Catalog No.
Product Name
Application
Product Information
Citations
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H1 Receptor Antagonist
Chloropyramine is a competitive reversible antagonist of the H1 receptor. It exhibits anti-tumor activity, particularly in breast cancer models. This compound is valuable for research into allergic conditions, including conjunctivitis and bronchial asthma, providing insights into histamine-mediated physiological responses and potential therapeutic interventions. -
LPAAT-β Inhibitor
CT 32228 is an inhibitor of lysophosphatidic acid acyltransferase-β (LPAAT-β), showing significant inhibition of tumor cell growth. It exhibits IC50 values in the range of 0.1-0.8 μM across various leukemia cell lines and effectively induces caspase activation in DHL-4 and Ramos cells. In combination with Rituximab, CT 32228 promotes apoptosis and demonstrates a 50% growth delay in xenograft models. This reagent is suitable for research applications targeting acute leukemia. -
Platelet Aggregation Inhibitor
Ergosta-7,22-dien-3-one functions as a platelet aggregation inhibitor, derived from the fruiting bodies of Ganoderma lucidum. This compound is known to enhance nitric oxide production and promote the expression of specific genes alongside the synthesis of Toll-like receptors (TLRs), cytokines, chemokines, and cellular adhesion molecules in vitro. Ergosta-7,22-dien-3-one is valuable for research in hematology, inflammation, and cellular signaling pathways. -
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. -
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). -
Monosaccharide
Rhamnose (L-Rhamnose) is a naturally occurring deoxysugar that primarily targets inflammatory pathways. It has been shown to inhibit pro-inflammatory interleukins and matrix metalloproteinases (MMPs) in models of skin aging, highlighting its potential in anti-aging research. Additionally, Rhamnose enhances the phosphorylation of protein kinase A (PKA) substrates and hormone-sensitive lipase (HSL) in adipocytes, promoting PKA signaling and fat metabolism. Its ability to stimulate dopamine receptors and induce thermogenesis makes Rhamnose a valuable compound in obesity studies, while Rhamnose monohydrate is also utilized in research involving Ehrlich’s solid tumors and sarcomas. -
CXCR2 Agonist
Ac-Pro-Gly-Pro-OH acts as a CXCR2 agonist and is an endogenous degradation product of extracellular collagen. This compound demonstrates significant bactericidal activity through hydrogen peroxide generation and plays a role in inhibiting pulmonary inflammation while reducing immune cell apoptosis. Ac-Pro-Gly-Pro-OH promotes the secretion of IFN-γ and suppresses the levels of pro-inflammatory cytokines such as TNF-α and IL-6 in leukocytes. It is relevant for research applications in sepsis, chronic obstructive pulmonary disease, cystic fibrosis, bronchiolitis obliterans syndrome, severe asthma, idiopathic pulmonary fibrosis, and corneal ulcers, notably influencing neutrophil behavior and tissue remodeling processes. -
Soluble Guanylate Cyclase Stimulator
Zagociguat is a soluble guanylate cyclase (sGC) stimulator that is orally active and penetrates the blood-brain barrier. This compound enhances intracellular levels of cGMP, leading to regulation of blood pressure, improved neuronal function, reduced inflammatory responses, and neuroprotective effects. Zagociguat is primarily utilized in research focused on neurodegenerative diseases. -
CXCR2 Antagonist
Elubrixin tosylate is a selective and reversible antagonist of the CXCR2 receptor, functioning as an IL-8 receptor antagonist. This compound effectively inhibits neutrophil CD11b upregulation with an IC50 of 260.7 nM and neutrophil shape change with an IC50 of 310.5 nM. Its biological activity positions Elubrixin tosylate as a valuable tool in research aimed at understanding and treating inflammatory diseases, including inflammatory bowel disease and airway inflammation. -
Platelet Aggregation Inhibitor
5(S),15(S)-DiHETE is a platelet aggregation inhibitor that functions as an activated intermediate in the biosynthesis of specialized pro-resolving mediators. With an IC50 of 1.3 μM, it effectively reduces platelet aggregation. Additionally, 5(S),15(S)-DiHETE enhances the rate of biosynthesis for lipoxins A4 (LXA4) and B4 (LXB4), making it valuable for research applications in inflammation and resolution processes. -
CXCR2 Antagonist
Elubrixin is a potent and selective CXCR2 antagonist, functioning as a competitive and reversible inhibitor of the IL-8 receptor. It effectively impedes neutrophil CD11b upregulation with an IC50 of 260.7 nM and inhibits shape change with an IC50 of 310.5 nM. This compound is valuable in the study of inflammatory diseases, including inflammatory bowel disease and airway inflammation, facilitating insights into pathophysiological mechanisms and therapeutic interventions. -
LPA3 G-protein-coupled Receptor Agonist
(2S)-OMPT is a selective agonist for the LPA3 G-protein-coupled receptor, functioning as a lysophosphatidic acid analogue. This compound triggers downstream signaling pathways, including calcium influx and interleukin-6 (IL-6) release in cancer cells. Additionally, (2S)-OMPT activates critical signaling pathways such as MAPK and Akt. Its unique properties make it a valuable tool for research on ovarian cancer and other related studies. -
Formoterol Enantiomer
(S,S)-Formoterol is the (S,S)-enantiomer of Formoterol, primarily targeting beta-2 adrenergic receptors. This compound has been shown to enhance IL-4 production in mast cells, contributing to inflammatory responses associated with asthma. Its activities make it valuable for research in respiratory pharmacology and the study of asthma pathophysiology. -
CXCR2 Antagonist
Elubrixin hydrochloride is a potent, selective CXCR2 antagonist that operates as a competitive, reversible inhibitor of the IL-8 receptor. It effectively inhibits neutrophil CD11b upregulation and shape change, with an IC50 of 260.7 nM and 310.5 nM, respectively. This compound is valuable for research applications related to inflammatory diseases, including inflammatory bowel disease and airway inflammation. -
CXCR4 Antagonist
Burixafor hydrobromide is a potent CXCR4 antagonist with a pIC50 of 7.4, effectively inhibiting the binding of CXCL12 to the CXCR4 receptor. This compound antagonizes CXCL12-induced recruitment of Gαᵢ and β-arrestin2, thereby obstructing the downstream Gαᵢ-mediated inhibition of cAMP signaling. Burixafor hydrobromide is utilized in research for mobilizing CD34+ hematopoietic stem/progenitor cells from the bone marrow to peripheral blood, making it valuable in studies related to autologous hematopoietic stem cell transplantation. -
hD4 Receptor Antagonist
L 741742 hydrochloride is a highly selective antagonist of the human D4 dopamine receptor, exhibiting a Ki value of 3.5 nM for the D4 receptor while demonstrating much lower affinity for D3 and D2 receptors. This compound disrupts signaling pathways associated with PDGFRβ, ERK1/2, and mTOR, and impairs autophagic processes by affecting lysosomal function. Biologically, it induces G0/G1 cell-cycle arrest and apoptosis in various cell types and promotes neuronal differentiation in human neural stem cells. L 741742 hydrochloride is particularly relevant for research on schizophrenia and glioblastoma, demonstrating efficacy against glioblastoma neural stem cells and enhancing the effects of Temozolomide in vitro. -
mGluR2 Negative Allosteric Modulator
mG2N001 is a negative allosteric modulator of the metabotropic glutamate receptor mGluR2, exhibiting an IC50 of 93 nM and a binding affinity (Ki) of 63 nM. This compound demonstrates significant biological activity by modulating glutamatergic signaling pathways, making it valuable for neurological research. Additionally, its radioisotope [11C]mG2N001 is suitable for PET imaging, providing high brain heterogeneity and penetration, allowing for selective accumulation in mGluR2-rich regions, which enhances imaging contrast in neurobiological studies. -
mGluR5 Antagonist
AZD-2066 hydrochloride is a selective antagonist of the metabotropic glutamate receptor 5 (mGluR5) with the ability to penetrate the blood-brain barrier. This compound activates the brain-derived neurotrophic factor (BDNF) and trkB signaling pathway, making it relevant for research into neuropathic pain, major depressive disorder, and gastroesophageal reflux disease. AZD-2066 hydrochloride serves as a valuable tool for investigating the therapeutic potential of mGluR5 modulation in these conditions. -
H1 Receptor Blocker
(R)-(+)-Dimethindene maleate is a selective H1 receptor antagonist, displaying significant antihistaminic activity. It is utilized in research to study allergic responses and histamine-mediated mechanisms in various biological models, including porcine studies. This compound serves as a valuable tool for exploring the effects of histamine signaling and the therapeutic potential of H1 receptor blockade. -
βH Inhibitor AND H1 Receptor Antagonist
Desmethylastemizole is a β-hematin (βH) inhibitor and a Histamine H1 receptor antagonist. It exhibits potent antiplasmodium activity against Plasmodium falciparum, with IC50 values of 0.12, 0.11, and 0.06 μM for the Pf3D7, PfDd2, and PfItG strains, respectively. Additionally, Desmethylastemizole effectively blocks hERG K+ channels and inhibits histone-lysine N-methyltransferase EZH2 activity. This compound is relevant for research in long QT syndrome and malaria. -
H4/H1 Receptor Antagonist
H4R Antagonist 3 is a selective histamine H4 and H1 receptor antagonist with an EC50 of ≤10 mM. This compound is valuable for investigating the mechanisms underlying inflammatory, autoimmune, allergic, and ocular diseases. Its ability to modulate histamine receptor activity makes it a useful tool for research applications focused on these conditions. -
Histamine H3 Receptor Antagonist
Proxyfan is a potent antagonist of the histamine H3 receptor, exhibiting Ki values of 2.9 nM and 2.7 nM for rat and human H3 receptors, respectively. This compound demonstrates over 1000-fold selectivity for the H3 receptor compared to other histamine receptors. Proxyfan is useful in research applications focused on neurological disorders, cognitive enhancement, and sleep regulation, making it a valuable tool for studying histaminergic signaling pathways. -
Histamine H3 Receptor Antagonist
PF-03654764 is a potent and selective antagonist of the histamine H3 receptor, demonstrating Ki values of 1.2 nM for human H3 and 7.9 nM for rat H3 in whole cell assays. This compound exhibits significant potential in research applications related to allergies, particularly in the treatment of allergic rhinitis when combined with other antihistamines. Its oral bioactivity provides a valuable tool for investigating the role of histamine signaling in various physiological and pathological processes. -
Histamine H1 Receptor Antagonist
Diphenylpyraline is a potent histamine H1 receptor antagonist. This compound exhibits anticholinergic and antiallergic properties, making it effective as an orally active antihistamine. Diphenylpyraline is applicable in research focused on allergic conditions, including rhinitis and hay fever, as well as pruritic skin disorders.
