes.
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- HY-P5130
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Endothelin Receptor
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Cardiovascular Disease
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Big endothelin-1 (rat 1-39) is a 39-residues peptide. Big endothelin-1 (rat 1-39) induces diuretic and natriuretic response in conscious Sprague-Dawley rats. Big endothelin-1 (rat 1-39) raises blood pressure in mice .
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- HY-P3610
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Endothelin Receptor
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Others
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[Ala18] Endothelin-1, human is a biologically active peptide. [Ala18] Endothelin-1, human can be used for the research of various biochemical studies.
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-
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- HY-P4159
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ERK
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Cardiovascular Disease
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Endothelin-1 (1-31) (Human) is a potent vasoconstrictor and hypertensive agent. Endothelin-1 (1-31) (Human) is derived from the selective hydrolysis of big ET-1 by chymase .
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- HY-P0207
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endothelin-2 (human, canine); Human endothelin-2
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Endothelin Receptor
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Cardiovascular Disease
Cancer
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Endothelin-2 (49-69), human (Endothelin-2 (human, canine)) is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.
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- HY-P4159B
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ERK
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Cardiovascular Disease
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Endothelin-1 (1-31) (Human) acetate is a potent vasoconstrictor and hypertensive agent. Endothelin-1 (1-31) (Human) acetate is derived from the selective hydrolysis of big ET-1 by chymase .
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- HY-P1019
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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[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
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- HY-P4159A
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ERK
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Cardiovascular Disease
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Endothelin-1 (1-31) (Human) TFA is a potent vasoconstrictor and hypertensive agent. Endothelin-1 (1-31) (Human) TFA is derived from the selective hydrolysis of big ET-1 by chymase .
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- HY-P0207A
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endothelin-2 (49-69) (human, canine) TFA; Human endothelin-2 TFA
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Endothelin Receptor
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Cardiovascular Disease
Cancer
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Endothelin-2 (49-69), human (TFA) (Endothelin-2 (49-69) (human, canine) (TFA)) is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.
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- HY-P1019A
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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[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 .
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- HY-P2496
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Endothelin Receptor
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Cardiovascular Disease
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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 .
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- HY-106182
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- HY-P0202
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- HY-B0323A
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Sulfafurazole diethanolamine
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Endothelin Receptor
Antibiotic
Bacterial
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Infection
Endocrinology
Cancer
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Sulfisoxazole (Sulfafurazole) diethanolamine is an endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole diethanolamine is a sulfonamide antibacterial with an oxazole substituent. Sulfisoxazole diethanolamine inhibits breast cancer exosome release by targeting endothelin receptor A .
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- HY-B0323
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Sulfafurazole
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Endothelin Receptor
Bacterial
Antibiotic
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Infection
Endocrinology
Cancer
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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 .
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- HY-P0202A
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Endothelin Receptor
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Cardiovascular Disease
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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 .
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- HY-135283
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A-216546
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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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 .
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- HY-15402
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BMS 207940
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Endothelin Receptor
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Cardiovascular Disease
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Edonentan (BMS 207940) is an antagonist for endothelin receptor (ETA receptor), 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 .
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- HY-A0013A
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- HY-A0013
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- HY-B0323R
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Sulfafurazole (Standard)
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Reference Standards
Endothelin Receptor
Bacterial
Antibiotic
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Infection
Endocrinology
Cancer
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Sulfisoxazole (Standard) is the analytical standard of Sulfisoxazole. This product is intended for research and analytical applications. 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 .
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- HY-106994A
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YM598
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Endothelin Receptor
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-P3571
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Endothelin Receptor
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Cancer
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[Ala2] Endothelin-3, human is a linear analog of endothelin-3 (ET-3) where substitution of Ala for Cys residues. TE-3 is a vasoactive peptide, produced by human rhabdomyosarcoma cell lines, whereas it is not expressed by human sarcoma cell lines of non-muscle origin. ET-3 acts as a paracrine factor, since it promotes migration of endothelial cells .
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- HY-106994
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YM598 free base
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Endothelin Receptor
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-P1112
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- HY-P5769
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Endothelin Receptor
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Cardiovascular Disease
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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 .
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- HY-78096
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Endogenous Metabolite
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Metabolic Disease
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O-Deshydroxyethyl bosentan is a metabolite of Bosentan (HY-A0013), which is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors .
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- HY-12378
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BQ-123
2 Publications Verification
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Endothelin Receptor
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Cardiovascular Disease
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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 .
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- HY-P1112A
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Endothelin Receptor
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Cardiovascular Disease
Neurological Disease
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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 .
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- HY-P0204
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- HY-19890
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- HY-12378A
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Endothelin Receptor
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Cardiovascular Disease
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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 .
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- HY-P0204A
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- HY-P3733
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Endothelin Receptor
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Cardiovascular Disease
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Big Endothelin-1 (22-38), human is derived from human, is the 22-38 fragment of Big Endothelin-1 (ET-1) (1-38). Big ET-1 (1-38) is a propeptide of ET-1, which has potent and long-lasting vasoconstrictor effects, equips a specific enzymatic cleavage of the 38 amino acid chain to form ET-1 (1-21) and the C-terminal fragment Big ET-1 (22-38) .
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- HY-115417
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- HY-A0013AR
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- HY-P1236
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Atrial natriuretic factor (1-28) (rat, mouse)
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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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.
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- HY-P2057
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- HY-P1236A
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Atrial natriuretic factor (1-28) (rat, mouse) TFA
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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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.
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- HY-N5171
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Endothelin Receptor
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Cardiovascular Disease
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Aselacin B targets endothelin-1 receptor (ET-1 receptor), inhibits the the binding of ET-1 to ETA receptor and ETB receptor. Aselacin B can be used for research of cardiovascular diseases .
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- HY-102092
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PD 147953
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Endothelin Receptor
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Cardiovascular Disease
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FR139317 (PD 147953) is a selective ETA receptor antagonist. FR139317 inhibits cerebral activation by intraventricular endothelin-1 in conscious rats. FR139317 also ameliorates cerebral vasospasm in dogs .
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- HY-120148A
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Others
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Others
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SM19712 serves as an inhibitor of the nonpeptide endothelin converting enzyme.
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- HY-18211
-
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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CGS 35601 is the inhibitor for endothelin-converting enzyme-1 (ECE-1), neutral endopeptidase 24.11 (NEP), and angiotensin-converting enzyme (ACE), with IC50s of 55, 2, and 22 nM, respectively. CGS 35601 suppresses the big endothelin-1 (big ET-1)- and angiotensin I-induced pressor response, and enhances circulation of atrial natriuretic peptide (ANP), regulates the cardiovascular function in SD rats .
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- HY-114674A
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- HY-P1235A
-
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Atrial Natriuretic Peptide (ANP) (1-28), human, porcine acetate
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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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.
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- HY-P1018
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- HY-122237
-
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Endothelin Receptor
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Cardiovascular Disease
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ATZ-1993 is an orally active, nonpeptide endothelin receptor subtype Aand endothelin receptor subtype B antagonist with pKi values of 8.69, 7.20, respectively. ATZ-1993 has the potential for the research of intimal hyperplasia after balloon denudation of the carotid artery .
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- HY-76520
-
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- HY-118294
-
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16-Phenoxy tetranor prostaglandin F2α isopropyl ester; 16-Phenoxy tetranor PGF2α isopropyl ester
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Prostaglandin Receptor
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Cardiovascular Disease
|
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15-OH Tafluprost, a prostaglandin F2a (PGF2a) analog, relieves endothelin-1 (ET-1)-induced optic nerve head (ONH) blood flow impairment and ET-1-induced contraction of isolated ciliary artery segments .
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- HY-15403
-
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- HY-119667
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- HY-100312
-
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- HY-16465
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- HY-125386
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- HY-15403A
-
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- HY-P1235
-
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Atrial Natriuretic Peptide (ANP) (1-28), human, porcine
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
|
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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.
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- HY-113046
-
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5-Methyl THF; 5-MTHF
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Endogenous Metabolite
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Cardiovascular Disease
Metabolic Disease
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5-Methyltetrahydrofolic acid (5-Methyl THF) is the main circulating form of folic acid in the body and is involved in a variety of biochemical reactions. 5-Methyltetrahydrofolic acid regulates cardiovascular function by increasing the production of endothelin-1 (ET-1) in low-density lipoprotein-treated endothelial cells and can be used in the study of cardiovascular diseases .
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- HY-N5170
-
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Endothelin Receptor
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Cardiovascular Disease
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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 .
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- HY-16465A
-
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- HY-101262
-
-
- HY-157658
-
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- HY-135390
-
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Ro 64-1056
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Drug Metabolite
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Cardiovascular Disease
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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 .
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- HY-P990089
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- HY-17351
-
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- HY-15404
-
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Lu-135252
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
|
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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 .
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- HY-119545
-
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- HY-15402D
-
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BMS 207940 hydrate
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Endothelin Receptor
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Cardiovascular Disease
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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 .
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- HY-17621
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-
- HY-135500
-
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Endothelin Receptor
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Endocrinology
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ACT-373898 is an inactive carboxylic acid metabolite of Macitentan. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist .
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- HY-120148
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- HY-133829
-
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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Zofenoprilat is an orally active inhibitor for angiotensin converting enzyme (ACE) with an IC50 of 1.7 nM. Zofenoprilat inhibits the expression of angiotensin II, reduces the blood pressure, exhibits thus cardioprotective and renalprotective activity. Zofenoprilat promotes the NO production, decreases endothelin-1 (ET-1) expression, exhibits protective effect on vascular endothelial function. Zofenoprilat regulates oxidative stress-related molecules, exhibits antioxidant activity .
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- HY-P4641
-
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
|
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H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitory activity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice .
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- HY-11103R
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- HY-105183
-
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Endothelin Receptor
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Others
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PD 145065 is a highly potent but non-selective endothelin receptor antagonist with an IC50 value of 4 nM for the ETA receptor for rabbit renal artery vascular smooth muscle cells .
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- HY-114674
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- HY-113046S1
-
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5-Methyl THF-13C6; 5-MTHF-13C6
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Isotope-Labeled Compounds
Endogenous Metabolite
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Cardiovascular Disease
Metabolic Disease
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5-Methyltetrahydrofolic acid- 13C6 (5-Methyl THF- 13C6) is 13C labeled 5-Methyltetrahydrofolic acid. 5-Methyltetrahydrofolic acid (5-Methyl THF) is the main circulating form of folic acid in the body and is involved in a variety of biochemical reactions. 5-Methyltetrahydrofolic acid regulates cardiovascular function by increasing the production of endothelin-1 (ET-1) in low-density lipoprotein-treated endothelial cells and can be used in the study of cardiovascular diseases .
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- HY-P4201
-
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Vasopressin Receptor
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Cardiovascular Disease
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JKC 301 is a selective Endothelin A receptor antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking .
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- HY-102029
-
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SRTX-c
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Endothelin Receptor
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Cardiovascular Disease
|
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Sarafotoxin S6c (SRTX-c) is a potent endothelin-B receptor agonist. Sarafotoxin S6c can cause vasoconstriction in both endothelium-intact and endothelium-denuded vessels .
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- HY-17621S
-
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- HY-P10151
-
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Endothelin Receptor
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Cardiovascular Disease
|
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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.
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- HY-14184
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- HY-17352
-
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Ro 61-1790; VML 588; AXV-034343
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Endothelin Receptor
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Cardiovascular Disease
|
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Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction .
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- HY-76520S
-
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- HY-P3563
-
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Endothelin Receptor
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Cardiovascular Disease
|
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[Lys4] Sarafotoxin S6c, a sarafotoxin analogue, is a potent and partial agonist of endothelin receptor. [Lys4] Sarafotoxin S6c elicits contraction of pig coronary artery, with an EC50 of 1.5 nM .
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- HY-19529
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- HY-P10328
-
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DNA/RNA Synthesis
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Metabolic Disease
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Vasoactive intestinal contractor is a novel member of the endothelin family. Vasoactive intestinal contractor stimulates a rapid increase in the intracellular Ca 2+ concentration in fura-2-overexpressed Swiss 3T3 cells [1.
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- HY-14184A
-
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
|
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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).
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- HY-120843
-
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Endothelin Receptor
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Cardiovascular Disease
|
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WS009A is an antagonist for endothelin receptor (ET Receptor) with IC50 of 5.8 and 6.9 μM for ET-1 receptor and ET-2 receptor. WS009A can be used in research of cardiovascular diseases .
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- HY-14184S
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- HY-17352A
-
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Ro 61-1790 disodium; VML 588 disodium; AXV-034343 disodium
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Endothelin Receptor
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Cardiovascular Disease
|
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Clazosentan disodium (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan disodium inhibits ET-1-mediated vasoconstriction. Clazosentan disodium prevents cerebral vasospasm, vasospasm-related cerebral infarction .
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- HY-10088
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ZD4054
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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 .
|
-
- HY-19431
-
|
|
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) .
|
-
- HY-N7543
-
|
|
HIV
|
Infection
|
|
Schisantherin D is a dibenzocyclooctadiene lignan isolated from the fruit of Schisandra sphenanthera. Schisantherin D shows anti-HIV replication activities with an EC50 of 0.5 μg/mL. Schisantherin D inhibits endothelin receptor B (ETBR) and has hepatoprotective effects .
|
-
- HY-114953
-
|
|
Angiotensin Receptor
Endothelin Receptor
|
Cardiovascular Disease
|
|
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 .
|
-
- HY-145516
-
|
Ro 47-8634
|
Drug Metabolite
Cytochrome P450
|
Metabolic Disease
|
|
Desmethyl bosentan is an active metabolite of the endothelin receptor antagonist bosentan (HY-A0013).1 Desmethyl bosentan (25 μM) activates the pregnane X receptor (PXR) in CV-1 monkey kidney cells expressing the human receptor in a reporter assay.
|
-
- HY-103460
-
|
|
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 .
|
-
- HY-117634
-
-
- HY-105168
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
TAK 044 is an antagonist of Endothelin Receptor. TAK 044 strongly inhibits ET-induced deterioration in various animal models. TAK 044 can be used in study ET-related diseases such as acute myocardial infarction,acute renal failure, acute hepatic malfunction, and subarachnoid hemorrhage .
|
-
- HY-14184R
-
|
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) .
|
-
- HY-17352R
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Clazosentan (Standard) is the analytical standard of Clazosentan. This product is intended for research and analytical applications. Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction .
|
-
- HY-N2021
-
-
- HY-P3433
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Sarafotoxin S6b is a vasoconstrictor peptide, and a non-selective endothelin receptor agonist. Sarafotoxin S6b can induce contraction in isolated human coronary arteries , the Ki values of Coronary artery, Saphenous vein and Coronary artery are 0.27, 0.55 and 19.5 nM, respectively .
|
-
- HY-107762
-
|
|
Endothelin-Converting Enzyme (ECE)
|
Cardiovascular Disease
|
|
CGS35066 is a potent and selective aminophosphonate inhibitor of endothelin-converting enzyme-1 (ECE-1). CGS 35066 inhibits the activity of human ECE-1 and rat kidney neutral endopeptidase 24.11 (NEP) in vitro with IC50 values of 22 nM and 2.3 μM, respectively .
|
-
- HY-118497
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS 182874 is an orallyactive, highly selective endothelin receptor (ETA receptor) 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 .
|
-
- HY-103458
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS 182874 hydrochloride is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 hydrochloride reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research .
|
-
- HY-N2021A
-
-
- HY-10088R
-
|
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 .
|
-
- HY-P10135
-
|
|
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 .
|
-
- HY-P1016
-
|
|
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.
|
-
- HY-121300
-
|
(-)-TAN2162
|
Antibiotic
Bacterial
Endothelin Receptor
CGRP Receptor
|
Infection
Cancer
|
|
Kendomycin ((−)-TAN 2162) is a polyketide antibiotic with remarkable antibacterial and cancer cells cytotoxic activities. Kendomycin tends to be bacteriostatic rather than bactericidal and inhibits the growth of the methicillin-resistant Staphylococcus aureus (MRSA) strain COL at a low concentration (MIC of 5 μg/mL). Kendomycin is a potent antagonist of the endothelin receptor and a calcitonin receptor agonist which plays its role as an anti-osteoporotic agent .
|
-
- HY-103459
-
|
PD156707
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration .
|
-
- HY-119843
-
|
Dimethylosoic acid; RES-1214-1; TAN 1415A
|
Antibiotic
|
Infection
|
|
Asterric acid is an antibiotic fungal metabolite that completely inhibits the binding of the potent vasoconstrictor endothelin (ET)-1 to the ETA receptor 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.
|
-
- HY-118497R
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS 182874 (Standard) is the analytical standard of BMS 182874. This product is intended for research and analytical applications. BMS 182874 is an orallyactive, highly selective endothelin receptor (ETA receptor) 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 .
|
-
- HY-P3749
-
|
|
Fluorescent Dye
|
Others
|
|
Mca-(ala7,lys(dnp)9)-bradykinin is a sensitive fluorogenic substrate for ECE-1 (endothelin-converting enzyme-1). The incorporation of a (7-methoxycoumarin-4-yl)acetyl (Mca) fluorescent group and a 2,4-dinitrophenyl (Dnp) quenching group has resulted in a large fluorescence increase upon substrate cleavage .
|
-
- HY-P1016B
-
|
|
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 . .
|
-
- HY-N2575
-
|
|
PKC
Bacterial
Parasite
HIV
VSV
VEGFR
Bcl-2 Family
Apoptosis
|
Infection
Metabolic Disease
Cancer
|
|
Hypocrellin A is a PKC inhibitor that exerts antidiabetic activity by reversing the effects of high glucose on endothelin (ET-1) expression. Hypocrellin A is also a photosensitizer for photodynamic therapy (PDT) with anticancer, antibacterial and antiviral activities, especially against human immunodeficiency virus (HIV). In addition, Hypocrellin-A also possesses anti-Leishmania activity (IC50=0.27 μg/ml) .
|
-
- HY-120295
-
|
|
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 .
|
-
- HY-123744
-
|
|
Endothelin Receptor
|
Cardiovascular 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 .
|
-
- HY-W781265
-
|
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).
|
-
- HY-N2575R
-
|
|
Reference Standards
PKC
Bacterial
Parasite
HIV
VSV
VEGFR
Bcl-2 Family
Apoptosis
|
Infection
Metabolic Disease
Cancer
|
|
Hypocrellin A (Standard) is the analytical standard of Hypocrellin A. This product is intended for research and analytical applications. Hypocrellin A is a PKC inhibitor that exerts antidiabetic activity by reversing the effects of high glucose on endothelin (ET-1) expression. Hypocrellin A is also a photosensitizer for photodynamic therapy (PDT) with anticancer, antibacterial and antiviral activities, especially against human immunodeficiency virus (HIV). In addition, Hypocrellin-A also possesses anti-Leishmania activity (IC50=0.27 μg/ml)[1][2][3][4][5][6][7][8][9].
|
-
- HY-19210
-
|
|
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 .
|
-
- HY-15195
-
|
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 .
|
-
- HY-15195R
-
|
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.
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-P3749
-
|
|
Fluorescent Dyes/Probes
|
|
Mca-(ala7,lys(dnp)9)-bradykinin is a sensitive fluorogenic substrate for ECE-1 (endothelin-converting enzyme-1). The incorporation of a (7-methoxycoumarin-4-yl)acetyl (Mca) fluorescent group and a 2,4-dinitrophenyl (Dnp) quenching group has resulted in a large fluorescence increase upon substrate cleavage .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P2538
-
-
- HY-P4159A
-
|
|
ERK
|
Cardiovascular Disease
|
|
Endothelin-1 (1-31) (Human) TFA is a potent vasoconstrictor and hypertensive agent. Endothelin-1 (1-31) (Human) TFA is derived from the selective hydrolysis of big ET-1 by chymase .
|
-
- HY-P2539
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
Big Endothelin-1 (1-39), porcine is the precursor of endothelin-1. Endothelin-1 (ET-1) is a potent vasopressor peptide. Big Endothelin-1 (1-39), porcine has similar pressor effects in vivo .
|
-
- HY-P3615
-
-
- HY-P5130
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Big endothelin-1 (rat 1-39) is a 39-residues peptide. Big endothelin-1 (rat 1-39) induces diuretic and natriuretic response in conscious Sprague-Dawley rats. Big endothelin-1 (rat 1-39) raises blood pressure in mice .
|
-
- HY-P3610
-
|
|
Endothelin Receptor
|
Others
|
|
[Ala18] Endothelin-1, human is a biologically active peptide. [Ala18] Endothelin-1, human can be used for the research of various biochemical studies.
|
-
- HY-P4159
-
|
|
ERK
|
Cardiovascular Disease
|
|
Endothelin-1 (1-31) (Human) is a potent vasoconstrictor and hypertensive agent. Endothelin-1 (1-31) (Human) is derived from the selective hydrolysis of big ET-1 by chymase .
|
-
- HY-P0207
-
|
endothelin-2 (human, canine); Human endothelin-2
|
Endothelin Receptor
|
Cardiovascular Disease
Cancer
|
|
Endothelin-2 (49-69), human (Endothelin-2 (human, canine)) is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.
|
-
- HY-P4159B
-
|
|
ERK
|
Cardiovascular Disease
|
|
Endothelin-1 (1-31) (Human) acetate is a potent vasoconstrictor and hypertensive agent. Endothelin-1 (1-31) (Human) acetate is derived from the selective hydrolysis of big ET-1 by chymase .
|
-
- HY-P1019
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
[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
|
-
- HY-P3734
-
-
- HY-P0207A
-
|
endothelin-2 (49-69) (human, canine) TFA; Human endothelin-2 TFA
|
Endothelin Receptor
|
Cardiovascular Disease
Cancer
|
|
Endothelin-2 (49-69), human (TFA) (Endothelin-2 (49-69) (human, canine) (TFA)) is a 21-amino acid vasoactive peptide that binds to G-protein-linked transmembrane receptors, ET-RA and ET-RB.
|
-
- HY-P1019A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
[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 .
|
-
- HY-P2496
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
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 .
|
-
- HY-P0202
-
-
- HY-P0202A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
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 .
|
-
- HY-P3614
-
|
|
Peptides
|
Others
|
|
[Ala3,11,18, Nle7] Endothelin-1, human is a synthetic peptide.
|
-
- HY-P3569
-
|
|
Peptides
|
Others
|
|
[D-Val22, Phe33] Big Endothelin-1 (16-38), human is a polypeptide.
|
-
- HY-P3571
-
|
|
Endothelin Receptor
|
Cancer
|
|
[Ala2] Endothelin-3, human is a linear analog of endothelin-3 (ET-3) where substitution of Ala for Cys residues. TE-3 is a vasoactive peptide, produced by human rhabdomyosarcoma cell lines, whereas it is not expressed by human sarcoma cell lines of non-muscle origin. ET-3 acts as a paracrine factor, since it promotes migration of endothelial cells .
|
-
- HY-P1112
-
-
- HY-P5769
-
|
|
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 .
|
-
- HY-12378
-
BQ-123
2 Publications Verification
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
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 .
|
-
- HY-P1112A
-
|
|
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 .
|
-
- HY-P0204
-
-
- HY-P0204A
-
-
- HY-P3733
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Big Endothelin-1 (22-38), human is derived from human, is the 22-38 fragment of Big Endothelin-1 (ET-1) (1-38). Big ET-1 (1-38) is a propeptide of ET-1, which has potent and long-lasting vasoconstrictor effects, equips a specific enzymatic cleavage of the 38 amino acid chain to form ET-1 (1-21) and the C-terminal fragment Big ET-1 (22-38) .
|
-
- HY-P1236
-
|
Atrial natriuretic factor (1-28) (rat, mouse)
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
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.
|
-
- HY-P2057
-
-
- HY-P1236A
-
|
Atrial natriuretic factor (1-28) (rat, mouse) TFA
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
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.
|
-
- HY-P1235A
-
|
Atrial Natriuretic Peptide (ANP) (1-28), human, porcine acetate
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
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.
|
-
- HY-P1018
-
-
- HY-P4912
-
|
|
Peptides
|
Others
|
|
Big Endothelin-1 (rat) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
|
-
- HY-P5080
-
|
|
Peptides
|
Others
|
|
Big Endothelin-2 (human) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
|
-
- HY-P4915
-
|
|
Peptides
|
Others
|
|
Big Endothelin-3 (22-41) amide (human) is a polypeptide that can be found by peptide screening. Peptide screening is a research tool that pools active peptides primarily by immunoassay. Peptide screening can be used for protein interaction, functional analysis, epitope screening, especially in the field of agent research and development .
|
-
- HY-16465
-
-
- HY-P1235
-
|
Atrial Natriuretic Peptide (ANP) (1-28), human, porcine
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
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.
|
-
- HY-16465A
-
-
- HY-P4641
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
H-Trp-Phe-OH is a dipeptide consisting of tryptophan and phenylalanine (Trp-Phe). H-Trp-Phe-OH is also an antihypertensive peptide with inhibitory activity on angiotensin-converting enzyme (ACE), dose-dependently increases NO levels, and decreases endothelin-1 (ET-1) levels. H-Trp-Phe-OH (2 mg/kg; subcutaneous injection; 6 injections over 3 days) causes an increase in ovarian weight in female mice .
|
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- HY-105183
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Endothelin Receptor
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Others
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PD 145065 is a highly potent but non-selective endothelin receptor antagonist with an IC50 value of 4 nM for the ETA receptor for rabbit renal artery vascular smooth muscle cells .
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- HY-P4201
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Vasopressin Receptor
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Cardiovascular Disease
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JKC 301 is a selective Endothelin A receptor antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking .
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- HY-102029
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SRTX-c
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Endothelin Receptor
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Cardiovascular Disease
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Sarafotoxin S6c (SRTX-c) is a potent endothelin-B receptor agonist. Sarafotoxin S6c can cause vasoconstriction in both endothelium-intact and endothelium-denuded vessels .
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- HY-P10151
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Endothelin Receptor
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Cardiovascular Disease
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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.
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- HY-P3563
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Endothelin Receptor
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Cardiovascular Disease
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[Lys4] Sarafotoxin S6c, a sarafotoxin analogue, is a potent and partial agonist of endothelin receptor. [Lys4] Sarafotoxin S6c elicits contraction of pig coronary artery, with an EC50 of 1.5 nM .
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- HY-P10328
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DNA/RNA Synthesis
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Metabolic Disease
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Vasoactive intestinal contractor is a novel member of the endothelin family. Vasoactive intestinal contractor stimulates a rapid increase in the intracellular Ca 2+ concentration in fura-2-overexpressed Swiss 3T3 cells [1.
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- HY-105168
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Endothelin Receptor
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Cardiovascular Disease
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TAK 044 is an antagonist of Endothelin Receptor. TAK 044 strongly inhibits ET-induced deterioration in various animal models. TAK 044 can be used in study ET-related diseases such as acute myocardial infarction,acute renal failure, acute hepatic malfunction, and subarachnoid hemorrhage .
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- HY-P3433
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Endothelin Receptor
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Cardiovascular Disease
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Sarafotoxin S6b is a vasoconstrictor peptide, and a non-selective endothelin receptor agonist. Sarafotoxin S6b can induce contraction in isolated human coronary arteries , the Ki values of Coronary artery, Saphenous vein and Coronary artery are 0.27, 0.55 and 19.5 nM, respectively .
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- HY-P10135
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Endothelin Receptor
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Cardiovascular Disease
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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 .
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- HY-P1016
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Endothelin Receptor
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Cardiovascular Disease
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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.
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- HY-P3749
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Fluorescent Dye
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Others
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Mca-(ala7,lys(dnp)9)-bradykinin is a sensitive fluorogenic substrate for ECE-1 (endothelin-converting enzyme-1). The incorporation of a (7-methoxycoumarin-4-yl)acetyl (Mca) fluorescent group and a 2,4-dinitrophenyl (Dnp) quenching group has resulted in a large fluorescence increase upon substrate cleavage .
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- HY-P1016B
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Endothelin Receptor
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Cardiovascular Disease
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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 . .
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- HY-14184S
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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) .
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- HY-113046S1
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5-Methyltetrahydrofolic acid- 13C6 (5-Methyl THF- 13C6) is 13C labeled 5-Methyltetrahydrofolic acid. 5-Methyltetrahydrofolic acid (5-Methyl THF) is the main circulating form of folic acid in the body and is involved in a variety of biochemical reactions. 5-Methyltetrahydrofolic acid regulates cardiovascular function by increasing the production of endothelin-1 (ET-1) in low-density lipoprotein-treated endothelial cells and can be used in the study of cardiovascular diseases .
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- HY-17621S
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Sparsentan-d5 is deuterium labeled Sparsentan. Sparsentan (RE-021) is a highly potent dual angiotensin II and endothelin A receptor antagonist with Kis of 0.8 and 9.3 nM, respectively .
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- HY-76520S
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Sitaxsentan- 13C6 (IPI 1040- 13C6) is 13C labeled Sitaxsentan (HY-76520). Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist.
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