Catalog No.
Product Name
Application
Product Information
Citations
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Endothelin-A Receptor Antagonist
PD-156707 is a selective endothelin-A receptor antagonist that exhibits potent oral activity. This compound binds to human ET-A and ET-B receptors with Ki values of 0.17 nM and 133.8 nM, respectively. PD-156707 has demonstrated efficacy in reversing established chronic hypoxic pulmonary hypertension in rat models. It is suitable for research on diseases related to aberrant endothelin-A receptor activation, with potential applications in pulmonary hypertension, stroke, and heart failure studies. -
Stable Isotope
(Rac)-Ambrisentan-d3 is a deuterated form of (Rac)-Ambrisentan, a selective endothelin receptor antagonist. This stable isotope is utilized in pharmacokinetic studies and metabolic research, allowing for precise tracking of drug metabolism and distribution in biological systems. Its application is essential for understanding the pharmacological properties and efficacy of endothelin receptor-targeted therapies. -
Endothelin Receptor Agonist
[Lys4] Sarafotoxin S6c is a potent partial agonist of the endothelin receptor. This sarafotoxin analogue induces contraction in pig coronary artery tissues, demonstrating an EC50 of 1.5 nM. It serves as a valuable tool for research in cardiovascular physiology and the study of endothelin receptor signaling pathways. -
ETB Receptor Antagonist
RES-701-1 is a cyclic peptide that serves as a specific antagonist for the endothelin receptor type B (ETB). This compound effectively inhibits the binding of 125I-labeled endothelin-1 (ET-1) to the ETB receptor, demonstrating an IC50 value of 10 nM. RES-701-1 is primarily utilized for research applications aimed at studying the role of ETB receptors in cardiovascular and other physiological processes. -
Endothelin-B Receptor Antagonist
PD 142893 is an endothelin-B receptor antagonist that selectively inhibits the action of endothelin-1, a potent vasoconstrictor. This compound demonstrates significant biological activity in modulating blood pressure and vascular resistance, making it a valuable tool in cardiovascular research. PD 142893 is widely used to study the role of endothelin signaling in various physiological and pathological conditions, including pulmonary hypertension and heart failure. -
ETB Antagonist
K-8794 is a selective endothelin receptor type B (ETB) antagonist that exhibits oral bioactivity. This compound is valuable for investigating its potential therapeutic effects in cardiovascular diseases by modulating endothelin-mediated pathways. K-8794 can aid in elucidating the role of ETB receptors in various biological processes and support research on related cardiovascular conditions. -
Endothelin ETA Receptor Antagonist
S-1255 is a highly selective endothelin ETA receptor antagonist with a dissociation constant (Kd) of 0.39 nM. This compound effectively inhibits vasoconstriction, leading to sustained hypotensive effects in hypertensive animal models. S-1255 serves as a valuable tool in the study of hypertension and related cardiovascular disorders, providing insights into the endothelin signaling pathway and its role in vascular regulation. -
Endothelin-A Antagonist
BMS-187308 is an orally active antagonist of the endothelin-A (ETA) receptor, exhibiting a Ki of 4.7 nM for ETA and a Ki of 1.7 μM for ETB. This compound effectively inhibits the pressor response to endothelin-1 (ET-1) with an ED25 value of 1.2 µmol/kg when administered intravenously. BMS-187308 serves as a valuable tool for research focused on the physiological and pathophysiological roles of endothelin in various biological systems. -
Endothelin Receptor Agonist
Sarafotoxin S6b is a potent vasoconstrictor peptide and a non-selective agonist of endothelin receptors. This compound effectively induces contraction in isolated human coronary arteries, exhibiting Ki values of 0.27 nM, 0.55 nM, and 19.5 nM for the coronary artery, saphenous vein, and coronary artery, respectively. Sarafotoxin S6b is valuable for research applications focused on cardiovascular physiology and the roles of endothelin signaling in vascular constriction. -
Endothelin (ETA) Receptor Antagonist
CI-1020 is a selective antagonist of the endothelin (ETA) receptor, exhibiting an IC50 value of 0.3 nM. This compound effectively inhibits intimal hyperplasia in human saphenous vein organ culture. Furthermore, CI-1020 demonstrates potential in the treatment of hypoxic pulmonary hypertension by blocking ET-1-induced pressor responses following oral administration, making it a valuable tool for research in vascular biology and cardiovascular diseases. -
Endothelin A Receptor Antagonist
Fandosentan potassium is a selective antagonist of the endothelin A receptor (ETAR). It effectively reverses hypoxic pulmonary vasoconstriction in perinatal lamb models, making it a valuable tool for investigating pulmonary hypertension. Additionally, Fandosentan potassium inhibits the activities of CYP2C9 and CYP3A4 with IC50 values of 39.6 μM and 21.6 μM, respectively, supporting its application in exploring drug metabolism and interactions. -
ETB Receptor Agonist
BQ-3020 is a selective endothelin receptor (ETB receptor) agonist known for its ability to displace [125I] ET-1 binding at ETB receptors, exhibiting an IC50 of 0.2 nM. This compound induces vasoconstriction in the rabbit pulmonary artery and promotes relaxation of the pig urinary bladder neck. BQ-3020 is valuable for research in cardiovascular diseases, providing insights into endothelin signaling pathways and their physiological implications. -
Endothelin converting enzyme inhibitor
Daglutril targets the endothelin receptor, exhibiting the ability to modulate cytokine-induced endothelin-1 production in astrocytes. Its inhibitory effects on endothelin-1 generation make it a valuable research tool for screening compounds that regulate this peptide's synthesis in glial cells. This compound is particularly relevant for studies investigating the role of endothelin-1 in neuroinflammation and related neurological disorders. -
Endothelin Receptor Antagonist
TAK 044 is an antagonist of the Endothelin Receptor, exhibiting potent inhibitory effects on endothelin-induced pathological changes in various animal models. This compound is valuable for exploring the role of endothelin in diseases such as acute myocardial infarction, acute renal failure, acute hepatic malfunction, and subarachnoid hemorrhage. Researchers can leverage TAK 044 to investigate therapeutic strategies targeting endothelin-related conditions. -
Endothelin Antagonist
PD 156252 is a highly potent endothelin antagonist, primarily targeting the ETA and ETB receptor subtypes. It exhibits enhanced binding affinity with IC50 values of 1.0 nM for rabbit ETA receptors and 40 nM for rat ETB receptors. This compound is valuable for research applications focusing on the endothelin system, cardiovascular studies, and investigations into related pathophysiological conditions. -
Macitentan Metabolite
ACT-373898 is the inactive carboxylic acid metabolite of Macitentan, a non-peptide dual antagonist of ETA and ETB endothelin receptors. This compound serves as a valuable reference for studies examining the pharmacokinetics and metabolic pathways of Macitentan. Its characterization is essential for understanding the therapeutic efficacy and safety profiles associated with endothelin receptor modulation in cardiovascular research. -
Endothelin Receptor Antagonist
TA-0201 is a competitive, non-peptide antagonist targeting endothelin receptors. It effectively inhibits the binding of [125I]ET-1 to cloned human ETA and ETB receptors, demonstrating Ki values of 15 pM and 41 nM, respectively. TA-0201 further reduces the pressor response induced by exogenous big ET-1, making it a valuable tool for studies aimed at understanding endothelin-mediated pathways and potential therapeutic interventions in cardiovascular research. -
Endothelin Receptor Antagonist
Edonentan is a potent endothelin receptor antagonist, specifically targeting the ETA receptor with an affinity (Ki) of 10 pM. This compound demonstrates metabolic stability and favorable pharmacokinetic properties in rat models. Edonentan effectively modulates the endothelin system by inhibiting the hypertensive response induced by big endothelin, making it a valuable tool for research in cardiovascular and renal disease studies. -
Endothelin Receptor Antagonist
PD 145065 is a highly potent non-selective endothelin receptor antagonist, demonstrating an IC50 value of 4 nM for the ETA receptor in rabbit renal artery vascular smooth muscle cells. This compound effectively inhibits endothelin signaling, making it useful for investigating the role of endothelin in cardiovascular biology and related disorders. PD 145065 is a valuable tool for researchers studying vascular physiology and potential therapeutic interventions targeting endothelial dysfunction. -
ETA/ETB Receptor Antagonist
L-749329 is a potent antagonist of the endothelin receptor subtypes ETA and ETB, exhibiting binding affinities (Kis) of 0.062 nM and 2.25 nM, respectively. This compound effectively inhibits endothelin-1 (ET-1)-stimulated signaling pathways, making it a valuable tool for studying the role of endothelin receptors in pathophysiological conditions. L-749329 is applicable in research focused on cardiovascular diseases, vascular biology, and related fields where endothelin signaling is implicated. -
Endothelin Receptor Antagonist
Atrasentan sodium is a selective endothelin receptor antagonist, exhibiting an IC50 of 0.0551 nM for the ETA receptor. This compound demonstrates significant biological activity by inhibiting endothelin-1-mediated vasoconstriction and fibrosis. Atrasentan sodium is primarily utilized in research applications related to cardiovascular diseases, pulmonary hypertension, and kidney injury, making it valuable for studies on endothelin signaling pathways and potential therapeutic interventions. -
Endothelin Receptor Antagonist
WS009B is a selective endothelin receptor antagonist, exhibiting IC50 values of 0.67 μM for ET-1 and 0.8 μM for ET-2. This compound is useful for research into cardiovascular diseases, as it modulates the endothelin signaling pathway, which plays a critical role in vascular homeostasis and pathological conditions. WS009B's antagonistic properties make it a valuable tool for elucidating the mechanisms underlying endothelin-mediated physiological and pathological processes. -
ET(A)/ET(B) Antagonist
ATZ-1993 is a potent orally active nonpeptide antagonist of endothelin receptor subtype A and B, exhibiting pKi values of 8.69 and 7.20, respectively. This compound demonstrates significant potential in the study of intimal hyperplasia following balloon denudation of the carotid artery. ATZ-1993 can serve as a valuable tool in cardiovascular research, aiding in the exploration of vascular remodeling and related pathophysiological processes. -
Endothelin Receptor Antagonist
BMS 182874 hydrochloride is a highly selective antagonist of the endothelin ETA receptor, exhibiting an IC50 value of 0.150 μM and a Ki of 0.055 μM. This compound demonstrates efficacy in reducing arterial pressure in rat models of hypertension induced by deoxycorticosterone acetate. BMS 182874 hydrochloride is suitable for research applications focused on cardiovascular diseases and endothelin receptor modulation. -
Endothelin B Receptor Antagonist
IRL 1038 is a selective antagonist for the endothelin B receptor, with a binding affinity characterized by a Ki range of 6-11 nM. This compound effectively inhibits the actions of endothelin-1, crucial for studies investigating vascular function, cardiovascular diseases, and related physiological processes. Its application is valuable in elucidating the role of endothelin signaling in various pathophysiological conditions. -
ETA/ETB Receptor Antagonist
IRL-3630 is a selective antagonist of the ETA and ETB receptors, exhibiting binding affinities with Ki values of 1.9 nM and 1.2 nM, respectively. This compound is instrumental in studying the role of endothelin receptors in various physiological and pathological processes. Its applications include cardiovascular research, pulmonary hypertension studies, and investigations into renal function. -
Endothelin Receptor Antagonist
SB-209670 is a highly potent non-peptide antagonist of the endothelin (ET) receptor, exhibiting subnanomolar affinity with Ki values of 0.2 nM for ETA and 18 nM for ETB. This compound effectively inhibits the binding of 125I-labeled ET-1 to both human ET receptor subtypes, making it a valuable tool in cardiovascular and neurological research. SB-209670 demonstrates significant biological activity by reducing blood pressure in hypertensive models, offering neuroprotective effects against ischemia-induced neuronal degeneration, and inhibiting neointima formation following carotid artery balloon angioplasty in rats. -
ET Receptor Antagonist
WS009A is a potent antagonist of endothelin receptors, exhibiting IC50 values of 5.8 µM and 6.9 µM for the ET-1 and ET-2 receptors, respectively. This compound is valuable for investigating the role of endothelin signaling in cardiovascular diseases and potential therapeutic applications. Its effective inhibition of endothelin receptors makes WS009A a useful tool for researchers studying vascular dysfunction and related pathophysiological conditions. -
GPR120 Agonist
GPR120 Agonist 5 is a selective agonist for the GPR120 receptor, exhibiting an EC50 of 1.2 μM. This compound enhances the secretion of glucagon-like peptide-1 (GLP-1) through its interaction with GPR120, leading to increased insulin production and decreased blood glucose levels. Additionally, GPR120 Agonist 5 demonstrates anti-inflammatory properties, making it a valuable tool for studies focused on metabolic disorders, obesity, insulin resistance, and type 2 diabetes. This reagent is essential for investigating the biological functions and therapeutic potential of GPR120 in relevant disease models. -
GPR40 Full Agonist
AM-6226 is a potent full agonist of the G protein-coupled receptor 40 (GPR40), exhibiting an EC50 of 0.12 μM. This compound effectively activates GPR40 receptors on pancreatic β cells and enteroendocrine L cells, promoting insulin secretion in a glucose-dependent manner while enhancing the release of incretin hormones like GLP-1 and GIP. AM-6226 is valuable for research into metabolic diseases, particularly diabetes, due to its potential to mitigate hypoglycemia risks. -
GPR40 Agonist
GPR40 Agonist 7 is a potent and orally active agonist of the G protein-coupled receptor GPR40. This compound enhances insulin and GLP-1 secretion, demonstrating notable hypoglycemic effects in vivo, with an effective dose (ED50) of 0.58 mg/kg. It serves as a valuable research tool for studying glucose metabolism and related metabolic disorders. -
GPR40 Agonist
BMS-986118 is a selective agonist of GPR40, exhibiting potent biological activity with an EC50 of 0.07 µM. This compound enhances insulin secretion and stimulates GLP-1 release, leading to significant reductions in plasma glucose levels in acute animal models. BMS-986118 is valuable for research in diabetes and metabolic disorders, providing insights into the regulation of glucose homeostasis. -
GPR120 Agonist
LXT34 is a potent agonist of the GPR120 receptor, demonstrating significant anti-inflammatory activity. This compound enhances GLP-1 production in the gastrointestinal tract and ameliorates insulin resistance in both macrophages and pancreatic cells. LXT34 is applicable in studies related to inflammatory diseases, including type 2 diabetes, obesity, and non-alcoholic fatty liver disease. -
GPR40 Agonist
LY2881835 is a selective agonist of the G protein-coupled receptor 40 (GPR40), demonstrating potent activity in promoting the secretion of insulin and GLP-1, while effectively lowering glucose levels in a dose-dependent manner. This compound shows promise for research applications related to type 2 diabetes mellitus. Additionally, LY2881835 features an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) for click chemistry experiments. -
Anti-diabete Agent
Hyocholic acid is a bile acid primarily found in porcine sources, demonstrating significant anti-diabetic properties. Its mechanism involves promoting GLP-1 secretion through activation of TGR5 and inhibition of FXR in enteroendocrine cells. This compound has potential applications in research aimed at understanding and treating type 2 diabetes and related metabolic disorders. -
GPCR19 Agonist /FXR Antagonist
Ursodeoxycholic acid sodium is a potent agonist of the G-protein coupled receptor 19 (GPCR19) and antagonist of the farnesoid X receptor (FXR). This secondary bile acid plays a crucial role in maintaining intestinal barrier integrity and regulating lipid metabolism. Its ability to modulate bile acid-activated receptors makes it valuable for investigating various hepatic and gastrointestinal diseases. Ursodeoxycholic acid sodium is also orally active, making it suitable for diverse in vitro and in vivo research applications. -
TGR5 Agonist
Cholic acid 7-sulfate is a selective agonist for the TGR5 receptor with an EC50 of 0.17 μM. This compound enhances GLP-1 secretion in enteroendocrine L cells, leading to improved glucose tolerance through TGR5 activation. Additionally, as an endogenous ligand for MHC class I-related protein (MR1), it supports the survival of mucosal-associated invariant T (MAIT) cells and influences their development and function by modulating homeostatic gene expression. Cholic acid 7-sulfate is valuable in studies related to diabetes and MAIT cell-mediated immune regulation. -
TGR5 Activator
WB403 is a potent TGR5 activator with an EC50 of 5.5 μM for human TGR5. It enhances downstream signaling pathways associated with glucose metabolism, notably promoting GLP-1 secretion, improving glucose tolerance, and lowering fasting and postprandial blood glucose levels as well as HbA1c in murine models of type 2 diabetes. Additionally, WB403 contributes to increased pancreatic β-cell mass and the restoration of the islet cell distribution. This compound is valuable for studying mechanisms and therapeutic strategies in type 2 diabetes research. -
Stable Isotope
Cholic acid 7-sulfate-d4 is a deuterium-labeled derivative of cholic acid 7-sulfate, a selective agonist for the TGR5 receptor with an EC50 of 0.17 μM. This compound plays a crucial role in stimulating GLP-1 secretion and enhancing glucose tolerance through its action on enteroendocrine L cells. Additionally, cholic acid 7-sulfate-d4 serves as an endogenous ligand for MHC class I-related protein (MR1), influencing the development and function of mucosal-associated invariant T cells (MAIT). It is primarily utilized in research focused on diabetes and immune regulation related to MAIT cells. -
G Protein-coupled Receptor 40 Agonist
DS-1558 is an orally bioavailable small molecule that acts as an agonist for G Protein-coupled Receptor 40 (GPR40). It enhances glucose-stimulated insulin secretion mediated by glucagon-like peptide-1 (GLP-1) and amplifies the insulinogenic response to intravenous glucose in normal Sprague Dawley rats. This compound is a valuable tool for researching mechanisms underlying type 2 diabetes and developing potential therapeutic strategies. -
GLP-1R/GCGR Agonist
Mazdutide is a long-acting synthetic analog of oxyntomodulin that functions as a dual agonist of the glucagon-like peptide-1 receptor (GLP-1R) and the glucagon receptor (GCGR). By binding to these targets with high affinity (Ki values of 17.7 nM for GCGR and 28.6 nM for GLP-1R in humans), Mazdutide promotes insulin secretion from mouse islets (EC50: 5.2 nM). This compound is primarily utilized in research addressing obesity and type 2 diabetes (T2D) to explore its therapeutic potential and metabolic effects. -
GLP-1R Agonist
GLP-1R Agonist 2 is a potent agonist of the glucagon-like peptide-1 receptor (GLP-1R), functioning through the formation of hydrogen bonds with key residues Tyr42, Cys71, and Ser84. This compound demonstrates significant biological activity in stimulating insulin secretion and inhibiting glucagon release, making it a valuable tool for research into metabolic disorders such as type 2 diabetes and obesity. Its mechanism of action positions it as an important candidate for the development of therapeutics targeting these conditions. -
GCGR/GLP-1R Agonist
Survodutide is a potent dual agonist of the glucagon receptor (GCGR) and GLP-1 receptor (GLP-1R), exhibiting EC50 values of 0.52 nM and 0.33 nM, respectively, in CHO-K1 cells. This 29-amino-acid acylated peptide, featuring a C18 fatty acid, demonstrates significant anti-obesity effects through mechanisms that enhance energy expenditure and reduce food intake. Survodutide is valuable for research into metabolic disorders and obesity management. -
GLP-1 Receptor Antagonist
GLP-1(9-36)amide is a potent antagonist of the glucagon-like peptide-1 (GLP-1) receptor, generated from the enzymatic action of dipeptidyl peptidase-4 (DPP-4) on GLP-1(7-36)amide. This peptide plays a crucial role in glucose metabolism and insulin signaling and is utilized in research aimed at understanding metabolic disorders and the role of GLP-1 in obesity and diabetic conditions. The study of GLP-1(9-36)amide can provide insights into receptor regulation and potential therapeutic strategies for GLP-1 related pathologies. -
GLP-1R/GLP-2R Agonist
Dapiglutide is a dual agonist targeting the glucagon-like peptide-1 receptor (GLP-1R) and glucagon-like peptide-2 receptor (GLP-2R). This long-acting compound has been shown to mitigate intestinal dysfunction in mouse models of short bowel syndrome and exhibits significant anti-obesity properties. Dapiglutide is valuable for research into metabolic disorders and the therapeutic potential of GLP-1/GLP-2 receptor modulation. -
GCGR Modulator
LSN3318839 is an orally active positive modulator of the glucagon receptor (GCGR). This compound enhances insulin secretion and exhibits hypoglycemic effects, making it valuable in the study of glucose metabolism and diabetes management. It is suitable for research applications focused on metabolic disorders and endocrine signaling pathways. -
GLP-1 Receptor Agonist
TT-OAD2 is a non-peptide agonist of the glucagon-like peptide-1 (GLP-1) receptor, exhibiting a potent EC50 of 5 nM. This compound plays a significant role in enhancing glucose-dependent insulin secretion and may be utilized in the treatment of diabetes. Its selective activity makes it a valuable tool for studying GLP-1 receptor signaling pathways and their implications in metabolic disorders. -
GLP-1R Agonist
Orforglipron hemicalcium hydrate is a calcium salt hydrate derivative of Orforglipron, functioning as a GLP-1 receptor (GLP-1R) agonist. This compound demonstrates significant biological activity in enhancing insulin secretion and lowering blood glucose levels, making it a pivotal candidate for research in type 2 diabetes treatment. Its oral bioavailability and receptor selectivity support various studies aimed at understanding the therapeutic potential of GLP-1R modulation in metabolic disorders. -
GLP-1/GCGR Agonist
Cotadutide is a potent dual agonist of glucagon-like peptide-1 (GLP-1) and glucagon receptor (GCGR), demonstrating EC50 values of 6.9 pM and 10.2 pM, respectively. This compound effectively promotes weight loss, enhances glycemic control, and alleviates fibrosis. Cotadutide is suitable for research applications focused on obesity and type 2 diabetes (T2D). -
GCGR Agonist
Taspoglutide is a long-acting glucagon-like peptide 1 (GLP-1) receptor agonist that primarily targets the glucagon receptor (GCGR). It exhibits potent biological activity with an EC50 value of 0.06 nM. This compound is primarily investigated for its therapeutic potential in managing type 2 diabetes, promoting insulin secretion, and regulating glucose metabolism. Research applications include studying metabolic disorders and developing treatments for diabetes-related complications.
