Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Peptide Drug Conjugate
DOTA-EB-TATE is a peptide drug conjugate composed of a somatostatin (SST) peptide derivative, DOTA-octreotate, conjugated to an Evans blue analog. This compound enhances the pharmacokinetics of somatostatin receptor subtype 2 (SSTR2) analogs while decreasing associated toxicity in peptide receptor radionuclide therapy (PRRT). DOTA-EB-TATE is also applicable in the synthesis and research of radionuclide-drug conjugates (RDCs), making it valuable for investigations in targeted cancer therapies. -
Tumor Tracer
Pentetreotide is a somatostatin analog conjugated with diethylenetriaminopentaacetic acid (DTPA) and labeled with indium. It serves as a tumor tracer, primarily utilized in nuclear medicine imaging to detect neuroendocrine tumors and their metastases. The compound's ability to bind to somatostatin receptors enables effective scintigraphy, making it a valuable tool in oncological diagnostics and research applications focused on neuroendocrine malignancies. -
Antitumor Agent
Tyr3-Octreotate is a somatostatin analog that specifically targets somatostatin receptors. It demonstrates significant uptake in tumor tissues, allowing for effective labeling with radioactive metals, which enhances its antitumor efficacy. This compound is valuable for the development and research of Radionuclide-Drug Conjugates (RDCs) in cancer therapy. -
Biochemical Assay Reagent
DOTA-Octreotide is a chelator-conjugated peptide targeting somatostatin receptors, primarily used in biochemical assays. It facilitates the research of cancer by enabling the synthesis of radionuclide-drug conjugates (RDCs) when combined with radioactive isotopes. DOTA-Octreotide is crucial for studies in tumor imaging and targeted radiotherapy applications, enhancing the understanding of receptor-targeted approaches in oncology research. -
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. -
Tumor Tarcer
Depreotide is a novel tumor targeting agent that selectively binds to somatostatin receptors, facilitating effective imaging when complexed with technetium-99m (99mTc-depreotide). This compound plays a crucial role in somatostatin receptor imaging, aiding in the diagnosis and research of various tumors. Additionally, depreotide can be employed in the synthesis and investigation of Radionuclide-Drug Conjugates (RDCs) for targeted therapeutic applications. -
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. -
Serine Aminopeptidase
Dipeptidyl Peptidase IV, Porcine Kidney is a serine aminopeptidase that plays a vital role in glucose metabolism. This enzyme specifically hydrolyzes gastric inhibitory peptide (GIP) and glucagon-like peptide-1 (GLP-1), which are key incretins involved in insulin release regulation. Its biological activity makes it a valuable tool for research in diabetes, metabolism, and related endocrine functions. -
DPP-IV Inhibitor
Gosogliptin hydrochloride is a selective, competitive inhibitor of DPP-IV, an enzyme crucial for the degradation of incretin peptides such as GLP-1 and glucose-dependent insulinotropic polypeptide. This compound exhibits rapid and reversible inhibition of plasma DPP-4 activity, leading to enhanced insulin secretion and improved glucose tolerance. Gosogliptin hydrochloride is primarily utilized in research focused on diabetes and metabolic disorders, providing valuable insights into glucose regulation and insulin dynamics. -
DPP-4 Inhibitor
DPP-4-IN-10 is a potent DPP-4 inhibitor that acts to prevent the degradation of glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP). By inhibiting DPP-4, this compound may enhance glycemic control in individuals with type 2 diabetes mellitus (T2DM). Its oral bioavailability makes it suitable for pharmacological studies focused on glucose metabolism and diabetes management. -
DPP-IV Inhibitor
ASP8497 is a competitive inhibitor of dipeptidyl peptidase IV (DPP-IV), which plays a critical role in glucose metabolism. This compound effectively reduces blood glucose levels and elevates plasma active GLP-1 and insulin concentrations without inducing hypoglycemia in fasted normal mice. ASP8497 is suitable for research applications focused on antihyperglycemic mechanisms and glucose regulation. -
DPP-IV Inhibitor
Carmegliptin is a potent and orally active DPP-IV inhibitor, demonstrating an IC50 value of 6.8 nM for human DPP-IV. By binding to the S1 pocket of DPP-IV, it effectively inhibits the degradation of GLP-1, leading to increased plasma insulin levels, improved glucose tolerance, and alleviation of hyperglycemia. Carmegliptin serves as a substrate for human P-glycoprotein without inhibiting the transporter, exhibiting low in vitro cell permeability. This compound is valuable for research focused on type 2 diabetes and non-insulin-dependent diabetes mellitus. -
DPP-4 Inhibitor
16-Hydroxycleroda-3,13-dien-15,16-olide is a potent dipeptidyl peptidase 4 (DPP-4) inhibitor, targeting the serine protease class of enzymes. This clerodane diterpene demonstrates key biological activities, including the down-regulation of lipopolysaccharide (LPS)-induced ERK phosphorylation in myocytes and inhibition of glucagon-like peptide-1 (GLP-1) induced protein kinase A (PKA) expression. Additionally, it exhibits hypolipidemic, hepatoprotective, and hypoglycemic effects, making it a valuable compound for research in metabolic and cardiovascular diseases. -
DPP-IV Inhibitor
Carmegliptin hydrochloride is a potent DPP-IV inhibitor, exhibiting a human DPP-IV IC50 of 6.8 nM. By binding to the S1 pocket of DPP-IV, it prevents the degradation of GLP-1, leading to increased plasma insulin levels, improved glucose tolerance, and relief from hyperglycemia. This compound can serve as a valuable reagent for research into type 2 diabetes and non-insulin-dependent diabetes mellitus, providing insights into GLP-1 modulation and its effects on metabolic regulation. -
DPP-IV Inhibitor
TS-021 is a selective, orally active, reversible DPP-IV inhibitor with long-lasting effects. It demonstrates significant selectivity against DPP-8 and DPP-9, exceeding 600-fold and 1,200-fold, respectively, as well as a greater than 15,000-fold selectivity over other peptidases. With an IC50 value of 5.34 nM for DPP-IV inhibition in human plasma, TS-021 is effective in enhancing active GLP-1 levels and exhibits potent antihyperglycemic activity, making it valuable for research in diabetes and metabolic disorders. -
Stable Isotope
Doxofylline-d4 is a deuterium-labeled derivative of Doxofylline, which functions primarily as an antagonist of the adenosine A1 receptor while also inhibiting phosphodiesterase IV. This reagent is valuable for studying pharmacokinetics and metabolic pathways in research involving adenosine receptor modulation and phosphodiesterase activity. Its stable isotope labeling allows for enhanced detection and quantification in various analytical applications. -
Adenosine Receptor Antagonist
Acefylline piperazine is an adenosine receptor antagonist known for its ability to activate peptidylarginine deiminase (PAD). This xanthine derivative exhibits significant bronchodilator and cardiac stimulant properties, while also inhibiting rat lung cAMP phosphodiesterase isoenzymes. As a result, Acefylline piperazine is a valuable tool in asthma research and studies exploring pulmonary function and cardiovascular effects. -
Stable Isotope
Rimonabant-d10 is a deuterium-labeled analog of Rimonabant, a highly potent and selective antagonist of the central cannabinoid receptor (CB1) with a Ki of 1.8 nM. This compound not only exhibits strong brain penetration but also inhibits Mycobacterial membrane protein Large 3 (MMPL3). Rimonabant-d10 serves as a valuable tool for studying cannabinoid receptor signaling and the role of CB1 in various biological processes, as well as for applications in mycobacterial research. -
Cannabinoid
O,O-Dimethyl-cannabigerol primarily targets cannabinoid receptors and is derived from Cannabis sativa. It exhibits antibacterial activity against drug-resistant strains of Staphylococcus aureus, demonstrating a minimum inhibitory concentration (MIC) of 1 to 2 μg/mL. As a nonpsychoactive constituent, O,O-Dimethyl-cannabigerol is valuable for research into therapeutic applications of cannabinoids, particularly in antimicrobial studies. -
Stable Isotope
(R)-Propranolol-d7 is a deuterated derivative of (R)-Propranolol, serving as a stable isotope-labeled compound. This reagent is invaluable for pharmacokinetic studies and metabolic pathway analysis, enabling the tracking of drug metabolism and distribution in biological systems. Researchers can utilize (R)-Propranolol-d7 in studies focused on cardiovascular research, anxiety treatments, and the mechanisms of action associated with beta-adrenergic receptors. -
Platelet Aggregation Inhibitor
SCH 38519 is a potent platelet aggregation inhibitor that effectively inhibits thrombin-induced aggregation of human platelets, exhibiting an IC50 of 68 μg/mL. In addition to its antiplatelet activity, SCH 38519 demonstrates antibacterial properties against both Gram-positive and Gram-negative bacteria. This compound is valuable for research applications focused on thrombosis, cardiovascular diseases, and bacterial infections. -
HK Inhibitor
Antibacterial agent 241 is a histidine kinase (HK) inhibitor with IC50 values of 14 μM for CckA and 238 μM for PhoQ. It demonstrates moderate antibacterial activity against various bacterial strains, including E. coli DC2, Bacillus cereus, and Bacillus subtilis, with minimum inhibitory concentration (MIC) values ranging from 12 to 74 μg/mL. This compound is suitable for research applications targeting bacterial signaling pathways and antibiotic resistance mechanisms. -
CCK2R Antagonist
Ceclazepide is a cholecystokinin-2 receptor (CCK2R) antagonist that serves as an orally active inhibitor of Mycobacterium abscessus. This compound effectively reduces acid secretion in rat models and demonstrates significant suppression of both wild-type and multiple subspecies of M. abscessus. Importantly, Ceclazepide inhibits the growth of M. abscessus within macrophages while maintaining cell integrity, making it a valuable tool for research into mycobacterial infections and related therapeutic strategies. -
β-Adrenoceptor Blocker
Propranolol is a non-selective β-adrenoceptor antagonist that effectively crosses the blood-brain barrier. It exhibits high affinity for both β1 and β2 adrenergic receptors, with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol has demonstrated inhibitory activity against [3H]-DHA binding in rat brain membrane preparations, with an IC50 of 12 nM. This compound is commonly employed in research related to hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy. -
Somatostatin Receptor Activator
Reltecimod is a somatostatin receptor activator that modulates the immune response by targeting the CD28/B7-2 co-stimulatory pathway. This compound exhibits protective effects against various bacterial infections, their toxins, and ionizing radiation. Reltecimod is particularly relevant for research into necrotizing soft-tissue infections (NSTIs), providing insights into therapeutic interventions and immune modulation.
