Catalog No.
Product Name
Application
Product Information
Citations
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5-HT4 Receptor Agonist
Relenopride hydrochloride is a selective agonist of the 5-HT4 receptor, exhibiting a Ki value of 4.96 nM, which confirms its high affinity for this target. With significantly lower affinities for the 5-HT2A and 5-HT2B receptors, Relenopride hydrochloride is a valuable tool for studying gastrointestinal physiology. It is primarily utilized in research on enhancing gastrointestinal motility and investigating conditions related to digestive function. -
α2B/C-Adrenergic Receptor Antagonist
ARC 239 is a selective antagonist of the α2B and α2C adrenergic receptors, exhibiting a pKi of 7.06 for rat kidney α2B and 6.95 for human α2C. In addition, ARC 239 inhibits the 5-HT1A receptor with a Ki value of 63.1 nM. This compound is valuable in research involving adrenergic signaling pathways and the modulation of neurotransmitter systems, making it suitable for studies on cardiovascular function and psychiatric disorders. -
5-HT2C Agonist
5-HT2C agonist-3 is a selective agonist for the 5-HT2C receptor, exhibiting an EC50 of 24 nM and a Ki of 78 nM. This compound demonstrates antipsychotic-like properties and effectively inhibits amphetamine-induced hyperactivity. It serves as a valuable tool for research into neuropharmacology and the modulation of serotonergic systems. -
5-HT/Serotonin Receptors Ligand
1-(2-Methoxyphenyl)piperazine hydrochloride is a ligand targeting 5-HT (serotonin) receptors, crucial for the development of various antipsychotic agents. Its high affinity for serotonin receptors makes it a valuable compound in synthesizing pharmacological agents, such as Piperazine phosphate, Piperazine citrate, and Fluphenazine dihydrochloride. Additionally, this reagent can be utilized in the synthesis of Rifampicin, contributing to studies in neuroscience and psychiatric research. -
Ziprasidone Impurity
Keto Ziprasidone is a known impurity of the antipsychotic agent Ziprasidone, which functions primarily as a combined antagonist of serotonin (5-HT) and dopamine receptors. This compound is crucial for research applications focusing on drug metabolism and pharmacokinetics, particularly in understanding the potential effects of impurities on therapeutic efficacy and safety profiles. Its analysis can aid in the development of quality control measures in pharmaceutical formulations. -
5-HT(6/7/2A)/ Dopamin D2 Receptors Antagonist
5-HT6/7 Antagonist 1 is a potent antagonist of the 5-HT6, 5-HT7, and D2 receptors, exhibiting selectivity that spares M1 receptors and hERG channels. This compound's multifunctional activity makes it valuable for research into neuropharmacology and the modulation of serotonergic and dopaminergic systems. It provides a useful tool for studying disorders related to these receptor pathways, including anxiety, depression, and schizophrenia. -
5HT-4/5HT-3 Antagonist
Lintopride is a benzamide that acts as a potent antagonist of the 5HT-4 receptor, with moderate antagonistic properties at the 5HT-3 receptor. This compound enhances gastric emptying, stimulates motility in the antrum and duodenum, and accelerates intestinal transit in animal models. Additionally, Lintopride significantly increases the basal tone of the lower oesophageal sphincter, highlighting its potential applications in gastrointestinal research and therapy. -
Ziprasidone Impurity
Hydroxy ziprasidone is a known impurity of the antipsychotic agent ziprasidone, which functions primarily as a combined antagonist of both serotonin (5-HT) and dopamine receptors. This compound is useful for researchers studying the pharmacological properties and metabolic pathways of ziprasidone, as well as for quality control in the synthesis of pharmaceutical formulations. Its presence can provide insights into the drug's safety, efficacy, and potential side effects. -
Cannabinoid Receptor Agonist
AM9405 is a selective agonist for cannabinoid receptor type 1 (CB1) and serotonin type 3 (5-HT3) receptors. It demonstrates potent inhibitory effects on twitch contractions in the ileum and colon, with half-maximal inhibitory concentrations (IC50) of 45.71 nM and 0.076 nM, respectively. AM9405 is valuable for research in gastrointestinal motility and cannabinoid signaling pathways. -
5-HT5A Receptor Probe
UCSF648 is a chemical probe targeting the 5-HT5A serotonin receptor. It demonstrates weak activation of the ADRA2A and MTNR1A receptors, making it valuable for studies investigating serotonin signaling pathways. This reagent is suitable for research applications related to neuropharmacology and the modulation of serotonin receptor activity. -
5-HT1A Receptor Agonist
Tandospirone hydrochloride is a selective partial agonist of the 5-HT1A receptor, exhibiting a Ki value of 27 nM. This compound displays notable anxiolytic and antidepressant properties, making it valuable in the study of central nervous system disorders. Its unique action at the 5-HT1A receptor contributes to the understanding of underlying mechanisms related to anxiety and depression, facilitating research aimed at developing novel therapeutic approaches. -
Dopamine D2/D3/5-HT7 Receptor Inhibitor
LB-102 is an orally bioavailable inhibitor of dopamine D2, D3, and 5-HT7 receptors. It exhibits significant antagonistic activity, making it a valuable tool for investigating the neurochemical pathways involved in schizophrenia and other psychiatric disorders. This compound is useful for studies aimed at understanding the role of these receptors in various neuropsychiatric conditions. -
5-HT/DA Receptor Antagonist
Ziprasidone mesylate trihydrate is an orally active antagonist of serotonin (5-HT) and dopamine (DA) receptors, primarily targeting the 5-HT2A and D2 receptor subtypes. With a high affinity for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM), and 5-HT1A (Ki=3.4 nM), this compound is significant for studies related to mood disorders, schizophrenia, and neuropharmacology. Ziprasidone mesylate trihydrate serves as a valuable tool for exploring receptor mechanisms and assessing therapeutic effects in relevant biological models. -
TAAR1/5-HT1A Agonist
Ulotaront is a novel TAAR1 and 5-HT1A agonist that operates through a distinct mechanism separate from traditional D2 and 5-HT2A pathways. This compound exhibits significant antipsychotic-like properties, making it a valuable tool for researching schizophrenia and related neuropsychiatric disorders. Its unique profile allows for exploration of alternative treatment strategies that may enhance therapeutic options for psychiatric conditions. -
5-HT Receptor Antagonist
Clocapramine is a selective antagonist of the 5-HT2A receptor, with additional inhibitory effects on D2 dopamine receptors. This compound exhibits notable properties in modulating serotonin and dopamine signaling, making it relevant for neuropharmacological research. Clocapramine can be utilized in studies related to psychiatric disorders, including depression and schizophrenia, as well as the characterization of receptor interactions in neural pathways. -
PKC Inhibitor
NA 0345 is a potent protein kinase C (PKC) inhibitor, exhibiting IC50 values of 70 nM in the presence of 12-O-tetradecanoyl-13-acetate and 110 nM in its absence. This compound selectively inhibits PKC activity, effectively reducing the positive inotropic effects associated with α1-adrenergic receptors. NA 0345 is useful in research applications aimed at elucidating the role of PKC in cardiovascular function and signal transduction pathways. -
Protein Kinase C Inhibitor/LTD4 Antagonist
LY 170198 is a potent protein kinase C inhibitor and LTD4 antagonist. This compound exhibits significant biological activity relevant to studies on tumor promotion, oncogene activation, and protein phosphorylation. Additionally, it is valuable for investigating feedback mechanisms in signal transduction pathways and cellular responses to growth factors, making it a useful tool for cancer research and related fields. -
PAD4 Inhibitor
JBI-589 is a non-covalent inhibitor selectively targeting the PAD4 isoform. This compound effectively reduces CXCR2 expression and inhibits neutrophil chemotaxis, making it instrumental in the study of inflammatory processes. JBI-589 demonstrates potential in diminishing primary tumors and metastases while enhancing the efficacy of checkpoint inhibitors. It is suitable for various applications in cancer research. -
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. -
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. -
SSTR2 Ligand
Edotreotide is a selective ligand for the somatostatin receptor subtype 2 (SSTR2), capable of competitive binding to the receptor. It facilitates the targeted delivery of radionuclides, such as 90Y, 177Lu, and 68Ga, to SSTR-positive tumors, promoting tumor cell apoptosis through the emission of β rays. Edotreotide's strong tumor-targeting capabilities make it a valuable tool in the development of radionuclide-drug conjugates (RDCs) and in research applications focused on neuroendocrine tumors, including metastatic carcinoids and lung and thymus neuroendocrine tumors. -
SSTR2 Antagonist
Satoreotide is a selective antagonist of the somatostatin receptor subtype 2 (SSTR2). It has demonstrated potential in enhancing neuroendocrine tumor imaging when conjugated with radiolabeled chelators. This compound is significant in research applications focused on the development of targeted imaging agents for diagnostic purposes in oncological settings. -
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). -
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. -
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. -
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.
