Catalog No.
Product Name
Application
Product Information
Citations
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Vasoconstrictor
Endothelin-1 (1-31) (Human) is a potent vasoconstrictor that primarily targets endothelin receptors to induce vascular smooth muscle contraction. This peptide plays a significant role in regulating blood pressure and is involved in various cardiovascular pathologies. It is widely utilized in research applications focused on cardiovascular physiology, hypertension, and related therapeutic interventions. -
Stable Isotope
Carvedilol-d4 is a deuterated derivative of Carvedilol, a non-selective β/α-1 adrenergic receptor antagonist. It exhibits dose-dependent inhibition of lipid peroxidation with an IC50 value of 5 μM. Carvedilol acts as a multifaceted antihypertensive agent, demonstrating potential therapeutic applications in managing conditions such as angina and congestive heart failure. Additionally, it has been identified as an autophagy inducer and a modulator of the NLRP3 inflammasome, making it a valuable tool for research into cardiovascular and inflammatory diseases. -
Platelet Aggregation Inhibitor
Notoginsenoside Fc is a protopanaxadiol-type saponin derived from the leaves of Panax notoginseng, functioning primarily as a platelet aggregation inhibitor. This compound effectively mitigates platelet aggregation and has been shown to enhance reendothelialization after vascular injury in diabetic rat models by promoting autophagy. Its biological activity makes Notoginsenoside Fc a valuable reagent for research in cardiovascular health and vascular regeneration. -
Stable Isotope
Theophylline-d6 is a deuterium-labeled analog of Theophylline, primarily utilized as a stable isotope in research. Theophylline functions as a nonselective phosphodiesterase (PDE) inhibitor and adenosine receptor antagonist, while also acting as an activator of histone deacetylase (HDAC). This compound is valuable in studies exploring cellular signaling pathways, pharmacology, and the biochemical mechanisms underlying various therapeutic effects. -
Dopamine Receptors Blocker
Trifluoperazine dimaleate is a potent dopamine receptor blocker, primarily indicated for research into antipsychotic mechanisms. This compound exhibits significant α1-adrenergic receptor antagonism and serves as an inhibitor of NUPR1, highlighting its potential anticancer properties. Additionally, trifluoperazine dimaleate functions as a calmodulin inhibitor and inhibits P-glycoprotein activity. Its versatile applications extend to studying schizophrenia and the reversible inhibition of influenza virus morphogenesis. -
Stable Isotope
Carvedilol-d3 is a deuterium-labeled analogue of Carvedilol, functioning primarily as a non-selective β/α-1 adrenergic receptor blocker. It exhibits significant biological activity by inhibiting lipid peroxidation in a dose-dependent manner with an IC50 value of 5 μM. This compound serves as a versatile antihypertensive agent and has potential applications in the treatment of angina and congestive heart failure. Furthermore, Carvedilol-d3 promotes autophagy and is known to inhibit the NLRP3 inflammasome, making it valuable for research involving inflammatory processes. -
5-HT6R Antagonist
PUC-10 is a potent antagonist of the 5-HT6 receptor, exhibiting a Ki value of 14.6 nM and an IC50 of 32 nM. Computational studies indicate that PUC-10 is orally bioactive and capable of penetrating the blood-brain barrier. This compound effectively induces autophagy in SH-SY5Y neuronal cells by inhibiting the mTOR signaling pathway. PUC-10 is ideally suited for studies focused on neurological disorders and related therapeutic strategies. -
Stable Isotope
Trifluoperazine-d3 dihydrochloride is a deuterated derivative of Trifluoperazine, primarily targeting dopamine receptors to exert its antipsychotic effects. This compound is a potent α1-adrenergic receptor antagonist and an effective inhibitor of NUPR1, showcasing anticancer properties. Additionally, it functions as a calmodulin inhibitor and can interfere with P-glycoprotein activity. Trifluoperazine-d3 dihydrochloride is valuable for research applications related to schizophrenia and serves as a reversible inhibitor of influenza virus morphogenesis. -
Stable Isotope
Yangonin-d3 is a deuterium-labeled derivative of Yangonin, acting as a stable isotope. This compound demonstrates binding affinity for the human recombinant cannabinoid CB1 receptor, with an IC50 of 1.79 μM and a Ki of 0.72 μM. Yangonin-d3 is valuable for research applications in cannabinoid receptor studies, enabling the exploration of receptor mechanisms and the development of cannabinoid-based therapeutics. -
Stable Isotope
Carvedilol-d5 is a deuterium-labeled analogue of Carvedilol, a non-selective β/α-1 adrenergic receptor blocker. It exhibits lipid peroxidation inhibition with an IC50 of 5 μM and serves as a versatile antihypertensive agent, showing potential in the treatment of angina and congestive heart failure. Additionally, Carvedilol functions as an autophagy inducer and inhibits the NLRP3 inflammasome, making it relevant for research in inflammatory pathways and cardiovascular health. -
Autophagy Inducer
Cabergoline diphosphate is an ergot alkaloid that acts as an agonist of dopamine D2-like receptors, demonstrating high affinity for D2, D3, and 5-HT2B receptors with Ki values of 0.7, 1.5, and 1.2, respectively. It serves as an autophagy inducer, making it a valuable tool for research focused on cellular processes related to autophagy and neurobiology. This compound is instrumental in studies investigating neurodegenerative diseases and metabolic regulation, providing insights into the role of dopamine receptors in cellular homeostasis. -
Stable Isotope
Dronedarone-d6 hydrochloride is a deuterium-labeled derivative of Dronedarone, serving as a stable isotope for research applications. This compound functions primarily as a class III antiarrhythmic agent, effective in the study of atrial fibrillation (AF) and atrial flutter. Dronedarone-d6 hydrochloride exhibits potent blockade of various ion currents, including potassium, sodium, and L-type calcium currents, and also demonstrates antiadrenergic activity through noncompetitive binding to β-adrenergic receptors. Additionally, it acts as a substrate and moderate inhibitor of the CYP3A4 enzyme, making it valuable for pharmacokinetic studies. -
Stable Isotope
Cabergoline-d6 is a stable isotope-labeled form of Cabergoline, an ergot-derived dopamine D2-like receptor agonist. This compound exhibits high affinity for dopamine receptors D2 and D3, as well as 5-HT2B receptors, with Ki values of 0.7, 1.5, and 1.2 nM respectively. Cabergoline-d6 is utilized in pharmacokinetic studies and metabolic research to investigate the behavior of Cabergoline in biological systems. -
Stable Isotope
Dronedarone-d6 is a deuterium-labeled derivative of the antiarrhythmic agent Dronedarone, primarily targeting various ion channels, including potassium, sodium, and L-type calcium channels. This compound is vital for investigating the mechanisms underlying atrial fibrillation (AF) and atrial flutter, as well as for studying its antiadrenergic properties through its noncompetitive binding to β-adrenergic receptors. In addition, Dronedarone-d6 serves as a substrate and moderate inhibitor of CYP3A4, making it relevant for pharmacokinetic studies in cardiovascular research. -
CB1 Antagonist/PPARα Agonist
OLHHA is a dual CB1 receptor antagonist and PPARα agonist. This compound demonstrates notable activity in inhibiting alcohol intake with an EC50 value of 0.2 mg/kg. Additionally, OLHHA effectively reduces hepatic lipid accumulation and circulating triglyceride levels, exhibiting anti-steatotic properties. Its mechanism and effects make it a valuable tool for research into non-alcoholic fatty liver disease (NAFLD). -
D4R Antagonist
Dopamine D4 receptor ligand 3 is a selective antagonist of the dopamine D4 receptor (D4R), exhibiting a pKi of 8.86. It demonstrates significant activity with pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 signaling pathways in HEK-293T cells, respectively. Additionally, this compound has been shown to inhibit cell viability in three human glioma cell lines—U87 MG, T98G, and U251 MG—while also inducing reactive oxygen species (ROS) production and mitochondrial dysfunction in these glioma cells. This makes it a valuable tool for studying the role of D4R antagonism in cancer biology and neuropharmacology. -
β1-adrenoceptor Antagonist
Landiolol is a highly selective, ultra-short-acting antagonist of β1-adrenergic receptors. By competitively inhibiting these receptors, Landiolol effectively reduces heart rate and myocardial oxygen demand while minimally affecting cardiac ion channels and exhibiting a weak negative inotropic effect. Its ability to inhibit TNF-α-induced mitochondrial hyperactivity and reactive oxygen species production makes it valuable in models of sepsis, where it can mitigate renal injury. Landiolol is applicable in research involving perioperative tachycardia management and investigations into sepsis-related acute kidney injury. -
CB1 Receptor Inhibitor
Pregnenolone monosulfate sodium (3β-Hydroxy-5-pregnen-20-one monosulfate sodium) is a selective inhibitor of the cannabinoid CB1 receptor. This neurosteroid, a key precursor in steroid hormone synthesis, can mitigate the effects of tetrahydrocannabinol (THC) by blocking its action at CB1 receptors. Additionally, Pregnenolone monosulfate sodium serves as a TRPM3 channel activator and has been shown to weakly activate TRPM1 channels. Its unique properties make it a valuable tool for investigating cannabinoid signaling and neuroprotective strategies against cannabis-related effects. -
Dopamine Receptors Blocker
Trifluoperazine is an antipsychotic agent primarily acting as a blocker of central dopamine receptors. It exhibits significant activity as a potent α1-adrenergic receptor antagonist and a NUPR1 inhibitor, demonstrating anticancer properties. Additionally, Trifluoperazine functions as a calmodulin inhibitor and inhibits P-glycoprotein, contributing to its diverse biological effects. This compound is utilized in research on schizophrenia and shows potential as a reversible inhibitor of influenza virus morphogenesis. -
CB1 Receptor Inhibitor
Pregnenolone monosulfate (3β-Hydroxy-5-pregnen-20-one monosulfate) is a selective inhibitor of the cannabinoid CB1 receptor. By inhibiting the effects of tetrahydrocannabinol (THC) mediated through the CB1 receptors, it offers potential neuroprotective properties against cannabis intoxication. Additionally, Pregnenolone monosulfate serves as a TRPM3 channel activator and exhibits weak activation of TRPM1 channels, making it valuable for research in neuropharmacology and cannabinoid signaling pathways. -
Icmt Inhibitor
Cysmethynil is an inhibitor of Isoprenylcysteine carboxylmethyltransferase (Icmt) with an IC50 of 2.4 μM. It disrupts RAS membrane binding and interferes with EGF signal transduction, leading to cell cycle arrest in the G1 phase and the induction of autophagy. Cysmethynil effectively inhibits the proliferation of PC3 prostate cancer cells and demonstrates synergistic effects with chemotherapeutic agents such as Paclitaxel and Doxorubicin. This compound is applicable for research into solid tumors, including prostate cancer. -
RDC-related Molecule
NOTA-NHS ester is a chelating agent that allows for the creation of radiolabeled compounds, specifically through coupling with T140 to form NOTA-T140. This compound can then be radiolabeled with Al[18F], enabling visualization of tumor uptake that correlates with CXCR4 expression levels. Al[18F]NOTA-T140 is particularly valuable for PET imaging studies of tumors. Additionally, NOTA-NHS ester serves as a versatile tool for fluorescent labeling in various biological applications. -
CXCR4 Targeting Peptide
Pentixafor is a synthetic peptide that targets the CXCR4 receptor, playing a critical role in various cellular processes, including cell migration and signaling. This compound can be labeled with 68Gallium (68Ga), enabling its application in positron emission tomography (PET) imaging for assessing CXCR4 expression in vivo. Additionally, Pentixafor serves as a vital component in the development of Radionuclide-Drug Conjugates (RDCs) for targeted cancer therapies. -
Somatostatin Receptor Ligand
DOTA-NOC (DOTA-Nal3-octreotide) is a high-affinity ligand for somatostatin receptor subtypes 2, 3, and 5. This compound is primarily utilized for radiolabeling with various radiometals, facilitating the development of radiopeptide imaging techniques. Additionally, DOTA-NOC plays a crucial role in the synthesis and research of Radionuclide-Drug Conjugates (RDCs), making it a valuable reagent in oncological and diagnostic studies. -
Endoradiotherapeutic vector
Anditixafortide is a CXCR4-targeting peptide derivative that functions as an endoradiotherapeutic vector. This reagent is primarily utilized in the synthesis and research of Radionuclide-Drug Conjugates (RDCs), leveraging its ability to selectively target CXCR4-expressing cells. Its application is significant in the field of targeted cancer therapies, facilitating precise delivery of therapeutic radionuclides to tumor sites. -
Liposome
DOTA Conjugated JM#21 derivative 7 is a CXCR4-targeting peptide conjugated with DOTA, designed for the synthesis of radioligands. When radiolabeled as 177Lu-DOTA, it demonstrates superior targeting of CXCR4-expressing tumors while exhibiting minimal uptake in non-targeted organs, except for the kidneys. This compound is ideal for research applications involving Radionuclide-Drug Conjugates (RDCs), facilitating advancements in targeted radiotherapy. -
GLP-1R Agonist
Naperiglipron is a potent agonist of the glucagon-like peptide-1 receptor (GLP-1R) with an EC50 of 1.14 nM for human GLP-1R. This compound has demonstrated significant efficacy in reducing blood glucose levels in GLP-1R knock-in mouse models, indicating its potential for managing type II diabetes mellitus (T2DM) and obesity. Additionally, Naperiglipron inhibits phosphodiesterase 10A1 activity with an IC50 of 7.43 μM and exhibits weak hERG inhibitory activity, making it relevant for various metabolic research applications. -
5-HT Reuptake Inhibitor
Mesembrine, also known as (+)-Mesembrine, is a potent inhibitor of the 5-HT transporter with a Ki value of 1.4 nM. This alkaloid, characterized by its aryloctahydroindole structure, also inhibits phosphodiesterase 4B (PDE4B) with an IC50 of 7.8 μM. Due to its selective targeting of serotonin reuptake, Mesembrine is valuable for studies related to mood regulation and various neuropsychiatric disorders, as well as investigations into PDE4B's role in inflammatory processes. -
PAFR Antagonist
Benafentrine maleate is an antagonist of the platelet activating factor receptor (PAFR) and a phosphodiesterase 4 (PDE4) inhibitor. This compound is primarily utilized in research focused on inflammation, neurological disorders, and cardiovascular diseases. By blocking PAFR activity, Benafentrine maleate has the potential to modulate various cellular responses associated with these conditions, making it a valuable tool in pharmacological studies. -
β₂-adrenergic receptor Agonist/PDE4 Inhibitor
GS-5759 is a dual-action compound functioning as a β₂-adrenergic receptor agonist and a phosphodiesterase 4 (PDE4) inhibitor. By activating the β₂ receptor, GS-5759 elevates intracellular cAMP levels, resulting in bronchial dilation. Additionally, its inhibition of PDE4 activity decreases cAMP degradation, thereby enhancing anti-inflammatory responses. This compound is relevant for research into respiratory disorders, particularly chronic obstructive pulmonary disease (COPD), demonstrating significant bronchodilatory and anti-inflammatory effects in preclinical models. -
LPA Pan-Antagonist
BrP-LPA sodium is a pan-antagonist of lysophosphatidic acid (LPA), displaying antagonistic activity against LPA1, LPA2, LPA3, and LPA4, with IC50 values of 4520 nM and 468 nM, respectively. It also exhibits partial agonistic activity for LPA5, with an EC50 of 1282 nM, and demonstrates inhibitory effects on autotaxin (ATX). BrP-LPA sodium has been shown to effectively inhibit migration and invasion of breast cancer cells and promotes tumor regression along with anti-angiogenic effects in a mouse breast cancer xenograft model. This reagent is valuable for research focused on breast cancer mechanisms and therapeutic strategies. -
Cardiac
UK-1745 is a cardiotonic agent that targets phosphodiesterase III, leading to increased intracellular levels of cyclic adenosine monophosphate (cAMP) in cardiomyocytes. This elevation enhances myocardial contractility while also exhibiting β-adrenergic receptor antagonism, which decreases cardiac oxygen consumption and mitigates calcium overload. Due to these properties, UK-1745 is a valuable tool for research applications focused on congestive heart failure and cardiac function modulation. -
LPA Antagonist/ATX Inhibitor
BrP-LPA is a potent lysophosphatidic acid (LPA) antagonist and autotoxin (ATX) inhibitor. It exhibits broad-spectrum antagonism against LPA receptors LPA1-4, resulting in decreased blood vessel density and reduced anxiety-like behaviors. Additionally, BrP-LPA demonstrates significant anticancer activity, effectively inhibiting cell proliferation in breast, colon, and lung cancer models. This compound is valuable for research focused on cancer biology and vasculature modulation. -
PDE-10A/A2AR Antagonist
PBF-999 is a dual antagonist of phosphodiesterase 10A (PDE-10A) and adenosine A2A receptors (A2AR). This compound exhibits significant modulation of intracellular signaling pathways, contributing to its potential in neuroscience research, particularly in studying disorders such as schizophrenia and Parkinson's disease. PBF-999 may facilitate insights into the therapeutic effects of PDE-10A and A2A receptor signaling in cognitive and motor function. -
GCGR Antagonist
Glucagon receptor antagonist-8 is a selective antagonist of the human glucagon receptor (GCGR) and p38 mitogen-activated protein (MAP) kinase. It exhibits IC50 values of 0.27 μM for GCGR and 0.16 μM for p38 MAP kinase, demonstrating significant inhibitory activity. This compound is applicable in research focused on metabolic disorders, glucose homeostasis, and signaling pathways associated with glucagon activity. -
Adenosine Receptor Antagonist
CGH2466 dihydrochloride is an orally active antagonist of adenosine receptors A1, A2B, and A3, exhibiting IC50 values of 19 nM, 21 nM, and 80 nM, respectively. This compound also inhibits p38 MAPK with an IC50 ranging from 187 to 400 nM and phosphodiesterase type 4D with an IC50 of 22 nM. CGH2466 dihydrochloride demonstrates significant anti-inflammatory properties in both in vitro and in vivo models, making it a valuable tool for research in asthma and chronic obstructive pulmonary disease (COPD). -
hA2A AR/hCA XII Inhibitor
hA2A/hCA XII modulator 1 is a potent inhibitor of the human A2A adenosine receptor (hA2AAR) and human carbonic anhydrase XII (hCA XII). It demonstrates high affinity with IC50 values of 6.4 nM for hA2AAR and 6.2 nM for hCA XII, while exhibiting selectivity against other adenosine receptor subtypes and carbonic anhydrases. This compound is valuable for cancer research, particularly in studies related to tumor microenvironment modulation and metabolic pathways involving adenosine signaling and carbonic anhydrase activity. -
CGRP Receptor Antagonist/5-HT1F Receptor Agonist
PCC0105005 is a potent CGRP receptor antagonist, exhibiting an IC50 of 1.01 nM, coupled with partial agonist activity at the 5-HT1F receptor, with an EC50 of 77.91 nM. This compound demonstrates significant efficacy in preclinical migraine models, effectively reducing the expression levels of CGRP and c-Fos proteins and inhibiting ERK and CREB phosphorylation. PCC0105005 is suitable for research focused on migraine pathophysiology and potential therapeutic interventions. -
hA3AR Probe
LUF7690 is a clickable and covalent affinity-based probe designed to target the human A3 adenosine receptor (hA3AR). This compound enables the detection and characterization of hA3AR in various granulocytes and other cell types, facilitating studies in receptor biology and signaling pathways. LUF7690 serves as a valuable tool for research applications focused on adenosine receptor functions and their roles in immunological responses. -
Fluorescent α1-Adrenergic Antagonist
BODIPY FL prazosin is a fluorescent α1-adrenergic antagonist, exhibiting Ki values of 14.5 nM and 43.3 nM for the α1a and α1b adrenergic receptors, respectively. This compound acts as a fluorescent ligand, with excitation and emission wavelengths at 485 nm and 535 nm. BODIPY FL prazosin is valuable for elucidating the subcellular localization and distribution of different α1-adrenoceptor subtypes in various biological contexts. -
CRTh2 Receptor Antagonist
AZ-11665362 is a selective antagonist of the CRTh2 (DP2) receptor, exhibiting a potent IC50 of 2.6 nM. While it demonstrates slight activity towards aldose reductase and the serotonin transporter, it shows negligible inhibition of COX-1 and COX-2 enzymes. This compound is primarily utilized in research focused on asthma and other inflammatory diseases, providing valuable insights into therapeutic pathways targeting eosinophilic inflammation. -
Dopamine-mimetic Probe
DAyne is a dopamine-mimetic probe that covalently interacts with proteins modified by dopamine oxidation products, such as dopaquinone, to create stable adducts. This compound is valuable for investigating the biochemical mechanisms underlying Parkinson’s disease, focusing on neurotoxicity and the modification of proteins. Its applications extend to exploring pathways affected by dopamine dysregulation, including endoplasmic reticulum stress and cytoskeletal instability. -
Glucagon-binding Fluorescent Probe
BD-105 is a glucagon-binding fluorescent probe with a dissociation constant (Ka) of 13.3 μM. This reagent displays significant changes in fluorescence intensity upon binding to glucagon, enabling the visualization of glucagon-secreting cells in various biological contexts. BD-105 selectively labels these cells while avoiding staining of insulin-secreting and non-endocrine control cells. It is an invaluable tool for imaging glucagon in live cells and tissues, facilitating studies in metabolic regulation and endocrine functions. -
Smoothened/Hedgehog Antagonist
AZD8542 is a potent Smoothened (SMO) antagonist that effectively disrupts the Hedgehog (Hh) signaling pathway, which is crucial in tumor progression. This compound is particularly relevant in oncology research, focusing on the interactions within the tumor microenvironment and the stroma compartment. AZD8542's ability to inhibit Hh pathway activity makes it a valuable tool in the study of cancer therapies and tumor biology. -
DPP-IV Inhibitor
AGFAGDDAPR is a competitive and orally active inhibitor of dipeptidyl peptidase-IV (DPP-IV). By inhibiting DPP-IV, AGFAGDDAPR increases levels of glucagon-like peptide-1 (GLP-1), which stimulates insulin secretion, enhances β-cell function, and suppresses excessive α-cell proliferation, resulting in beneficial anti-diabetic effects. This peptide is suitable for investigating mechanisms and therapeutic approaches related to type 2 diabetes. -
DPPIV Inhibitor
K579 is a potent dipeptidyl peptidase IV (DPPIV) inhibitor that exhibits oral bioactivity. This compound effectively mitigates blood glucose elevation by increasing plasma insulin levels and enhancing the active forms of glucagon-like peptide-1 (GLP-1). K579 is suitable for research applications focused on diabetes and glucose metabolism regulation. -
DPP-4 Inhibitor
(2S,4R)-Teneligliptin is a selective inhibitor of dipeptidyl peptidase IV (DPP-4). By enhancing the plasma concentration of active glucagon-like peptide-1 (GLP-1), it promotes insulin secretion in response to elevated blood glucose levels, demonstrating significant hypoglycemic activity. This compound holds promise for research applications focused on type 2 diabetes management and related metabolic disorders. -
Dipeptidyl Peptidase Inhibitor
Retagliptin hydrochloride is an effective inhibitor of dipeptidyl peptidase-4 (DPP-4), a key enzyme in glucose metabolism. This compound enhances glycemic control in type 2 diabetes by prolonging the action of incretin hormones, including glucagon-like peptide-1 (GLP-1). It is utilized in research applications focused on metabolic disorders and the regulation of insulin secretion. -
DPP4 Inhibitor
Cetagliptin is an orally active dipeptidyl peptidase 4 (DPP-4) inhibitor that also engages CYP2D6 with an IC50 value of 6 µM. By inhibiting DPP-4, cetagliptin effectively reduces the degradation of glucagon-like peptide-1 (GLP-1), contributing to the regulation of postprandial blood glucose levels. This compound is primarily utilized in type 2 diabetes mellitus research, making it a valuable tool for studying glucose homeostasis and metabolic responses. -
DPP-4 Inhibitor
DPP-4-IN-18 is a potent and selective Dipeptidyl Peptidase-4 (DPP-4) inhibitor with an IC50 of 27 nM. By inhibiting DPP-4, this compound prevents the degradation of glucagon-like peptide 1 (GLP-1), leading to increased levels of active GLP-1. DPP-4-IN-18 is primarily utilized in research focused on type 2 diabetes and related metabolic disorders.
